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1.
Cureus ; 16(7): e63781, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38974403

RESUMO

Pulmonary large-cell neuroendocrine carcinoma (LCNEC) is a rare but aggressive malignancy of the lung. Its nonspecific presentation and propensity for severe disease at the time of diagnosis create challenges in treatment. We report a case of an asymptomatic 61-year-old female who was incidentally found to have a pulmonary nodule after a fall. Upon further workup, she was found to have an aggressive LCNEC. The patient underwent a robotic-assisted left upper lobectomy, which was complicated by left lower lobe bronchus kinking and post-obstructive atelectasis, warranting further management by thoracic surgery. The patient additionally underwent video-assisted thoracoscopic surgery (VATS), open thoracotomy, pneumopexy, and bronchial stenting. This case highlights the need for strategies for early detection in at-risk populations. A multidisciplinary approach, which may involve both medical and surgical subspecialties, is essential in the management of this complex disease from the time of diagnosis to follow-up postoperatively to achieve the best clinical outcome.

2.
Cureus ; 16(7): e64387, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-39007020

RESUMO

Cryptococcal meningitis, a severe fungal infection of the central nervous system, is usually found in immunocompromised patients, especially those with human immunodeficiency virus/acquired immunodeficiency syndrome. Its occurrence in immunocompetent individuals is rare and the presentation can be nonspecific. We present a case of cryptococcal meningitis in a young, immunocompetent male with a known history of intravenous drug abuse who was also found to have hepatitis C during admission. Induction therapy with amphotericin B and flucytosine was completed for 14 days. This shorter duration was considered as he had a good clinical response with rapid improvement in mental status and intracranial pressure with an extraventricular drain and negative repeat cerebrospinal fluid (CSF) culture. However, during the consolidation phase with fluconazole, the patient developed new neurologic symptoms and the induction phase had to be re-initiated for a total of 28 days. The patient likewise required the re-placement of an extraventricular drain and the creation of a ventriculoperitoneal shunt due to persistent CSF accumulation and increased intracranial pressure. He was eventually discharged on fluconazole for a planned consolidation phase of eight weeks, followed by a prolonged maintenance phase, but the patient was lost to follow-up.

3.
Cureus ; 16(7): e64085, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38979027

RESUMO

The coronavirus disease 2019 (COVID-19) pandemic has unveiled numerous clinical challenges, particularly its association with thrombotic events, which significantly contribute to morbidity and mortality. While thrombotic complications such as arterial and venous thromboembolism (VTE) are well-documented, instances of intracardiac thrombus are notably rare. This case report discusses a 60-year-old male with COVID-19 who came to the hospital due to respiratory distress. Despite treatment with remdesivir, the patient's condition worsened prompting further workup. His nuclear medicine (NM) ventilation-perfusion scan was inconclusive, but a 2D echocardiogram showed an intracardiac thrombus in the right atrium (RA) and right ventricle (RV). As the patient's condition worsened, necessitating a transition from nasal cannula to high-flow nasal cannula, a decision was made to treat him with intravenous (IV) thrombolytic therapy. The patient received 100 mg IV alteplase and IV heparin, resulting in significant respiratory improvement and symptomatic relief. A repeat echocardiogram after 48 hours showed normal ejection fraction and complete thrombus resolution. In conclusion, this case highlights the complex link between COVID-19 infection and prothrombotic states, leading to severe complications such as intracardiac thrombus in transit. The successful treatment of this patient through a multidisciplinary approach and thrombolytic therapy underscores the importance of prompt recognition and intervention in high-risk cases.

4.
Cureus ; 16(6): e61908, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38975411

RESUMO

Oral ulcers are one of the most common complaints seen by general practitioners in their offices. Recurrent aphthous stomatitis affects roughly 20% of the general population. When ulcers persist despite conventional treatment, it is crucial to consider systemic diseases such as Behçet's disease to prevent delays in care. Early recognition and appropriate management of underlying conditions are essential for improving patient outcomes and quality of life. We present a case of a 41-year-old Scottish male who came in with complaints of recurrent oral ulcers and oral thrush. Initial treatment by an infectious disease specialist resolved the oral thrush but not the ulcers. Despite further treatment attempts for three years, including biopsy and antiviral therapy, ulcers persisted. Finally, referral to rheumatology led to comprehensive autoimmune testing, revealing positive HLA B51 and a diagnosis of Behçet's disease. Treatment with topical steroids and colchicine yielded significant improvement.

5.
Cureus ; 16(6): e61807, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38975437

RESUMO

Trichilemmal carcinoma (TC) is a rare, low-grade, malignant adnexal tumor. It is usually less than 3 cm long and arises from the external root sheath of the hair follicle, most commonly in sun-exposed areas of the body. The treatment of choice is wide local excision with tumor-free margins. We present an 88-year-old male patient who presented with an incidental large, dry, fumigating mass on his scalp for a one-year duration requiring surgical excision. The mass, initially thought to be a benign sebaceous cyst, was a 12-cm trichilemmal carcinoma diagnosed based on the histopathologic features of the mass. The specimen was composed of keratinaceous material and necrotic debris. The viable tumor was consistent with atypical squamous proliferation. The mass was fully excised down to the scalp on the first encounter, leaving no further tissue to excise. The patient's scalp site remained clean and without bleeding or recurrence. Currently, there is an increasing incidence of trichilemmal carcinoma. The pathophysiology of this disease is still unclear. The radiation from the sun is one of the factors that causes the growth of the lesions due to its location and distribution. Trichilemmal cysts can also transform into malignant trichilemmal carcinomas due to the p53 deletion. TC has a non-aggressive course despite its aggressive histology. The prognosis is generally good as it has low metastatic potential, like cutaneous squamous cell carcinoma. However, TC with metastasis has a poor prognosis, and there is no consensus yet on treatment. For non-metastatic TC, simple surgical excision with adequate (0.5-1 cm) margins is an effective treatment. Different studies use different margins, and there is no consensus on the measurement for margin excision. Regular follow-up is recommended, but further studies regarding follow-up schedules are needed. Furthermore, despite the common use of chemotherapy in cases of malignant TC, only a limited number of studies have explored this treatment approach. Given the increasing incidence of the disease, we highly recommend more research to address this knowledge gap.

6.
Cureus ; 16(5): e60418, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38882999

RESUMO

Pericardial effusion, a clinical condition characterized by an abnormal accumulation of fluid in the pericardial cavity, has multiple etiological factors. One of the prominent causes is malignant effusion. The patient is a 69-year-old female with a past medical history of Crohn's disease, melanoma status post-resection, and osteoarthritis. She presented with complaints of abdominal discomfort, shortness of breath on exertion, and lower extremity swelling for the past 2-3 days. She was recently discharged four days before this visit after being treated for a viral infection. A physical examination was significant for tachycardia, muffled heart sounds, abdominal distention, and bilateral lower extremity swelling. Labs were in the normal range except for elevated liver enzymes and sodium of 130 mmol/L. A chest X-ray revealed a small bilateral effusion; a bedside echocardiogram showed an ejection fraction greater than 70% and a large pericardial effusion >2 cm, consistent with cardiac tamponade. Emergent pericardiocentesis was performed with the drainage of 250 milliliters of hemorrhagic fluid, which was sent for diagnostic studies. Post-procedure echo on the next day showed an EF of 35-40% and no recurrent pericardial effusion. The workup for connective tissue disease was negative except for elevated antinuclear antibodies (ANA). CT of the abdomen and pelvis revealed gastric wall thickening with no solid organ mass. Her pericardial fluid studies were consistent with exudative etiology and positive for atypical lymphoid cells, leading to the diagnosis of diffuse large B-cell lymphoma. Diffuse large B-cell lymphoma is the most common type of non-Hodgkin lymphoma. Malignant pericardial effusion is common due to solid organ malignancy; however, it is rare with diffuse large B cell lymphoma (DLBCL). We present an intriguing case where pericardial effusion was the precursor to the eventual diagnosis of DLBCL, highlighting the complexity and diverse manifestations of this lymphoma subtype.

7.
Cureus ; 16(5): e60300, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38746487

RESUMO

Symptomatic cerebral infarcts with cryptogenic ischemic stroke pose diagnostic challenges due to unknown etiology. Notably, up to half of young individuals with cryptogenic stroke exhibit patent foramen ovale (PFO), while finasteride, which is used for male pattern baldness, elevates testosterone levels, potentially increasing the risk of thrombosis. Here, we present a case of thalamic infarction in a 21-year-old male devoid of cerebrovascular risk factors but with PFO and finasteride use. The patient presented with short-term memory issues, otherwise lacking medical history or substance use. Examination revealed neurological deficits, with imaging indicating a left thalamic infarct. Subsequent investigations identified PFO, prompting referral for closure, yielding symptomatic improvement. Furthermore, discontinuation of finasteride was advised due to its thrombotic association. Finasteride's inhibition of 5-alpha reductase 2 increases testosterone conversion to estrogen, potentially promoting thrombosis. Finasteride use can cause thrombotic events, emphasizing its risk. In conclusion, young embolic stroke patients warrant PFO evaluation alongside hypercoagulable workup, with closure benefiting those under the age of 55. Additionally, discontinuing finasteride may mitigate thrombosis risk.

8.
Cureus ; 16(4): e59316, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38694661

RESUMO

Rhabdomyolysis is characterised by muscle breakdown and the release of myoglobin. It is a potentially serious condition that can lead to acute kidney injury (AKI). Factors, such as ischemia, trauma, muscle compression and drug toxicity, can trigger muscle breakdown. Treatment involves aggressive fluid resuscitation to maintain urine output and prevent renal injury. Severe cases with AKI may require temporary renal replacement therapy, such as haemodialysis. It has also been proposed that dialysis can speed up recovery by removing myoglobin that is secreted into the circulation by injured muscles. We present a case of a patient with alcohol abuse and prolonged immobility leading to severe rhabdomyolysis requiring hemodialysis. Our aim is to emphasise the importance of timely identification, and appropriate management of severe rhabdomyolysis not improving on fluids may require HD as soon as possible in order to minimise complications.

9.
Cureus ; 16(2): e54824, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38529436

RESUMO

Penile calciphylaxis is a rare presentation of calcific uremic arteriolopathy and can be a life-threatening condition usually seen in patients with end-stage renal failure with hemodialysis. The clear etiopathogenesis of calciphylaxis is not fully understood, but it is postulated to be characterized by the accumulation of calcium in the microvessels of adipose tissue and skin, which leads to ischemia and necrosis, causing painful ulcerations, and could potentially be complicated by sepsis and mortality. End-stage renal disease (ESRD) is one of the major risk factors for penile calciphylaxis. In this report, we describe a case of a 53-year-old Hispanic male patient with ESRD and diabetes on hemodialysis, who presented with a five-day history of acute, severe, burning, non-radiating pain to the head of his penis associated with black discoloration. He was diagnosed with penile calciphylaxis and received a combination of conservative and surgical interventions, resulting in a highly positive outcome marked by complete healing of the scar without any reported complications.

10.
Cureus ; 15(7): e42326, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37614259

RESUMO

Monkeypox (MPX) virus is endemic in Africa. However, since May 2022, many cases have been reported worldwide in many non-endemic regions as well. The virus usually spreads from animals to humans or from humans to humans through respiratory droplets or after contact with infected lesions. In the recent outbreak of MPX, many cases did not have any travel history to endemic areas and were reported in men who have sex with men (MSM) along with the diagnosis of other sexually transmitted diseases (STDs). However, MPX is not yet considered a sexually transmitted infection (STI), even though a relationship between MPX and other STIs may exist with a possible facilitating action on their spreading. We present a similar case of MPX infection in an MSM patient with concomitant HIV and syphilis infections and no travel history to an endemic area.

11.
Cureus ; 14(4): e23983, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35547409

RESUMO

Spontaneous coronary artery dissection (SCAD) is an infrequent presentation of acute myocardial infarction in young women and denotes the non-atherosclerotic separation of the coronary artery wall. Precipitating causes include fibromuscular dysplasia, postpartum hormonal changes, multiparity, connective tissue diseases like Marfan syndrome, autoimmune conditions, and hormonal therapy. It is often underdiagnosed due to a low index of suspicion based on age and gender bias as well as knowledge about different angiographic variants in SCAD. Intracoronary imaging with optical coherence tomography (OCT) or intravascular ultrasound (IVUS) is used for patients where coronary angiography fails to secure a diagnosis to increase the diagnostic yield. The mainstay of stable SCAD is conservative management. However, there are no definitive guidelines due to limited clinical experience. Treatment involving percutaneous coronary intervention (PCI), coronary artery bypass grafting (CABG), fibrinolytic therapy, and mechanical hemodynamic support should be individualized depending upon clinical presentation, type, and extent of dissection, hemodynamic instability, critical anatomy involvement, and the extent of ischemic myocardium. We are presenting a case of a young female who presented with non-ST-elevation myocardial infarction (NSTEMI) that progressed to ST-elevation myocardial infarction (STEMI). A coronary angiogram showed a tortuous left anterior descending artery (LAD) with a distal 100% occlusion due to SCAD. PCI was attempted but the guidewire could not be navigated intraluminally past the occlusion. CABG was not pursued due to the distal location of the occlusion and lack of visualization of the distal vessel. Our case provides a useful learning opportunity for physicians who may come across similar clinical presentations. In patients with high-risk features of SCAD who are deemed inoperable, timely and appropriate medical management may be a useful alternative for PCI/CABG and the recurrence rates of SCAD are very low.

12.
Cureus ; 13(7): e16345, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34395126

RESUMO

A 61-year-old male with no past medical history presented with intense abdominal pain for three days, associated with hematochezia, nausea, and non-bloody vomiting. CT scan of the abdomen showed distended small bowel, diffuse lymphadenopathy, and intussusception of the distal ileum into the cecum with obstruction. Ileocolic resection and histopathological staining confirmed the diagnosis of follicular lymphoma and appropriate treatment was initiated. Intussusception is a condition that involves the invagination of the proximal segment of a bowel tract into its contiguous distal segment as a result of enthusiastic or impaired peristalsis. Only 5% of the total intussusception cases are found in adults. Most cases in adults are caused by pathological lead points which can be benign or malignant. Lymphomas rarely present with intussusception and follicular lymphomas are even less common. To the best of our knowledge, there have only been a few such cases of follicular lymphomas with the initial presentation of intussusception. In this article, we present a rare case of follicular lymphoma presenting as intussusception. Considering lymphomas as a cause of intussusception in adults can decrease diagnostic delays and guide treatment.

13.
Cureus ; 13(7): e16354, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34395132

RESUMO

Lyme disease is a vector-borne illness of North America and Europe transmitted by Borrelia burgdorferi, over 30,000 cases are reported in the United States yearly. Patients typically present having early localized disease with fevers, headaches, myalgias, and a single erythema migrans. Usually, oral doxycycline is administered with a good disease prognosis but we report the case of a 58-year-old male who presented with Lyme disease diagnosed by immunoassay; he was treated with doxycycline but was refractory and saw an improvement in his symptoms with IV ceftriaxone.

14.
Med Chem ; 17(8): 887-902, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32851965

RESUMO

BACKGROUND: Diabetes mellitus is one of the most chronic metabolic disorders. Since past few years, our research group had synthesized and evaluated libraries of heterocyclic compounds against α and ß-glucosidase enzymes and found encouraging results. The current study comprises of evaluation of indane-1,3-dione as antidiabetic agents based on our previously reported results obtained from closely related moiety isatin and its derivatives. OBJECTIVE: A library of twenty three indane-1,3-dione derivatives (1-23) was synthesized and evaluated for α and ß-glucosidase inhibitions. Moreover, in silico docking studies were carried out to investigate the putative binding mode of selected compounds with the target enzyme. METHODS: The indane-1,3-dione derivatives (1-23) were synthesized by Knoevenagel condensation of different substituted benzaldehydes with indane-1,3-dione under basic condition. The structures of synthetic molecules were deduced by using different spectroscopic techniques, including 1H-, 13C-NMR, EI-MS, and CHN analysis. Compounds (1-23) were evaluated for α and ß-glucosidase inhibitions by adopting the literature protocols. RESULT: Off twenty three, eleven compounds displayed good to moderate activity against α- glucosidase enzyme, nonetheless, all compounds exhibited less than 50% inhibition against ß- glucosidase enzyme. Compounds 1, 14, and 23 displayed good activity against α-glucosidase enzyme with IC50 values of 2.80 ± 0.11, 0.76 ± 0.01, and 2.17 ± 0.18 µM, respectively. The results have shown that these compounds have selectively inhibited the α-glucosidase enzyme. The in silico docking studies also supported the above results and showed different types of interactions of synthetic molecules with the active site of enzyme. CONCLUSION: The compounds 1, 14, and 23 have shown good inhibition against α-glucosidase and may potentially serve as lead for the development of new therapeutic representatives.


Assuntos
Simulação por Computador , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Indanos/química , Indanos/farmacologia , alfa-Glucosidases/metabolismo , Domínio Catalítico , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/metabolismo , Humanos , Indanos/síntese química , Indanos/metabolismo , Cinética , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade , alfa-Glucosidases/química
15.
Med Chem ; 15(2): 162-174, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30081790

RESUMO

BACKGROUND: Inflammation is a biological rejoinder of vascular tissues against destructive agents e.g. irritants, damaged cell or pathogens. During inflammation, respiratory burst occurs by activated phagocytes which help to destroy invading pathogens. Phagocytic cells such as neutrophils and macrophages are one of the major sources of reactive oxygen species (ROS) and nitric oxide (NO). Normally, the redox environment is maintained by various antioxidant defense systems, however, these reactive oxygen species may be destructive and can lead to various pathological conditions. METHODS: Benzophenone esters and sulfonates (1-18) were synthesized through one pot synthesis by reacting 4-hydroxy benzophenone either different benzoyl chloride or sulfonyl chloride. These synthetic compounds were evaluated for their in vitro immunosuppressive potential on two parameters of innate immune response including inhibition of intracellular reactive oxygen species (ROS) and nitric oxide (NO). ROS were induced in polymorphonuclear leukocytes (PMNs) isolated from human whole blood by serum opsonized zymosan stimulation, whereas NO were produced in J774.2 cells by lipopolysachharides (LPS) stimulation. Moreover, cytotoxicity of compounds was also determined using NIH-3T3 fibroblast cells (ATCC, Manassas, USA) was evaluated by using the standard MTT colorimetric assay. RESULTS: All compounds inhibited the production of ROS at various extent among which compounds 2, 5, 6, 8, 10, 13 and 16 were found to be the potent inhibitors of ROS with IC50 values ranging between (1.0 - 2.2 µg/mL) as compared to ibuprofen (IC50 = 2.5 ± 0.6 µg/mL) as the standard drug. Compounds 2, 7, 11, 13, 14 and 18 showed good inhibition of NO production with % inhibition values ranging between (63.6% - 76.7%) at concentration of 25 µg/mL as compared to NG-monomethyl-Larginine (L-NMMA 65.6 ± 1.1 µg/mL) as the standard. All other derivatives showed moderate to low level of inhibition on both tested parameters. Cytotoxicity activity also showed nontoxicity of synthetic compounds. Structures of all the synthetic compounds were confirmed through 1H-NMR, 13C-NMR, EI-MS and HREI-MS spectroscopic techniques. CONCLUSION: Compounds 2 and 13 were found to be good dual antiinflammatory (ROS and NO) agent. However, compounds 5, 6, 8, 10 and 16 were found to be selectively active for ROS inhibitory studies. Compounds 7, 11, 14 and 18 were discriminatory active at NO inhibition assay. These initial findings of antiinflammatory activity concluded that these compounds might have the potential to develop a novel non-steroidal antiinflammatory drugs (NSAIDs), non-acidic antiinflammatory agent. Most active compounds 2, 5-8, 10, 13, 14 and 16 showed nontoxicity of synthetic compounds.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/farmacologia , Benzofenonas/síntese química , Benzofenonas/farmacologia , Ésteres/química , Ácidos Sulfônicos/química , Animais , Anti-Inflamatórios não Esteroides/química , Benzofenonas/química , Técnicas de Química Sintética , Camundongos , Células NIH 3T3 , Óxido Nítrico/metabolismo , Fagócitos/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Relação Estrutura-Atividade
16.
Bioorg Chem ; 78: 269-279, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29614438

RESUMO

Twenty-five derivatives of 5-chloro-2-aryl benzo[d]thiazole (1-25) were synthesized and evaluated for their α-glucosidase (S. cerevisiae EC 3.2.1.20) inhibitory activity in vitro. Among them eight compounds showed potent activity with IC50 values between 22.1 ±â€¯0.9 and 136.2 ±â€¯5.7 µM, when compared with standard acarbose (IC50 = 840 ±â€¯1.73 µM). The most potent compounds 4, 9, and 10 showed IC50 values in the range of 22.1 ±â€¯0.9 to 25.6 ±â€¯1.5 µM. Compounds 2, 5, 11, and 19 showed IC50 values within the range of 40.2 ±â€¯0.5 to 60.9 ±â€¯2.0 µM. Compounds 1 and 3 were also found to be good inhibitors with IC50 values 136.2 ±â€¯5.7 and 104.8 ±â€¯9.9 µM, respectively. Their activities were compared with α-glucosidase inhibitor drug acarbose (standard) (IC50 = 840 ±â€¯1.73 µM). The remaining compounds were inactive. Structure-activity relationships (SAR) have also been established. Kinetics studies indicated compounds 2, 3, 10, 19, and 25 to be non-competitive, while 1, 5, 9, and 11 as competitive inhibitors of α-glucosidase enzyme. All the active compounds (1-5, 9-11, and 19) were also found to be non-cytotoxic, in comparison to the standard drug i.e., doxorubicin (IC50 = 0.80 ±â€¯0.12 µM) in MTT assay. Furthermore, molecular interactions of active compounds with the enzyme binding sites were predicted through molecular modeling studies.


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Tiazóis/farmacologia , alfa-Glucosidases/metabolismo , Relação Dose-Resposta a Droga , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Cinética , Modelos Moleculares , Estrutura Molecular , Saccharomyces cerevisiae/enzimologia , Relação Estrutura-Atividade , Tiazóis/síntese química , Tiazóis/química
17.
Med Chem ; 14(7): 674-687, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29564980

RESUMO

BACKGROUND: Inflammation is defined as the response of immune system cells to damaged or injured tissues. The major symptoms of inflammation include increased blood flow, cellular influx, edema, elevated cellular metabolism, reactive oxygen species (ROS) nitric oxide (NO) and vasodilation. This normally protective mechanism against harmful agents when this normal mechanism becomes dysregulated that can cause serious illnesses including ulcerative colitis, Crohn's disease, rheumatoid arthritis, osteoarthritis, sepsis, and chronic pulmonary inflammation. METHOD: In this study synthetic transformations on diclofenac were carried out in search of better non-steroidal antiinflammatory drugs (NSAIDs), non-acidic, antiinflammatory agents. For this purpose diclofenac derivatives (2-20) were synthesized from diclofenac (1). All derivatives (2-20) and parent diclofenac (1) were evaluated for their antiinflammatory effect using different parameters including suppression of intracellular reactive oxygen species (ROS), produced by whole blood phagocytes, produced by neutrophils, and inhibition of nitric oxide (NO) production from J774.2 macrophages. The most active compound also evaluated for cytotoxicity activity. RESULTS: Diclofenac (1) inhibited the ROS with an IC50 of 3.9 ± 2.8, 1.2 ± 0.0 µg/mL respectively and inhibited NO with an IC50 of 30.01 ± 0.01 µg/mL. Among its derivatives 4, 5, 11, 16, and 20, showed better antiinflammatory potential. The compound 5 was found to be the most potent inhibitor of intracellular ROS as well as NO with IC50 values of 1.9 ± 0.9, 1.7 ± 0.4 µg/mL respectively and 7.13 ± 1.0 µg/mL, respectively, and showed good inhibitory activity than parent diclofenac. The most active compounds were tested for their toxic effect on NIH-3T3 cells where all compounds were found to be non-toxic compared to the standard cytotoxic drug cyclohexamide. CONCLUSION: Five derivatives were found to be active. Compound 5 was found to be the most potent inhibitor of ROS and NO compared to parent diclofenac 1 and standard drugs ibuprofen and L-NMMA, respectively. The most active compounds 1, 4, 5, 11 and 20 were found to be non-toxic on NIH-3T3 cells. Compound 4, 5, and 20 also showed good antiinflammatory potential, compound 11 and 16 showed moderate and low level of inhibition, respectively.


Assuntos
Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/síntese química , Diclofenaco/análogos & derivados , Diclofenaco/síntese química , Anti-Inflamatórios não Esteroides/efeitos adversos , Estrutura Molecular , Relação Estrutura-Atividade
18.
Cureus ; 9(10): e1804, 2017 Oct 26.
Artigo em Inglês | MEDLINE | ID: mdl-29308332

RESUMO

This case report discusses a suspected case of lithium toxicity following the administration of topiramate (TPM). Our patient is a 47-year-old man who has been an inpatient for the past year and was diagnosed with schizoaffective disorder bipolar type 1 for the past 20 years according to the criteria of the Diagnostic and Statistical Manual of Mental Disorders, fifth edition (DSM-5). He manifested symptoms of lithium toxicity following administration of TPM to ameliorate the compulsive consumption of food and liquids. The patient was already being treated with lithium carbonate for mania, labile mood, and aggressive behavior for the past year. The patient developed symptoms of lithium toxicity on the fourth day of the TPM treatment. We transferred the patient to the emergency department where he was diagnosed and treated for renal insufficiency due to lithium toxicity. After halting the TPM and reintroducing lithium carbonate, the patient's laboratory results improved. This case illustrates the potential toxic interaction of medications with a narrow therapeutic index like lithium.

19.
Indian J Dermatol ; 60(1): 102, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25657418

RESUMO

BACKGROUND: Chronic autoimmune urticaria (CAU) is one of the most challenging therapeutic problems faced by a dermatologist. Recently, weekly autologous serum injections have been shown to induce a prolonged remission in this disease. AIM: To evaluate the efficacy of repeated autologous serum injections in patients with CAU. MATERIALS AND METHODS: Seventy patients of CAU were prospectively analyzed for the efficacy of nine consecutive weekly autologous serum injections with a post-intervention follow-up of 12 weeks. Total urticaria severity score (TSS) was monitored at the baseline, at the end of treatment and lastly at the end of 12 weeks of follow up. Response to treatment was judged by the percentage reduction in baseline TSS at the end of treatment and again at the end of 12 weeks-follow-up. RESULTS: Out of the 70 patients enrolled, 11 dropped out of the injection treatment after one or the first few doses only. Among the rest of 59 patients, only 7 patients (12%) went into a partial or complete remission and remained so over the follow-up period of 12 weeks. Forty patients (68%) did not demonstrate any significant reduction in TSS at the end of the treatment period. Rest of the 12 patients showed either a good or excellent response while on weekly injection treatment, but all of them relapsed over the follow-up period of 12 weeks. CONCLUSION: Autologous serum therapy does not seem to lead to any prolonged remission in patients of CAU.

20.
Acta Crystallogr Sect E Struct Rep Online ; 69(Pt 3): o360, 2013 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-23476550

RESUMO

In the title compound, C14H10ClNOS, the dihedral angle between the benzothia-zole ring system and the meth-oxy-substituted benzene ring is 8.76 (16)°. In the crystal, mol-ecules are stacked in columns along the c axis and no significant inter-molecular inter-actions are observed.

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