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1.
Curr Top Med Chem ; 23(22): 2097-2115, 2023.
Article in English | MEDLINE | ID: mdl-37455456

ABSTRACT

Pyrazole is considered an important active scaffold that possesses various types of pharmacological activities. The overwhelming literature reported earlier reflects the immense biological potential of pyrazole derivatives. The presence of this moiety in various FDA-approved drugs, including celecoxib (anti-inflammatory), apixaban (anticoagulant), rimonabant (anti-obesity), difenamizole (analgesic), and sildenafil (for erectile dysfunction), has proved its pharmacological potential. Owing to its diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the literature supporting the research of the past 10 years related to the structures of pyrazole derivatives with their corresponding biological activities. The findings of this review may open new avenues for an upcoming scientific breakthrough.


Subject(s)
Anti-Inflammatory Agents , Chemistry, Pharmaceutical , Humans , Anti-Inflammatory Agents/pharmacology , Analgesics/pharmacology , Pyrazoles/pharmacology , Pyrazoles/chemistry , Obesity , Structure-Activity Relationship
2.
Nanotechnology ; 2021 Apr 21.
Article in English | MEDLINE | ID: mdl-33882473

ABSTRACT

The emergence of multi-drug resistant bacterial infections has resulted in increased interest in the development of alternative systems which can sensitize bacteria to overcome resistance. In an attempt to contribute to the existing literature of potential antibacterial agents, we present here, a first report of the antibacterial potential of FeCo nanoparticles, both as stand-alone devices and in presence of magnetic field, against the bacterial strains of S. aureus and E. coli. A relatively simple polyol process was employed for nanoparticle synthesis. Formation of FeCo alloy in the desired BCC phase was confirmed by X-Ray Diffraction with a high saturation magnetization (Ms~180 Am2kg-1). Uniformly sized spherical structures with sharp edges were obtained. Solution stability was confirmed by the zeta potential value of -27.8 mV. Dose dependent bacterial growth inhibition was observed, the corresponding linear correlation coefficients being, R2 = 0.74 for S. aureus and R2 = 0.76 for E. coli. Minimum inhibitory concentration was accordingly ascertained to be >1024 µg/ml for both. Bacterial growth curves have been examined upon concomitant application of external magnetic field of varying intensities and revealed considerable enhancement in the antibacterial response upto 63% in a field of 100 mT. An effort has been made to understand the bacterial inhibitory mechanism by relating with the chemical and physical properties of the nanoparticles. The ease of field assisted targeting and retrieval of these highly magnetic, antibacterial nano-devices, with considerably improved response with magnetic fields, make them promising for several medical and environment remediation technologies.

3.
Mini Rev Med Chem ; 20(12): 1091-1100, 2020.
Article in English | MEDLINE | ID: mdl-32107992

ABSTRACT

This article provides comprehensive and collective facts about teneligliptin. Teneligliptin is a dipeptide peptidase-4 (DPP-4) inhibitor that belongs to the third generation, used in the management of type 2 diabetes. It inhibits human DPP-4 enzyme activity. This drug falls under class 3; it interacts with S1, S2, and S2E extensive sub-sites. Teneligliptin and its metabolites are mainly determined in the human plasma matrix by hyphenated chromatographic methods. These developed methods could be foreseen for their clinical applications. Moreover, the stress degradation studies of Teneligliptin under different stress conditions provide an insight into degradation pathways and help in the elucidation of the structure of the degradation products by liquid mass spectroscopy. These methods are also used for routine quality control analysis of teneligliptin in pharmaceutical dosage forms.


Subject(s)
Dipeptidyl-Peptidase IV Inhibitors/chemistry , Pyrazoles/chemistry , Thiazolidines/chemistry , Blood Glucose/analysis , Cardiovascular Diseases/etiology , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/pathology , Dipeptidyl Peptidase 4/chemistry , Dipeptidyl Peptidase 4/metabolism , Dipeptidyl-Peptidase IV Inhibitors/adverse effects , Dipeptidyl-Peptidase IV Inhibitors/metabolism , Dipeptidyl-Peptidase IV Inhibitors/therapeutic use , Drug Interactions , Glucagon-Like Peptide 1/metabolism , Half-Life , Humans , Pyrazoles/adverse effects , Pyrazoles/metabolism , Pyrazoles/therapeutic use , Thiazolidines/adverse effects , Thiazolidines/metabolism , Thiazolidines/therapeutic use
4.
JNMA J Nepal Med Assoc ; 58(232): 1046-1051, 2020 Dec 31.
Article in English | MEDLINE | ID: mdl-34506372

ABSTRACT

INTRODUCTION: Nepal government enforced a lockdown as a social distancing measure to curb the COVID-19 pandemic. The lockdown has led to compromises in day to day choices like food, exercise, sleep, self-care routines and utilization of healthcare facilities - directly and indirectly influencing aspects of health. Identification of compromised health choices can assist in better planning of inevitable future crises. METHODS: This is a cross-sectional descriptive study based on an online self -administered questionnaire, done using CHERRIES criteria, conducted from March 30, 2020, to July 31, 2020. Ethical approval for the study was obtained from the Institutional Review Committee of Nepal Health Research Council (Registration number: 2119; 300/2020 P). Descriptive statistics was used for analysis. RESULTS: Our study had 340 (51%) female and 325 (48.7%) male participants. A total of 112 (67.9%) reported decreased consumption of tobacco and 178 (53.6%) reported decreased consumption of alcohol during the lockdown period. Participants who reported that they would have visited a hospital if they had a flu-like illness increased from 151 (22.6%) pre-pandemic to 391 (58.6%) post-pandemic. Increase in news consumption was reported by 528 (79.2%). Out of 43 (6.4%) participants with a chronic condition, 30 (69.8%) reported having missed follow up due to the lockdown. CONCLUSIONS: The health of an individual is determined by various choices s/he makes on a day to day basis. Many of those choices are in turn influenced by the availability and accessibility of commodities. Lessons learned from the affected lives due to COVID-19 can be used in proper planning of inevitable future crises.


Subject(s)
COVID-19 , Pandemics , Communicable Disease Control , Cross-Sectional Studies , Female , Humans , Male , SARS-CoV-2
5.
Asian J Endosc Surg ; 8(1): 63-6, 2015 Feb.
Article in English | MEDLINE | ID: mdl-25598057

ABSTRACT

Osseous metaplasia is a rare disorder of the endometrium that usually leads to secondary infertility and is frequently associated with recurrent abortions. Here we present two cases: one presenting with primary infertility and another presenting with oligomenorrhea. In both cases, vaginal ultrasonography showed an intrauterine structure that appeared hyperechogenic, suggesting calcification. Hysteroscopy revealed multiple white spicules of bony material in the uterine cavity. In both cases, the lesion was treated by hysteroscopic removal without complications. Histology established a diagnosis of endometrial osseous metaplasia. Thus, hysteroscopy was effective in the diagnosis and treatment of endometrial osseous metaplasia. The patient with primary infertility had spontaneous conception of twins 6 months after the procedure.


Subject(s)
Calcinosis/surgery , Endometrium/pathology , Hysteroscopy/methods , Uterine Diseases/pathology , Adult , Calcinosis/pathology , Endometrium/surgery , Female , Follow-Up Studies , Humans , Metaplasia/pathology , Metaplasia/surgery , Uterine Diseases/surgery
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