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1.
Cureus ; 15(6): e40676, 2023 Jun.
Article in English | MEDLINE | ID: mdl-37485154

ABSTRACT

Background and objective Moderate to deep sedation is a prerequisite during total intravenous anesthesia for short-duration surgeries, and it can be achieved by using individual drugs or in combination. Our study compared dexmedetomidine-ketamine (DK) versus ketamine-propofol (KP) in terms of sedation, procedural interference, hemodynamics, and incidence of side effects in patients undergoing short surgical procedures. Methods A total of 194 patients scheduled for short-duration elective surgeries were randomly allocated into two groups. Group DK received a loading dose of 1 µg/kg of dexmedetomidine and 1 mg/kg of ketamine followed by a maintenance infusion of dexmedetomidine at 0.3 µg/kg/h. Group KP received a loading dose of 1 mg/kg of ketamine and 1 mg/kg of propofol followed by a maintenance infusion of propofol at 25 µg/kg/h. For procedural interference, a rescue ketamine bolus was administered at 0.25 mg/kg. Patients were monitored for the requirement of rescue ketamine bolus, procedural interference, hemodynamics, sedation, recovery time, and adverse effects. Results The procedural interference was higher in group KP than in group DK and the difference was statistically significant (P=0.001). The time to the first rescue bolus was 8.72 ± 4.47 minutes in group KP and 10.82 ± 4.01 minutes in group DK, with a difference of 2.1 minutes (p=0.026). There was no statistically significant difference in the sedation scores between both groups except at time points of six minutes and 15 minutes. Conclusion For short-duration procedures, the DK combination is superior to the KP combination in terms of procedural interference and time to the first rescue bolus, while both groups were comparable with regard to safety and hemodynamics.

2.
Indian J Anaesth ; 67(4): 370-375, 2023 Apr.
Article in English | MEDLINE | ID: mdl-37303878

ABSTRACT

Background and Aims: Inguinal hernia repair is associated with moderate to severe pain that is most extreme in the first 24 hours. The aim of this study was to compare the efficacy of dexamethasone versus magnesium sulphate (MgSO4) with bupivacaine in ultrasound-guided transversus abdominis plane (TAP) block for patients undergoing unilateral inguinal hernioplasty. Methods: Eighty patients were randomly allocated to two groups to receive ultrasound-guided TAP block postoperatively with either 20 ml of 0.25% bupivacaine with 8 mg of dexamethasone (Group BD) or 20 ml of 0.25% bupivacaine with 250 mg of MgSO4 (Group BM). Patients were assessed for the first 24 hours after surgery for pain at rest and movement using a numerical rating scale (NRS). Two mg/kg of tramadol was administered as rescue analgesia. The time to first demand tramadol, total consumption of tramadol, patient satisfaction score and side effects were evaluated. Results: The time to the first dose of rescue analgesia was significantly longer in BD group (596.13 ± 57.93 min) than in the BM group (422.50 ± 51.95 min). The NRS scores in the BD group were significantly lower compared to the BM group both at rest and on movement. The total requirement of tramadol was significantly less in the BD group (154.55 ± 59.11 mg) compared to the BM group (270.25 ± 105.72 mg). The incidence of side effects was lower and patient satisfaction was higher in BD group compared to BM group. Conclusion: Bupivacaine with dexamethasone in TAP block after unilateral open inguinal hernioplasty provides increased duration of analgesia and decreased requirement for rescue analgesics compared to magnesium sulphate, with lesser side effects and better patient satisfaction.

3.
Cureus ; 14(10): e30431, 2022 Oct.
Article in English | MEDLINE | ID: mdl-36276602

ABSTRACT

Background Hypotension is commonly encountered in patients undergoing lower-segment cesarean section (LSCS) under the subarachnoid block (SAB) owing to decreased vascular resistance caused by the sympathetic blockade and decreased cardiac output because of blood pooling in blocked areas of the body. Perfusion index (PI) is a good indicator of systemic vascular resistance and can foretell hypotension. This study aimed to associate baseline PI with intraoperative hypotension after SAB in LSCS. Methodology This was a prospective observational study with a sample size of 50. The baseline PI was recorded every 10 seconds for one minute in a supine position on the right index finger at room temperature of 26°C to 28°C. The blood pressure (BP) and heart rate (HR) were recorded at an interval of one minute for three minutes. The mean of PI, BP, and HR were taken as the preoperative value. Spinal anesthesia was administered as per institutional protocol. Hypotension, defined as mean arterial pressure (MAP) <20% of baseline or MAP <60 mmHg was treated with vasopressors. Regression analysis with the Spearman correlation coefficient was done to correlate PI and hypotension. Results The incidence of hypotension in parturients with PI <2.85 was 28.6% (5/20) and in parturients with PI >2.85 was 82.8% (p < 0.001). The requirement of sympathomimetics was higher in parturients with PI >2.85.The area under the receiver operating characteristic curve was 0.8883. A cut-off PI value of 2.85 can identify parturients at risk for central neuraxial block-induced hypotension with a sensitivity of 80% and a specificity of 75% (p < 0.001). Conclusions The PI is a useful tool for predicting hypotension in healthy parturients undergoing elective cesarean section under SAB.

4.
Cureus ; 14(9): e28754, 2022 Sep.
Article in English | MEDLINE | ID: mdl-36211112

ABSTRACT

Background and objective Many tests are at hand to predict difficult intubation preoperatively to prevent morbidity and mortality of unanticipated difficult intubation. The present study was conducted to evaluate and compare the efficacy of the modified Mallampati test (MMT) and upper lip bite test (ULBT) to foresee difficult intubation. Materials and methods After obtaining written informed consent, this prospective comparative observational study was conducted on 225 patients scheduled for elective surgery under general endotracheal anesthesia. Preoperative MMT and ULBT were performed. MMT Grade III, IV, and ULBT Grade IV were regarded as predictors of difficult intubation. The laryngoscopic view was graded as per Cormack and Lehane's laryngoscopic grading after induction of anesthesia by an experienced anesthesiologist ignorant of preoperative airway evaluation. Patients with Cormack and Lehane Class III and IV were regarded as difficult intubation. Sensitivity, specificity, and positive and negative predictive values of MMT and ULBT were computed. Agreement between two tests with the Cormack Lehane test was determined by the Kappa coefficient. Results In our research, the occurrence of difficult intubation was found to be 10.2% (23 cases of difficult intubation out of 225 patients). In our analysis, we found the sensitivity (95.5% vs. 95.4%), specificity (54.8% vs 50.0%), positive predictive value (91.6% vs 93.1%), and negative predictive value (39.1% vs 39.1%) were almost comparable between modified Mallampati test and upper lip bite test. Kappa coefficient for the upper lip bite test (0.492) was slightly higher as compared to modified Mallampati scoring (0.454), but both the values are highly statistically significant (p-value <0.001). Conclusion Both the upper lip bite test and modified Mallampati test are comparable with each other and since the upper lip bite test is easy to perform bedside test we recommend it to be used alone or in collaboration with other tests in assessing difficult airways.

5.
Cureus ; 14(12): e32421, 2022 Dec.
Article in English | MEDLINE | ID: mdl-36644056

ABSTRACT

Background and objective The development of modern anesthetic agents has made it possible to conduct pain-free surgical procedures. The role of the anesthetist in choosing a suitable anesthetic agent to provide a good anesthetic and sedative effect is very important in any surgical procedure. There is always a degree of risk involved as the hemodynamic parameters may be altered. This study aimed to compare the hemodynamic changes and respiratory effects between the use of etomidate and propofol for the induction of general anesthesia (GA) as well as to compare the side effects of both drugs in daycare surgeries. Methods The study was a parallel-design, randomized, double-blinded control trial conducted over a period of three years among patients undergoing elective daycare surgeries under GA. The patients were classified into two groups depending on the type of drug received: Group A or the propofol group and Group B or the etomidate group. Randomization was done by computer-generated random number generator software. A total of 174 patients were selected (87 in each group) at a ratio of 1:1. A baseline evaluation of the hemodynamic parameters was done followed by continuous monitoring. Results The age, weight, and gender distribution of the patients in both groups were comparable. Significant hemodynamic changes were observed following induction in Group A. The fall in systolic blood pressure (SBP), diastolic blood pressure (DBP), and mean arterial blood pressure (MABP) in Group A following induction was found to be statistically significant (p<0.00). The rise in heart rate was almost similar in both groups, with Group A demonstrating a slightly higher rate. There were fewer signs of respiratory depression in Group B. The major side effects observed after induction were myoclonus, which was more prevalent in Group B patients (21.84%), and pain at the injection site, which was observed more frequently in Group A (17.1%). Conclusion  Based on our findings, etomidate is a drug with better hemodynamic stability and less pain at the site of injection compared to propofol. Hence, it may be a better induction agent in daycare surgeries.

6.
Cureus ; 13(11): e20058, 2021 Nov.
Article in English | MEDLINE | ID: mdl-34873557

ABSTRACT

BACKGROUND: Spinocerebellar ataxia (SCA) is a disease that refers to a category of inherited ataxias that are characterized by degenerative alterations in the cerebellum, pons, and spinocerebellar tracts. There are several different varieties of SCA and they are classified based on the mutant (altered) gene that causes the disease. OBJECTIVE: To analyze the cardiovascular autonomic regulation in patients with type-2 spinocerebellar ataxia (SCA-2) from the heart rate variability (HRV) of 20 minutes resting electrocardiogram (ECG) and compare with the age and gender-matched controls. MATERIALS AND METHODS: HRV of 27 type-2 spinocerebellar ataxia patients was calculated offline from the resting ECG recording and compared with 23 age and gender-matched controls. The HRV was analyzed by HRV software module MLS 310. The frequency and time domain parameters were computed and compared. RESULT:  Type-2 spinocerebellar ataxia patients have significantly low HRV and parasympathetic activity at rest compared to normal control. The total power in SCA-2 is 13491.63 ± 7660.77 ms2 and the normal control is 21784.76 ± 11008.67 ms2. High-frequency power (HF) which is a marker of parasympathetic activity in SCA-2 is 3823.1 ± 364 ms2 and in normal control is 9006.1 ± 920.64 ms2. The standard deviation of all NN intervals (SDNN), the square root of the mean-squared differences of successive intervals (RMSSD), spectral interval, and delta NN is significantly low in SCA-2. CONCLUSION: There is decreased parasympathetic tone and low HRV in SCA-2 as compared to normal controls.

7.
Cureus ; 13(11): e19793, 2021 Nov.
Article in English | MEDLINE | ID: mdl-34820250

ABSTRACT

Background and objective Several drugs have been used to prevent or attenuate succinylcholine-induced muscle fasciculations and myalgia. We designed the present study to evaluate the efficacy of rocuronium (ROC) and vecuronium (VEC) in preventing succinylcholine-induced fasciculations and postoperative myalgia (POM) in patients undergoing surgery under general anesthesia. Materials and methods After obtaining written informed consent, 125 patients were randomly selected to receive either ROC 0.06 mg/kg or VEC 0.01 mg/kg, with both diluted up to 2 ml, 90 seconds before the administration of propofol followed by succinylcholine. A standardized balanced anesthetic technique was used for all patients. The intensity of fasciculations and intubating conditions were assessed using a 4-point rating scale. All patients were evaluated up to the third postoperative day for the presence of POM, the severity of which was graded on a 4-point scale. Results The incidence of post-succinylcholine fasciculations during induction was nil in 74.58% of patients in the ROC group and 51.52% in the VEC group. Mild fasciculation was seen in 22.03% in the ROC group and 33.33% in the VEC group. Moderate fasciculation was seen in 3.39% and 15.15% in ROC and VEC groups respectively. When comparing both the groups, a significant decrease (p=0.015) in intraoperative fasciculation was observed in the ROC group than in the VEC group. Both drugs provided good intubating conditions without any statistical significance and with an overall intubating score of 8-9 in both groups as per Lund. On day one, 91.53% (n=54) of the ROC group and 65.15% (n=43) of the VEC group patients did not have any myalgia symptoms. Mild myalgia was observed in 8.47% (n=5) in the ROC group and 31.82% (n=21) in the VEC group, and only 1.8% had moderate myalgia in the VEC group. The results of the study showed that POM was significantly decreased in the ROC group than in the VEC group on day one (p=0.001). The incidence of POM on day two was significantly low in both groups. There was no statistical significance between the two groups based on Fisher's exact test (p=1.000). None of the patients had myalgia on day three. Conclusion Our results showed that the incidence and severity of fasciculations and POM were significantly decreased by pretreatment with ROC in contrast to that with VEC. Hence, ROC is a better option than VEC to combat succinylcholine-related complications like fasciculation and myalgia.

8.
Langmuir ; 33(38): 9620-9631, 2017 09 26.
Article in English | MEDLINE | ID: mdl-28846429

ABSTRACT

We experimentally investigate the impact dynamics of a microliter water droplet on a hydrophobic microgrooved surface. The surface is fabricated using photolithography, and high-speed visualization is employed to record the time-varying droplet shapes in the transverse and longitudinal directions. The effect of the pitch of the grooved surface and Weber number on the droplet dynamics and impact outcome are studied. At low pitch and Weber number, the maximum droplet spreading is found to be greater in the longitudinal direction than the transverse direction to the grooves. The preferential spreading inversely scales with the pitch at a given Weber number. In this case, the outcome is no bouncing (NB); however, this changes at larger pitch or Weber number. Under these conditions, the following outcomes are obtained as a function of the pitch and Weber number: droplet completely bounces off the surface (CB), bouncing occurs with droplet breakup (BDB), or no bouncing because of a Cassie to Wenzel wetting transition (NBW). In BDB and NBW, the liquid partially or completely penetrates the grooves beneath the droplet as a result of the wetting transition. The former results in droplet breakup alongside bouncing, while the latter suppresses the bouncing. These outcomes are demarcated on the Weber number-dimensionless pitch plane, and the proposed regime map suggests the existence of a critical Weber number or pitch for the transition from one regime to the other. CB and BDB are quantified by plotting the coefficient of restitution of the bouncing droplet and the volume of the daughter droplet left on the surface, respectively. The critical Weber number needed for the transition from CB to BDB is estimated using an existing mathematical model and is compared with the measurements. The comparison is good and provides insights into the mechanism of liquid penetration into the grooves. The present results on microgrooved surfaces are compared with published results on micropillared surfaces in order to assess the water-repelling properties of the two surfaces.

9.
Open Dent J ; 9: 98-102, 2015.
Article in English | MEDLINE | ID: mdl-25870716

ABSTRACT

UNLABELLED: Fluorosis is one of the factors which bring about mineralisation changes in a dentinal structure leading to dentin. The purpose of the present study was to compare and evaluate the dentinal tubular changes in fluorosed and nonfluorosed teeth subsequent to the application of citric acid,strontium acetate based sodium fluoride (SAF) using scanning electron microscopy (SEM). Dentin specimens from healthy fluorosed and nonfluorosed teeth were included in the study. Each of them was grouped into acid treated and SAF treatment groups. Using SEM, the photomicrographs (3500x) of dentin specimens were evaluated. Results showed while there was a significant difference in tubular width of partial occlusion ≤ 25%, being more in fluorosed group compared to nonfluorosed group after application SAF. Application of desensitising agents demonstrated higher number of dentinal tubular occlusion and diameter reduction in nonfluorosed dentin compared to fluorosed dentin. SUMMARY: Root biomodification and desensitising agent procedure brings in definite difference between fluorosed and non-fluorosed dentin specimens.

10.
J Enzyme Inhib Med Chem ; 30(1): 22-31, 2015 Feb.
Article in English | MEDLINE | ID: mdl-24666306

ABSTRACT

Abstract A series of novel pyrazole-based chalcones have been designed, synthesized from 1-methyl-5-(2,4,6-trimethoxyphenyl)-1H-pyrazole (6). The structures of regioisomers 6 and 7 were determined by 2D (1)H-(1)H COSY, (1)H-(13)C HSQC and (1)H-(13)C HMBC experiments. The newly synthesized compounds were tested for their inhibitory activity against COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Moreover, they were investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw edema model for acute inflammation and cotton pellet-induced granuloma model for chronic inflammation. All the synthesized compounds showed potential to demonstrate anti-inflammatory activities, of particular interest compounds 10i, 10e, 10f, and 10h were found to be potent anti-inflammatory agents.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Chalcones/chemical synthesis , Cyclooxygenase Inhibitors/chemical synthesis , Edema/drug therapy , Granuloma/drug therapy , Pyrazoles/chemical synthesis , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Carrageenan , Chalcones/chemistry , Chalcones/pharmacology , Cotton Fiber , Cyclooxygenase 1/chemistry , Cyclooxygenase 2/chemistry , Cyclooxygenase Inhibitors/chemistry , Cyclooxygenase Inhibitors/pharmacology , Drug Design , Edema/chemically induced , Edema/enzymology , Edema/pathology , Granuloma/chemically induced , Granuloma/enzymology , Granuloma/pathology , Hindlimb , Membrane Proteins/chemistry , Pyrazoles/chemistry , Pyrazoles/pharmacology , Rats , Stereoisomerism
11.
12.
Bioorg Med Chem Lett ; 23(5): 1315-21, 2013 Mar 01.
Article in English | MEDLINE | ID: mdl-23357629

ABSTRACT

A series of novel pyrazole amalgamated flavones has been designed and synthesized from 1-methyl-5-(2,4,6-trimethoxy-phenyl)-1H-pyrazole 6. The structures of regioisomers 6 and 7 were resolved by 2D (1)H-(1)H COSY, (1)H-(13)C HSQC and (1)H-(13)C HMBC experiments. The newly synthesized compounds were tested for their in vitro COX inhibition and in vivo carrageenan induced hind paw edema in rats and acetic acid induced vascular permeability in mice. Although the compounds have inhibitory profile against both COX-1 and COX-2, some of the compounds are found to be selective against COX-2, supported by inhibition of paw edema and vascular permeability. Docking studies were also carried out to determine the structural features which sway the anti-inflammatory activity of the tested compounds. The keto and phenolic -OH are major factors that are prominently involved in interaction with COX-2 active site.


Subject(s)
Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Flavones/chemistry , Flavones/pharmacology , Pyrazoles/chemistry , Pyrazoles/pharmacology , Animals , Anti-Inflammatory Agents/chemical synthesis , Cyclooxygenase Inhibitors/chemical synthesis , Cyclooxygenase Inhibitors/chemistry , Cyclooxygenase Inhibitors/pharmacology , Drug Design , Flavones/chemical synthesis , Mice , Models, Molecular , Pyrazoles/chemical synthesis , Rats
13.
Bioorg Med Chem Lett ; 23(3): 912-6, 2013 Feb 01.
Article in English | MEDLINE | ID: mdl-23290048

ABSTRACT

A series of novel pyrazole integrated benzophenones (9a-j) have been designed, synthesized from 1-methyl-5-(2,4,6-trimethoxy-phenyl)-1H-pyrazole 6. The structures of the regioisomers 6 and 7 were determined by 2D (1)H-(1)H COSY, (1)H-(13)C HSQC and (1)H-(13)C HMBC experiments. The newly synthesized compounds (9a-j) were evaluated for in vivo anti-inflammatory activity by carrageenan paw edema in rats and in vitro COX-1/COX-2 inhibition and antioxidant potential. Among the synthesized compounds, compounds 9b, 9d and 9f, were found to be active anti-inflammatory agents in addition to having potent antioxidant activity.


Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Antioxidants/chemical synthesis , Benzophenones/chemical synthesis , Benzophenones/pharmacology , Drug Design , Pyrazoles/chemical synthesis , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Benzophenones/chemistry , Cells, Cultured , Enzyme Activation/drug effects , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Pyrazoles/chemistry , Pyrazoles/pharmacology , Rats , Stereoisomerism
14.
J Enzyme Inhib Med Chem ; 28(3): 593-600, 2013 Jun.
Article in English | MEDLINE | ID: mdl-22380776

ABSTRACT

A series of novel carbazole chalcones has been synthesised and evaluated for radical scavenging activity, cytotoxicity and antimicrobial activities. Compounds 12m, 12o and 12c exhibited good 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, compounds 12e, 12m and 12d were excellent hydroxyl radical scavengers and compounds 12a, 12e, 12g, 12n and 12m have shown inhibition of oxidative DNA damage induced by 2,2'-azobis (2-amidinopropane hydrochloride). Compounds 12j, 12i, 12n, 12c, 12m and 12e were most active against the selected cancer cell lines. Compounds 12a, 12e and 12m showed good antibacterial activity and compounds 12h and 12m have shown good antifungal activity. All the compounds were subjected for absorption, distribution, metabolism and excretion (ADME) predictions by computational method and found that these molecules could be considered as potential candidates for oral drug development.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Anticarcinogenic Agents/chemical synthesis , Anticarcinogenic Agents/pharmacology , Carbazoles/chemistry , Chalcones/chemistry , Administration, Oral , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacokinetics , Anticarcinogenic Agents/chemistry , Anticarcinogenic Agents/pharmacokinetics , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Antioxidants/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Cell Line, Tumor , Chemistry Techniques, Synthetic , Drug Screening Assays, Antitumor , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacokinetics , Free Radical Scavengers/pharmacology , Humans , Structure-Activity Relationship , Tissue Distribution
15.
J Enzyme Inhib Med Chem ; 28(6): 1316-23, 2013 Dec.
Article in English | MEDLINE | ID: mdl-23230954

ABSTRACT

A novel series of carbazole substituted aminopyrimidines (5a-p) were synthesized and screened for their in vitro urease inhibition and antimicrobial activity. Among the compounds, 4-(2,4-dichlorophenyl)-6-(9-methyl-9H-carbazol-3-yl)-pyrimidin-2-amine (5i) was found to be the most potent showing urease inhibitory activity with an IC50 value 19.4 ± 0.43 µM. Compounds 5c, 5g, 5j and 5o showed good activity against all selected bacterial strains and compounds 5b, 5c, 5m and 5o showed good activity against selected fungal strains. All the compounds were subjected for ADME predictions by computational method.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Enzyme Inhibitors/pharmacology , Pyrimidines/pharmacology , Urease/antagonists & inhibitors , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemistry , Bacteria/drug effects , Canavalia/enzymology , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Fungi/drug effects , Microbial Sensitivity Tests , Molecular Structure , Pyrimidines/chemical synthesis , Pyrimidines/chemistry , Structure-Activity Relationship , Urease/metabolism
16.
Bioorg Med Chem Lett ; 22(18): 5839-44, 2012 Sep 15.
Article in English | MEDLINE | ID: mdl-22901385

ABSTRACT

A novel series of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines (5a-o) has been synthesized and the structures of newly synthesized compounds were characterized by IR, (1)H NMR and mass spectral analysis. All the synthesized compounds were evaluated for their in vitro and in vivo anti-inflammatory activity, and also for their antioxidant activity. Compounds 5b, 5c, 5d and 5n were found to be selective COX-2 inhibitors. Compound 5c was found to potent inhibitor of the carrageenin induced paw edema in rats. Most of the compounds exhibited good DPPH and superoxide radical scavenging activity, while compounds 5c, 5d, 5i and 5k exhibited good hydroxyl radical scavenging activity. Molecular docking result, along with the biological assay data, suggested that compound 5c was a potential anti-inflammatory agent.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antioxidants/chemical synthesis , Antioxidants/pharmacology , Edema/drug therapy , Pyrazoles/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Antioxidants/chemistry , Biphenyl Compounds/chemistry , Cyclooxygenase 1/metabolism , Cyclooxygenase 2/metabolism , Cyclooxygenase 2 Inhibitors/chemical synthesis , Cyclooxygenase 2 Inhibitors/chemistry , Cyclooxygenase 2 Inhibitors/pharmacology , Dose-Response Relationship, Drug , Edema/chemically induced , Free Radical Scavengers/chemistry , Models, Molecular , Molecular Structure , Picrates/chemistry , Pyrazoles/chemical synthesis , Pyrazoles/chemistry , Rats , Stereoisomerism , Structure-Activity Relationship , Superoxides/chemistry
17.
Bioorg Med Chem ; 20(18): 5649-57, 2012 Sep 15.
Article in English | MEDLINE | ID: mdl-22901670

ABSTRACT

Claisen-Schmidt condensation of 3-formyl-9-methylcarbazole with various amides of 3-aminoacetophenone afforded N-{3-[3-(9-methyl-9H-carbazol-3-yl)-acryloyl]-phenyl}-benzamide/amide derivatives. All compounds were investigated for their in vitro xanthine oxidase (XO), tyrosinase and melanin production inhibitory activity. Most of the target compounds had more potent XO inhibitory activity than the standard drug (IC(50) = 4.3-5.6 µM). Interestingly, compound 7q bearing cyclopropyl ring was found to be the most potent inhibitor of XO (IC(50) = 4.3 µM). Molecular modelling study gave an insight into its binding modes with XO. Compounds 7a, 7d, 7e, 7g, and 7k were found to be potent inhibitors of tyrosinase (IC(50) = 14.01-17.52 µM). These results suggest the possible use of these compounds for the design and development of novel XO and tyrosinase inhibitors.


Subject(s)
Benzamides/pharmacology , Carbazoles/pharmacology , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Melanoma, Experimental/drug therapy , Monophenol Monooxygenase/antagonists & inhibitors , Xanthine Oxidase/antagonists & inhibitors , Animals , Benzamides/chemical synthesis , Benzamides/chemistry , Carbazoles/chemical synthesis , Carbazoles/chemistry , Cell Survival/drug effects , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemistry , Melanins/antagonists & inhibitors , Melanins/biosynthesis , Melanoma, Experimental/metabolism , Melanoma, Experimental/pathology , Mice , Models, Molecular , Monophenol Monooxygenase/metabolism , Structure-Activity Relationship , Xanthine Oxidase/metabolism
18.
J Enzyme Inhib Med Chem ; 27(2): 267-74, 2012 Apr.
Article in English | MEDLINE | ID: mdl-21679049

ABSTRACT

Claisen-Schmidt condensation of 3-(1,2,3,6-tetrahydro-1-methylpyridin-4-yl)-2,4,5- trimethoxybenzaldehyde 3 and various aromatic, heterocyclic and alicyclic amides of 3- aminoacetophenone 6(a-s) afforded novel curcumin mimics. All the synthesized compounds were characterized by IR, (1)H NMR, Mass spectroscopy and evaluated for antioxidant, cytotoxicity and antimicrobial activity. Out of the 20 compounds screened, compounds 7i, 7l, 7q, and 7n have shown excellent radical scavenging activity, compounds 7o, 7t, 7f, and 7r have shown significant xanthine oxidase inhibition, and compounds 7a, 7k and 7l were found to be potent inhibitors of selected cancer cell lines. Compounds 7h, 7t, 7l, 7i, and 7e have shown good antibacterial activity, whereas compounds 7j, 7f, 7o, 7h, and 7t exhibited significant antifungal activity.


Subject(s)
Anti-Infective Agents/pharmacology , Antineoplastic Agents/pharmacology , Antioxidants/pharmacology , Biomimetics , Cell Proliferation/drug effects , Curcumin/chemistry , Enzyme Inhibitors/pharmacology , Anti-Infective Agents/chemical synthesis , Antineoplastic Agents/chemical synthesis , Antioxidants/chemical synthesis , Bacteria/drug effects , Curcumin/pharmacology , Enzyme Inhibitors/chemical synthesis , Fungi/drug effects , Humans , Neoplasms/drug therapy , Structure-Activity Relationship , Tumor Cells, Cultured , Xanthine Oxidase/antagonists & inhibitors
19.
J Assoc Physicians India ; 59: 258-60, 2011 Apr.
Article in English | MEDLINE | ID: mdl-21755767

ABSTRACT

A 61 year old male, with a bilateral persistent and recurrent pleural effusion, had undergone frequent tapping over a period of eight months, prior to the referral. The patient was treated earlier to the referral empirically for pulmonary tuberculosis with no response to the treatment. Malignancy was suspected and ruled out. A detailed examination showed that he also had atrophic nails with yellow discoloration and lymphedema of feet. Yellow nail syndrome was diagnosed on the basis of the clinical findings of the triad viz. yellow atrophic nails, lymphedema and bilateral pleural effusions. Pathogenesis still remains elusive for the syndrome. Pleurodesis provided both symptomatic relief and a respite from repeated tapping. The case is presented as a rare condition, which was missed for diagnosis, for quite some time by several specialists.


Subject(s)
Lymphedema/diagnosis , Pleural Effusion/diagnosis , Pleural Effusion/therapy , Yellow Nail Syndrome/diagnosis , Humans , Lymphedema/complications , Male , Middle Aged , Pleural Effusion/complications , Pleurodesis , Talc/therapeutic use , Yellow Nail Syndrome/complications
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