STUDY OF THE EVALUATION OF MUTAGENIC EFFECTS OF ANTIMALARIAL DRUG CHLOROQUINE IN AMES SALMONELLA ASSAY

Antimalarial drugs are frequently administered to people in topical regions of the world. It is known that commonly used antimalarial drug Chloroquine binds strongly to deoxyribonucleic acid (DNA).  In the present study the mutagenic effects of antimalarial drug Chloroquine was evaluated in the Ames Salmonella assay .CHQ is the most commonly used antimalarial drug at present in different parts of the world. After the malaria parasite Plasmodium falciparum started to develop widespread resistance to CHQ, new potential utilizations of this cheap and widely available drug have been investigated. CHQ has been extensively used in mass drug administration’s which may have contributed to the emergence and spread of resistance. As it mildly suppresses the immune system, it is used in some autoimmune disorders, such as rheumatoid arthritis. CHQ is in clinical trials as an investigational antiretroviral in humans with HIV-1/AIDS The results of the mutagenicity assay indicate that chloroquine is a weak mutagen in Salmonella strain TA100. CHQ showed a very weak mutagenic effect in the absence of S9 mix in strain TA100. But this compound didn’t show any mutagenic effect on TA98 strain both in presence or absence of S9 mix. This observation suggests that metabolic products of CHQ might not play a significant role in induction of mutation. Keywords: Chloroquine, Ames Salmonella assay, mutagenic effec

METHOD DEVELOPMENT AND VALIDATION FOR ESTIMATION OF IRBESARTAN IN BULK DRUG AND PHARMACEUTCAL DOSAGE

Simple, sensitive, accurate, precise and rapid ultraviolet (UV) spectrophotometric method was developed for the estimation of Irebesartan  in pure form, its formulations and stability samples. Sample recovery in both the formulations using the above method was in good agreement with their respective labeled claims, thus suggesting the validity of the method and non-interference of formulation excipients in the estimation. Detection wavelength was selected as 263 nm Linearity in response was observed in the range of 10-100 µg/ml having R2 = 0.999. ( R2= not less then  .996 ) The regeration equ. y= y=mx+c was calculated   as Y = The sandell’s sensitivity for the developed method was found to be1.6269. The values were founds to be within the official limit. The percentage purity of three different samples, 12, 14, and 16µg/ml was found to be 92.44 ,87.49, 83.47respectively. The percentage recovery results revealed that the value is 100%, which indicates that the proposed method is accurate as the results are within the official limits. Keywords: ultraviolet (UV) spectrophotometric method, Irebesrtan ,recovery experiment ,determination of linearit

SYNTHESIS AND BIOLOGICAL EVALUTION OF 3-CHLORO 2- METHYL PHENYL CARBAMOYL SUBSTITUTED SEMICARBAZONE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS

ABSTRACT A series of 3-chloro 2-methyl phenyl carbamoyl substituted semicarbazones (4-21) was synthesized and evaluated for anticonvulsant and CNS activities. The anticonvulsant activity of the synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximal electroshock seizure, subcutaneous pentylenetetrazole, and subcutaneous strychnine-induced seizure screens. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration . . Aryl semicarbazides have also been reported to display excellent anticonvulsant activity in mice and rats . In terms of interaction at the binding site, as proposed previously by Dimmock et al. the pharma-cophoric elements were thought to be a lipophilic aryl ring and hydrogen bonding semicarbazone moiety. The attach-ment of a second aryl ring designated as the distal ring to the proximal aryl ring to increase the van der Waal's bonding at the binding site and to increase potency have also been reported. Substitutions in the aryl ring by halogens have been found to increase potency in the MES screen

A key review on oxadiazole analogs as potential methicillin-resistant Staphylococcus aureus (MRSA) activity: structure-activity relationship studies

Methicillin-resistant Staphylococcus aureus (MRSA) is becoming dangerous to human beings due to easy transmission mode and leading to the difficult-to-treat situation. The rapid resistance development of MRSA to many approved antibiotics is of major concern. There is a lot of scope to develop novel, efficient, specific, and nontoxic drug candidates to fight against MRSA isolates. The interesting molecular structure and adaptable feature of oxadiazole moiety which are bioisosteres of esters and amides, and these functional groups show improved resistance to esterases mediated hydrolytic cleavage, attracting researchers to develop required novel antibiotics based on oxadiazole core. This review summarizes the developments of oxadiazole-containing derivatives as potent antibacterial agents against multidrug-resistant MRSA strains and discussing the structure-activity relationship (SAR) in various directions. The current survey is the highlight of the present scenario of oxadiazole hybrids on MRSA studies, covering articles published from 2011 to 2020. This collective information may become a good platform to plan and develop new oxadiazole-based small molecule growth inhibitors of MRSA with minimal side effects. (C) 2021 Elsevier Masson SAS. All rights reserved