Search Results - "Reshma, Rudraraju Srilakshmi"
-
1
Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors
Published in European journal of medicinal chemistry (10-02-2018)“…In the present study, we attempted to develop novel class of Mycobacterium tuberculosis (Mtb) inhibitors by exploring the pharmaceutically underexploited…”
Get full text
Journal Article -
2
Synthesis, in vitro, and in vivo (Zebra fish) antitubercular activity of 7,8-dihydroquinolin-5(6H)-ylidenehydrazinecarbothioamides
Published in Bioorganic chemistry (01-03-2020)“…[Display omitted] •Twenty-two dihydroquinolinylidenehydrazinecarbothioamides 4a–v was synthesized.•Five compounds 4a, 4e, 4g, 4j and 4k were resulted as the…”
Get full text
Journal Article -
3
Lead identification and optimization of bacterial glutamate racemase inhibitors
Published in Bioorganic & medicinal chemistry (01-01-2018)“…[Display omitted] Mycobacterium tuberculosis glutamate racemase is an essential enzyme involved in peptidoglycan synthesis and conserved in most bacteria…”
Get full text
Journal Article -
4
Synthesis and anti-mycobacterial activity of 4-(4-phenyl-1H-1,2,3-triazol-1-yl)salicylhydrazones: revitalizing an old drug
Published in Archives of pharmacal research (01-02-2017)“…The antitubercular drug; para -aminosalicylic acid (PAS) was used as the core scaffold for the design of a series of 1 H -1,2,3-triazolylsalicylhydrazones upon…”
Get full text
Journal Article -
5
Design and development of novel inhibitors for the treatment of latent tuberculosis
Published in International journal of mycobacteriology (01-12-2016)“…Abstract Objective/background “The captain of all these men of death”, is the apt sobriquet for the age-old disease tuberculosis (TB). Despite the availability…”
Get full text
Journal Article -
6
Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors
Published in European journal of medicinal chemistry (21-10-2016)“…A structure based medium throughput virtual screening campaign of BITS-Pilani in house chemical library to identify novel binders of Mycobacterium tuberculosis…”
Get full text
Journal Article -
7
Synthesis and evaluation of 4′,5′-dihydrospiro[piperidine-4,7′-thieno[2,3-c]pyran] analogues against both active and dormant Mycobacterium tuberculosis
Published in Bioorganic & medicinal chemistry (01-05-2018)“…[Display omitted] Need for new drugs to fight against tuberculosis (TB) is increasing day by day. In the present work we have taken a spiro compound (GSK…”
Get full text
Journal Article -
8
A robust synthesis of functionalized 2H-indazoles via solid state melt reaction (SSMR) and their anti-tubercular activity
Published in Bioorganic & medicinal chemistry letters (01-04-2017)“…[Display omitted] A facile and convenient approach has been developed for the synthesis of functionalized indazoles via solid state melt reaction using easily…”
Get full text
Journal Article -
9
Engineering of Ancestors as a Tool to Elucidate Structure, Mechanism, and Specificity of Extant Terpene Cyclase
Published in Journal of the American Chemical Society (17-03-2021)“…Structural information is crucial for understanding catalytic mechanisms and to guide enzyme engineering efforts of biocatalysts, such as terpene cyclases…”
Get full text
Journal Article -
10
Lead derivatization of ethyl 6-bromo-2-((dimethylamino)methyl)-5-hydroxy-1-phenyl-1H-indole-3-carboxylate and 5-bromo-2-(thiophene-2-carboxamido) benzoic acid as FabG inhibitors targeting ESKAPE pathogens
Published in European journal of medicinal chemistry (15-01-2022)“…Our previous studies on FabG have identified two compounds 5-bromo-2-(thiophene-2-carboxamido) benzoic acid (A) and ethyl…”
Get full text
Journal Article -
11
A FabG inhibitor targeting an allosteric binding site inhibits several orthologs from Gram-negative ESKAPE pathogens
Published in Bioorganic & medicinal chemistry (15-01-2021)“…[Display omitted] •FabG from the bacterial fatty acid biosynthesis (FAS-II) system is a potential target for antibiotics.•Inhibitors were identified by…”
Get full text
Journal Article -
12
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors
Published in Bioorganic & medicinal chemistry (15-05-2017)“…[Display omitted] MTB lysine-ɛ-aminotransferase (LAT) was found to play a crucial role in persistence and antibiotic tolerance. LAT serves as a potential…”
Get full text
Journal Article -
13
Design and development of new class of Mycobacterium tuberculosis l-alanine dehydrogenase inhibitors
Published in Bioorganic & medicinal chemistry (15-09-2016)Get full text
Journal Article -
14
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors
Published in Bioorganic & medicinal chemistry (01-01-2016)“…This kind of compounds retains good potency and showed reduced cardiotoxicity compared to aminopiperidines. [Display omitted] Recently numerous…”
Get full text
Journal Article -
15
Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis
Published in Journal of medicinal chemistry (28-07-2016)“…Cysteine is an important amino acid in the redox defense of Mycobacterium tuberculosis, primarily as a building block of mycothiol. Genetic studies have…”
Get full text
Journal Article -
16
A robust synthesis of functionalized 2 H -indazoles via solid state melt reaction (SSMR) and their anti-tubercular activity
Published in Bioorganic & medicinal chemistry letters (01-04-2017)Get full text
Journal Article -
17
Profiling of in vitro activities of urea-based inhibitors against cysteine synthases from Mycobacterium tuberculosis
Published in Bioorganic & medicinal chemistry letters (01-10-2017)“…[Display omitted] CysK1 and CysK2 are two members of the cysteine/S-sulfocysteine synthase family in Mycobacterium tuberculosis, responsible for the de novo…”
Get full text
Journal Article -
18
Enabling the (3 + 2) cycloaddition reaction in assembling newer anti-tubercular lead acting through the inhibition of the gyrase ATPase domain: lead optimization and structure activity profiling
Published in Organic & biomolecular chemistry (01-01-2015)“…DNA gyrase, the sole type II topoisomerase present in Mycobacterium tuberculosis, is absent in humans and is a well validated target for anti-tubercular drug…”
Get more information
Journal Article -
19
Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors
Published in Bioorganic & medicinal chemistry (15-09-2016)“…[Display omitted] Mycobacterium tuberculosisl-alanine dehydrogenase (MTB l-AlaDH) is one of the important drug targets for treating latent/persistent…”
Get full text
Journal Article -
20
Structure-Guided Discovery of Antitubercular Agents That Target the Gyrase ATPase Domain
Published in ChemMedChem (04-03-2016)“…In this study we explored the pharmaceutically underexploited ATPase domain of DNA gyrase (GyrB) as a potential platform for developing novel agents that…”
Get full text
Journal Article