Evaluation of heteroatom-rich derivatives as antitubercular agents with InhA inhibition properties
Sign Up to like & getrecommendations! Published in 2017 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-017-2064-x
Abstract: Two series of heterocyclic compounds derived from 3-acetyl-4-hydroxy-6-methyl-2H-pyran-2-one (DHA) and 2-acetylbutyrolactone have been synthesized and characterized. The compounds were evaluated for their activities against Mycobacterium tuberculosis strain, and as inhibitors of InhA, a key enzyme… read more here.
Keywords: antitubercular agents; rich derivatives; agents inha; evaluation heteroatom ... See more keywords
Benzene sulfonamide pyrazole thio-oxadiazole hybrid as potential antimicrobial and antitubercular agents
Sign Up to like & getrecommendations! Published in 2018 at "Research on Chemical Intermediates"
DOI: 10.1007/s11164-018-3396-y
Abstract: To fulfil the development goals towards the synthesis of innovative, potent and highly effective antimicrobial and antimycobacterial agents, a set of benzene sulfonamide pyrazole thio-oxadiazole derivatives (6a–6l) have been synthesized by the reaction of 4-[5-(3-fluoro-4-methoxyphenyl)-3-(5-mercapto-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl]benzenesulfonamide… read more here.
Keywords: pyrazole thio; antimicrobial antitubercular; antitubercular agents; benzene sulfonamide ... See more keywords
S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.11.041
Abstract: Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains,… read more here.
Keywords: antitubercular agents; dinitrophenyl oxadiazole; oxadiazole thiols; substituted dinitrophenyl ... See more keywords
Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00652
Abstract: The 6-trifluoro substituted 8-nitrobenzothiazinones (BTZs) represent a novel type of antitubercular agents, and their high antimycobacterial activity is related to the inhibition of decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1), an enzyme essential for the biosynthesis of mycobacterial cell… read more here.
Keywords: development methanesulfonyl; methanesulfonyl nitrobenzothiazinone; nitrobenzothiazinone based; methanesulfonyl ... See more keywords
Synthesis, Characterization, and Biological Evaluation of New Derivatives Targeting MbtI as Antitubercular Agents
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DOI: 10.3390/ph14020155
Abstract: Tuberculosis (TB) causes millions of deaths every year, ranking as one of the most dangerous infectious diseases worldwide. Because several pathogenic strains of Mycobacterium tuberculosis (Mtb) have developed resistance against most of the established anti-TB… read more here.
Keywords: antitubercular agents; characterization biological; biological evaluation; mbti ... See more keywords
Novel 1,3,4-oxadiazoles as antitubercular agents with limited activity against drug-resistant tuberculosis.
Sign Up to like & getrecommendations! Published in 2019 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2018-0378
Abstract: AIM In recent times, heterocyclic chemotypes are being explored for the development of new antimycobacterials that target the drug-resistant tuberculosis. Here, we are disclosing the 5-substitued 2-mercapto-1,3,4-oxadiazoles as potent antitubercular agents. METHODOLOGY A small library… read more here.
Keywords: antitubercular agents; drug resistant; tuberculosis; activity ... See more keywords