The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 52-52-8, Name is 1-Aminocyclopentanecarboxylic acid, SMILES is O=C(C1(CCCC1)N)O, in an article , author is Yang, Dongyan, once mentioned of 52-52-8, Application In Synthesis of 1-Aminocyclopentanecarboxylic acid.
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones
In this study, three novel series of benzoxazinone, benzothiopyranone and benzopyranone derivatives were designed through scaffold morphing from benzothiazinones to target DprE1. All compounds were evaluated for their in vitro activities against Mycobacterium tuberculosis and cytotoxicity against Vero cell line. Among these three series, the benzothiopyranone series displayed excellent antimycobacterial activity and low cytotoxicity. In particular, compound 6b exhibited potent in vitro activity against both drug-susceptible and drug-resistant tuberculosis clinical strains with MICs <0.016 mu g/mL. In addition, compound 6b demonstrated excellent ADME/T and PK properties and potent in vivo efficacy with bactericidal activity in an acute mouse model of tuberculosis. The antituberculosis effect of compound 6b is most likely attributed to its excellent anti-DprE1 activity. As such, compound 6b is under evaluation as a potential clinical candidate for treatment of tuberculosis. The current study provided new insight into the structural and pharmacological requirements for DprE1 inhibitors as potent antitubercular agents. (C) 2018 Elsevier Masson SAS. All rights reserved. Interested yet? Read on for other articles about 52-52-8, you can contact me at any time and look forward to more communication. Application In Synthesis of 1-Aminocyclopentanecarboxylic acid.