Literature DB >> 30119957

Design, synthesis and evaluation of oxime-functionalized nitrofuranylamides as novel antitubercular agents.

Yi-Lei Fan1, Jian-Bing Wu2, Xing Ke2, Zhong-Ping Huang3.   

Abstract

A series of oxime-functionalized nitrofuranylamides were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against MTB H37Rv and drug-resistant clinical isolates. Among them, two compounds 7a and 7b exhibited excellent activity against the three tested strains. Both of them were comparable to the first-line anti-TB agents INH and RIF against MTB H37Rv, and were far more potent than INH and RIF against MDR-TB 16833 and 16995 strains. Thus, both of them could act as leads for further optimization.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anti-mycobacterial; Anti-tubercular; Multi-drug resistant; Nitrofuran; Nitrofuranylamides; Oxime; Structure-activity relationship

Mesh:

Substances:

Year:  2018        PMID: 30119957     DOI: 10.1016/j.bmcl.2018.07.046

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Optimization of N-benzyl-5-nitrofuran-2-carboxamide as an antitubercular agent.

Authors:  Ricardo Gallardo-Macias; Pradeep Kumar; Mark Jaskowski; Todd Richmann; Riju Shrestha; Riccardo Russo; Eric Singleton; Matthew D Zimmerman; Hsin Pin Ho; Véronique Dartois; Nancy Connell; David Alland; Joel S Freundlich
Journal:  Bioorg Med Chem Lett       Date:  2018-12-24       Impact factor: 2.823

2.  Oxy-imino saccharidic derivatives as a new structural class of aldose reductase inhibitors endowed with anti-oxidant activity.

Authors:  Felicia D'Andrea; Stefania Sartini; Ilaria Piano; Matteo Franceschi; Luca Quattrini; Lorenzo Guazzelli; Lidia Ciccone; Elisabetta Orlandini; Claudia Gargini; Concettina La Motta; Susanna Nencetti
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.