title: Modified calanolides incorporated with furan-2-nitro mimics against Mycobacterium tuberculosis.
abstract: (+)-Calanolide A was identified as an active agent against both HIV-1 and Mycobacterium tuberculosis (Mtb). We modified Ring D of calanolide compounds with furan-2-nitro mimics and obtained 15 compounds. After in vitro tests, two compounds were shown to be active against replicating (R) Mtb, but not against non-replicating (NR) Mtb. Further optimization for potent candidates against both R Mtb and NR Mtb will result from this research.
authors: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors: Zijie
authors: Z
authors: Liu
authors: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors: Xiaoyong
authors: X
authors: Guo
authors: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Tsinghua-Peking Center for Life Sciences and Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing 100084, China. Electronic address: gangliu27@tsinghua.edu.cn.
authors: Gang
authors: G
authors: Liu
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D005663:Furans / Q000737:chemistry*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D039681:Pyranocoumarins / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000995:Antitubercular Agents; D005663:Furans; D039681:Pyranocoumarins; C039281:furan
keywords: (+)-Calanolide A; Benzofuran; Mycobacterium tuberculosis; Nature product