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Pyrrolidine‐containing or Piperazine‐containing Nitrofuranylamides: Design, Synthesis, and In Vitro Anti‐mycobacterial Activities
Author(s) -
Zhao ShiJia,
Lv ZaoSheng,
Deng JiaLun,
Zhang GuangDe,
Xu Zhi
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3340
Subject(s) - chemistry , piperazine , rifampicin , isoniazid , pyrrolidine , mycobacterium tuberculosis , minimum inhibitory concentration , in vitro , tuberculosis , ic50 , microbiology and biotechnology , multiple drug resistance , antibiotics , stereochemistry , biochemistry , organic chemistry , medicine , biology , pathology
We report herein the design, synthesis, and in vitro anti‐mycobacterial activities of 11 pyrrolidine‐containing or piperazine‐containing nitrofuranylamides. Results revealed that all derivatives 3a–k endowed with excellent activity [minimum inhibitory concentration (MIC): <0.016–0.482 μg/mL] against Mycobacterium tuberculosis (MTB) H37Rv strain and more than half of them were more potent than the first‐line anti‐tuberculosis agents isoniazid (MIC: 0.078 μg/mL) and rifampicin (MIC: 0.078 μg/mL). The most active six derivatives were further evaluated against two clinically isolated multidrug‐resistant MTB strains resistant to both of isoniazid and rifampicin. In particular, four of them 3a , 3c , 3d , and 3j (MIC: 1.412–3.230 μg/mL) showed promising activity against the two clinically isolated multidrug‐resistant MTB strains and could act as starting points for further investigation.