期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 22, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127576
关键词
4-aminoquinoline-isoindoline-dione-isoniazid; Anti-mycobacterial activity; Cytotoxicity; Selectivity index; Molecular docking
资金
- Council of Scientific and Industrial Research, New Delhi, India [09/254(0269)/2017-EMR-I]
- Labex EpiGenMed under the program Investissements d'avenir [ANR-10-LABX-12-01]
- Fondation pour la Recherche Medicale (FRM) [DEQ20150331719]
- National Research Foundation (NRF), South Africa [121276]
A series of 4-aminoquinoline-isoindoline-dione-isoniazid triads were synthesized and assessed for their antimycobacterial activities and cytotoxicity. Most of the synthesized compounds exhibited promising activities against the mc26230 strain of M. tuberculosis with MIC in the range of 5.1-11.9 mu M and were non-cytotoxic against Vero cells. The conjugates lacking either isoniazid or quinoline core in their structural framework failed to inhibit the growth of M. tuberculosis; thus, further strengthening the proposed design of triads in the present study.
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