期刊
ARCHIV DER PHARMAZIE
卷 355, 期 10, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.202200224
关键词
antitubercular activity; antiviral activity; influenza virus; nicotinohydrazide; spirothiazolidinone
资金
- Bilimsel Arastirma Projeleri Birimi, Istanbul Universitesi [22981]
We synthesized a novel series of hybrid spirothiazolidinone derivatives and evaluated their antiviral and antitubercular activities. Some of these compounds showed specific antiviral activity against the influenza A/H3N2 virus, with the most active compound being 3a with an antiviral EC50 value of 5.2μM. In addition, some compounds also exhibited inhibitory activity against Mycobacterium tuberculosis.
We here report the synthesis, structural characterization, and evaluation of the antiviral and antitubercular activities of a novel series of hybrid spirothiazolidinone derivatives (2a-f and 3a-f) containing the nicotinohydrazide moiety, which is an isomer form of the approved antitubercular drug isoniazid. When evaluated for activity against influenza A/H1N1, A/H3N2, and B viruses, three of the new compounds proved to possess specific antiviral activity against the influenza A/H3N2 virus. The most active analog 3a, bearing a 2,8-dimethyl group at the spiro ring, displayed an antiviral EC50 value of 5.2 mu M. Compound 3a produced no cytotoxicity at 100 mu M, the highest concentration tested, giving a selectivity index of at least 19. Structure-activity relationship analysis indicated that the absence of the methyl substituent at the 2-position and the presence of a bulky substituent at the 8-position of the spirothiazolidinone system caused a significant decrease in antiviral activity. The in vitro antitubercular activity of compounds 2a-f and 3a-f was determined for six different drug-sensitive/drug-resistant laboratory strains and clinical isolates of Mycobacterium tuberculosis. Compounds 2c, 2d, 3b, 3c, and 3d showed weak antitubercular activity against different strains, with MIC values of 125-250 mu M.
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