Combined drug design of potential Mycobacterium tuberculosis and HIV-1 inhibitors: 3′,4′-di-substituted -4′H-spiro [isothiochromene-3,5′-isoxazol]-4(1H)-one

Bennani, B.; Kerbal, A.; Daoudi, M.; Baba, B.; Al Houari, G.; Jalbout, A.; Mimouni, M.; Benazza, M.; Demailly, G.; AKKURT, MEHMET; Yildirim, SEMA; Ben Hadda, T.

doi:10.3998/ark.5550190.0008.g03

Combined drug design of potential Mycobacterium tuberculosis and HIV-1 inhibitors: 3′,4′-di-substituted -4′H-spiro [isothiochromene-3,5′-isoxazol]-4(1H)-one

Bennani B., Kerbal A., Daoudi M., Baba B. F., Al Houari G., Jalbout A. F., ...More

Arkivoc, vol.2007, no.16, pp.19-40, 2007 (SCI-Expanded, Scopus)

Publication Type: Article / Article
Volume: 2007 Issue: 16
Publication Date: 2007
Doi Number: 10.3998/ark.5550190.0008.g03
Journal Name: Arkivoc
Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Page Numbers: pp.19-40
Keywords: tuberculosis, HIV-1, spiro-isoxazolines, combined pharmacophore sites
Open Archive Collection: AVESIS Open Access Collection
Erciyes University Affiliated: Yes

Abstract

We report herein the design and synthesis of 17 new spiroheterocycles 10-26, on the basis of two hypothetical pharmacophore structures designed to interact with both of Mycobacterium tuberculosis bacteria and HIV-1 virus. The in vitro biological evaluation of these compounds allowed us to point out seven new potential non-nucleoside hits, with MIC values in the range of 6.25 μg/mL and two new potential anti-HIV-1 inhibitors. ©ARKAT USA, Inc.