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

被引：41

作者：

Bennani, B. ^{[1
]}

Kerbal, A. ^{[1
]}

Daoudi, M. ^{[1
]}

Baba, B. Filali ^{[1
]}

Al Houari, G. ^{[1
]}

Jalbout, A. F. ^{[2
]}

Mimouni, M.

Benazza, M. ^{[4
]}

Demailly, G. ^{[4
]}

Akkurt, M. ^{[5
]}

Yildirim, S. S. Oeturrk ^{[5
]}

Ben Hadda, T. ^{[3
]}

机构：

[1] Fac Sci Dhar El Mehraz, Chim Organ Lab, Fes, Morocco

[2] Arizona State Univ, Dept Chem, Tempe, AZ 85287 USA

[3] Fac Sci, Lab Chim Mat, Oujda 60000, Morocco

[4] UPJV, Lab Glucides, UMR 6219, F-80039 Amiens, France

[5] Erciyes Univ, FAS, Dept Phys, TR-38039 Kayseri, Turkey

来源：

ARKIVOC | 2007年

关键词：

tuberculosis; HIV-1; spiro-isoxazolines; combined pharmacophore sites;

D O I：

10.3998/ark.5550190.0008.g03

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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 mu g/mL and two new potential anti-HIV-1 inhibitors.

引用

页码：19 / 40

页数：22

共 22 条

[1] 3-Nitroso-2-phenylimidazo[1,2-a]pyrimidine [J].