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Original Article

pnr. 2013; 4(1): 13-18


Lack of human immunodeficiency virus-1 integrase inhibitory activity of novel 3a, 4, 7, 7a-tetrahydro-1H-isoindole-1,3 (2H)-dione derivatives

Ashok Penta, Kakamanu Kishore Babu, Swastika Ganguly, Sankaranarayanan Murugesan.

Abstract
Background: Majority of reported integrase (IN) inhibitors had an important structural feature, i.e., 1,3-diketo functional group. It plays a vital role in IN inhibition by the formation of chelating triod with Mg +2 ions. Materials and Methods: A novel series of fifteen 3-(1,3-dioxo-3a, 4-dihydro-1H-isoindol-2 (3H,7H,7aH)-yl)-N-(substituted phenyl) propanamide 4(a-o) analogs were synthesized by reacting the corresponding 3-chloro-N-(substituted phenyl) propanamides 2(a-o) with 3a, 4,7,7a-tetrahydro-1H-isoindole-1,3 (2H)-dione (3) in acetonitrile medium in the presence of potassium carbonate. Various substituted 3-chloro-N-(substituted phenyl) propanamides 2(a-o) were synthesized by treating appropriate substituted anilines 1(a-o) with 3-chloro propionyl chloride in dichloromethane as solvent in the presence of triethylamine as base. The synthesized compounds have been characterized on the basis of fourier transform infrared spectrophotometerproton nuclear magnetic resonance spectrophotometer, 1 H NMR, Mass spectral and Elemental Analysis. Results: All the synthesized compounds were evaluated for their human immunodeficiency virus (HIV)-1 INinhibitory activity. However, unlike other anti-IN agents, none of these molecules showed inhibition of either 3' processing, and strand transfer reactions of HIV-1 IN.

Key words: Acquired immune deficiency syndrome, highly active anti-retroviral therapy, human immunodeficiency virus-1 integrase, tetrahydrophthalimide






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