Design of Second Generation HIV-1 Integrase Inhibitors

Title: Design of Second Generation HIV-1 Integrase Inhibitors

Volume: 13 Issue: 2

Author(s): Jinxia Deng, Raveendra Dayam, Laith Q. Al-Mawsawi and Nouri Neamati

Affiliation:

Keywords: HIV-1 integrase inhibitor, S-1360, L-870, 810, Antiretroviral drugs, Pharmacophore, Database screening

Abstract: The prospect of HIV-1 integrase (IN) as a therapeutically viable retroviral drug target is on the verge of realization. The observed preclinical and clinical performance of β-diketo containing and naphthyridine carboxamide compounds provides direct proof for the clinical application of IN inhibition. These validated lead compounds are useful in the design and development of second generation IN inhibitors. The results from preclinical and clinical studies on the first generation IN inhibitors reiterate a demand for novel second generation inhibitors with improved pharmacokinetic and metabolic properties. Pharmacophore-based drug design techniques facilitate the discovery of novel compounds on the basis of validated lead compounds specific for a drug target. In this article we have comprehensively reviewed the application of pharmacophore-based drug design methods in the field of IN inhibitor discovery.

Cite this article as:

Deng Jinxia, Dayam Raveendra, Al-Mawsawi Q. Laith and Neamati Nouri, Design of Second Generation HIV-1 Integrase Inhibitors, Current Pharmaceutical Design 2007; 13 (2) . https://dx.doi.org/10.2174/138161207779313687