Ellis, David, Kuhen, Kelli, Anaclerio, Beth, Wu, Baogen, Wolff, Karen, Yin, Hong, Bursulaya, Badry, Caldwell, Jeremy, Karanewsky, Donald and He, Yun (2006) Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorganic & Medicinal Chemistry Letters, 16 (16). pp. 4246-4251. ISSN 0960-894X

Abstract

A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.05.073
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	Quinolones; HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI); SAR; Molecule modeling; HIV replication
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.05.073
Date Deposited:	14 Dec 2009 14:04
Last Modified:	31 Jan 2013 01:26
URI:	https://oak.novartis.com/id/eprint/146