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Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.

Ellis, David and Kuhen, Kelli and Anaclerio, Beth and Wu, Baogen and Wolff, Karen and Yin, Hong and Bursulaya, Badry and Caldwell, Jeremy and 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
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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
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:26
URI: https://oak.novartis.com/id/eprint/146

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