Synthesis and Quantitative Structure-Activity Relationship Analysis of 2-(Aryl or Heteroaryl)quinolin-4-amines, a New Class of Anti-HIV-1 Agents

Lucjan Strekowski, Vidya A. Honkan, Agnieszka Czarny, Marek T. Cegla, Roman L. Wydra, Steven Patterson, Raymond F. Schinazi

Research output: Contribution to journalArticlepeer-review

157 Scopus citations

Abstract

Thirty-eight 2-(aryl or heteroaryl)quinolin-4-amines, N,N-disubstituted, N-monosubstituted, and without a substituent at the amino group have been synthesized with use of novel chemistries developed by us recently. Some of these derivatives show anti-HIV-1 activity at a concentration level of 1 μM and low cell toxicity in vitro. The most active and least toxic compounds are derivatives of 2-(3-pyridyl)quinoline. The results of the quantitative structure-activity relationship analyses, including several classical, linear regression correlations and a Free-Wilson approach of de novo model, provide guidelines for the design of new active compounds of this class.

Original languageEnglish (US)
Pages (from-to)1739-1746
Number of pages8
JournalJournal of medicinal chemistry
Volume34
Issue number5
DOIs
StatePublished - May 1 1991

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