Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and-alkylamino analogs

…, RB Levin, JA O'Brien, ME Goldman

文献索引：Hoffman; Wai; Thomas; Levin; O'Brien; Goldman Journal of Medicinal Chemistry, 1992 , vol. 35, # 21 p. 3784 - 3791

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被引用次数: 50

摘要

A potent (ICs0= 30 nM), specific nonnucleoside HIV-1 reverse transcriptase (RT) inhibitor 3- [N-(phthalimidomethyl) aminol-5-ethyl-6-methylpyridin-2 (1H)-one (l), was discovered through an in vitro screening program. This compound did not inhibit (ICs0> 300 pm) other DNA and RNA polymerases, including HIV-2 RT and SIV-RT. Unfortunately, hydrolytic instability of this (aminomethy1) phthalimide precluded use as an antiviral agent. In the ...