Synthesis and Anti‐HIV‐1 Evaluation of Some Novel MC‐1220 Analogs as Non‐Nucleoside Reverse Transcriptase Inhibitors. Issue 5 (21st March 2016)

• Record Type: Journal Article
• Authors: Loksha, Yasser M.; Pedersen, Erik B.; Loddo, Roberta; La Colla, Paolo
• Is Part Of: Archiv der Pharmazie. Volume 349:Issue 5(2016)
• Page Start: 363
• Page End: 372
• Publication Date: 2016-03-21
• Subjects: 4, 6‐Dichloro‐N, N‐dimethylpyrimidin‐2‐amine -- 2, 6‐Difluorobenzyl cyanide -- HIV‐1 -- MC‐1220 analogs -- Non‐nucleoside reverse transcriptase inhibitor (NNRTI); Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201600008
• Languages: English
• ISSNs: 0365-6233

Abstract

Abstract : Some novel MC‐1220 analogs were synthesized by condensation of 4, 6‐dichloro‐ N‐ methylpyrimidin‐2‐amine derivatives (1a, b and15) and/or 4‐chloro‐6‐methoxy‐ N, N, 5‐trimethylpyrimidin‐2‐amine (2a ) with the sodium salt of 2, 6‐difluorophenylacetonitrile followed by treatment with aqueous sodium hydroxide in methanol, alkylation, reduction, halogenation, and/or acidic hydrolysis. All synthesized compounds were evaluated for their activity against HIV‐1. The most active compound in this study was compound7, which showed activity against HIV‐1 comparable to that of MC‐1220. The only difference in structure between compound7 and MC‐1220 is a fluoro atom instead of a CH3 group. Abstract : Novel MC‐1220 analogs were synthesized and evaluated for their anti‐HIV‐1 effect, by measuring their non‐nucleoside reverse transcriptase inhibitory activity. Compound7 as the most active compound in this study showed activity against HIV‐1 comparable to that of MC‐1220. The only difference in structure between compound7 and MC‐1220 is a fluoro atom instead of a CH3 group.