Synthesis and Anti-HIV-1 Activity of New Delavirdine Analogues Carrying Arylpyrrole Moieties

Gérard Aimè PINNA; Giovanni LORIGA; Gabriele MURINEDDU; Giuseppe GRELLA; Massimo MURA; Laura VARGIU; Chiara MURGIONI; Paolo LA COLLA

doi:10.1248/cpb.49.1406

Regular Articles

Synthesis and Anti-HIV-1 Activity of New Delavirdine Analogues Carrying Arylpyrrole Moieties

Gérard Aimè PINNA, Giovanni LORIGA, Gabriele MURINEDDU, Giuseppe GRELLA, Massimo MURA, Laura VARGIU, Chiara MURGIONI, Paolo LA COLLA

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Keywords: delavirdine analogue, arylpyrrole motif synthesis, anti-human immunodeficiency virus (HIV) activity

JOURNAL FREE ACCESS

2001 Volume 49 Issue 11 Pages 1406-1411

DOI https://doi.org/10.1248/cpb.49.1406

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Abstract

In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC₅₀) values in the submicromolar range.

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