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New 4‐[(1‐Benzyl‐1 H ‐indol‐3‐yl)carbonyl]‐3‐hydroxyfuran‐2(5 H )‐ones, β‐Diketo Acid Analogs as HIV‐1 Integrase Inhibitors
Author(s) -
Ferro Stefania,
Barreca Maria Letizia,
De Luca Laura,
Rao Angela,
Monforte Anna Maria,
Debyser Zeger,
Witvrouw Myriam,
Chimirri Alba
Publication year - 2007
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700066
Subject(s) - integrase , moiety , chemistry , integrase inhibitor , stereochemistry , cytotoxicity , chemical synthesis , enzyme inhibitor , enzyme , combinatorial chemistry , biological activity , human immunodeficiency virus (hiv) , structure–activity relationship , in vitro , biochemistry , dna , medicine , family medicine , antiretroviral therapy , viral load
In addition to our recent report on a series of rationally designed benzylindolyldiketo acids acting as potent HIV‐1 integrase strand transfer inhibitors, we disclose the results obtained with novel compounds chemically modified on the diketo acid moiety in order to investigate its influence on the biological activity and cytotoxicity. The activity of designed and synthesized 4‐[(1‐benzyl‐1 H ‐indol‐3‐yl)carbonyl]‐3‐hydroxyfuran‐2(5 H )‐one derivatives lies in the micromolar range with regard to HIV IN enzymatic activity. The microwave‐assisted synthesis was employed in some steps of the chemical procedures.