Title of article
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides Original Research Article
Author/Authors
Naoyuki Masuda، نويسنده , , Osamu Yamamoto، نويسنده , , Masahiro Fujii، نويسنده , , Tetsuro Ohgami، نويسنده , , Jiro Fujiyasu، نويسنده , , Toru Kontani، نويسنده , , Ayako Moritomo، نويسنده , , Masaya Orita، نويسنده , , Hiroyuki Kurihara، نويسنده , , Hironobu Koga، نويسنده , , Hideaki Nakahara، نويسنده , , Shunji Kageyama، نويسنده , , Mitsuaki Ohta، نويسنده , , Hiroshi Inoue، نويسنده , , Toshifumi Hatta، نويسنده , , Hiroshi Suzuki، نويسنده , , Kenji Sudo، نويسنده , , Yasuaki Shimizu، نويسنده , , Eiichi Kodama، نويسنده , , Masao Matsuoka، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
12
From page
6171
To page
6182
Abstract
A random high-throughput screening (HTS) program to discover novel nonnucleoside reverse transcriptase inhibitors (NNRTIs) has been carried out with MT-4 cells against a nevirapine-resistant virus, HIV-1IIIB-R. The primary hit, a thiazolidenebenzenesulfonamide derivative, possessed good activity. A systematic modification program examining various substituents at the 3-, 4-, and 5-positions on the thiazole ring afforded compounds with enhanced anti-HIV-1 and reverse transcriptase (RT) inhibitory activities. These results confirm the important role of the substituents at these positions and the thiazolidenebenzenesulfonamide motif as a valuable lead series for the next generation NNRTIs.
Keywords
Benzenesulfonamide , Nonnucleoside HIV-1 reverse transcriptase inhibitor , Thiazolidene
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2004
Journal title
Bioorganic and Medicinal Chemistry
Record number
1303373
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