| Literature DB >> 15519161 |
Naoyuki Masuda1, Osamu Yamamoto, Masahiro Fujii, Tetsuro Ohgami, Jiro Fujiyasu, Toru Kontani, Ayako Moritomo, Masaya Orita, Hiroyuki Kurihara, Hironobu Koga, Hideaki Nakahara, Shunji Kageyama, Mitsuaki Ohta, Hiroshi Inoue, Toshifumi Hatta, Hiroshi Suzuki, Kenji Sudo, Yasuaki Shimizu, Eiichi Kodama, Masao Matsuoka, Masatoshi Fujiwara, Tomoyuki Yokota, Shiro Shigeta, Masanori Baba.
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-1(IIIB-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.Entities:
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Year: 2004 PMID： 15519161 DOI： 10.1016/j.bmc.2004.08.050
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641