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Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides. 2004
Naoyuki Masuda, and
Osamu Yamamoto, and
Masahiro Fujii, and
Tetsuro Ohgami, and
Jiro Fujiyasu, and
Toru Kontani, and
Ayako Moritomo, and
Masaya Orita, and
Hiroyuki Kurihara, and
Hironobu Koga, and
Hideaki Nakahara, and
Shunji Kageyama, and
Mitsuaki Ohta, and
Hiroshi Inoue, and
Toshifumi Hatta, and
Hiroshi Suzuki, and
Kenji Sudo, and
Yasuaki Shimizu, and
Eiichi Kodama, and
Masao Matsuoka, and
Masatoshi Fujiwara, and
Tomoyuki Yokota, and
Shiro Shigeta, and
Masanori Baba
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co. Ltd, 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. masuda.naoyuki@yamanouchi.co.jp
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.
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