Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere |
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| Authors: | Hidaka Koushi Kimura Tooru Hayashi Yoshio McDaniel Keith F Dekhtyar Tatyana Colletti Lynn Kiso Yoshiaki |
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| Affiliation: | Department of Medicinal Chemistry, Center of Frontier Reseach in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Japan. |
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| Abstract: | Pseudo-symmetric HIV-1 protease inhibitors containing a novel HMC-hydrazide isostere as the transition-state mimic were designed and synthesized. Most of the synthetic compounds with varied structures at the P and P' sites around this core unit showed potent inhibitory activity against HIV-1 protease with nanomolar K(i) values. |
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