Hidaka Koushi, Kimura Tooru, Hayashi Yoshio, McDaniel Keith F, Dekhtyar Tatyana, Colletti Lynn, Kiso Yoshiaki
Department of Medicinal Chemistry, Center of Frontier Reseach in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Japan.
Bioorg Med Chem Lett. 2003 Jan 6;13(1):93-6. doi: 10.1016/s0960-894x(02)00848-x.
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.
设计并合成了含有新型HMC-酰肼电子等排体作为过渡态模拟物的伪对称HIV-1蛋白酶抑制剂。该核心单元周围P和P'位点具有不同结构的大多数合成化合物对HIV-1蛋白酶表现出有效的抑制活性，其抑制常数（K(i)）值为纳摩尔级别。
