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Substituted alkylpyridines as P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles

✍ Scribed by B. Moon Kim; Colleen M. Hanifin; C. Blair Zartman; Joseph P. Vacca; Stuart R. Michelson; Jiunn H. Lin; I.-W. Chen; Kari Vastag; Paul L. Darke; Joan A. Zugay; Emilio A. Emini; William Schleif; Paul S. Anderson; Joel R. Huff


Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
277 KB
Volume
5
Category
Article
ISSN
0960-894X

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✍ B. Moon Kim; James P. Guare; Joseph D. Vacca; Stuart R. Michelson; Paul L. Darke 📂 Article 📅 1995 🏛 Elsevier Science 🌐 English ⚖ 297 KB

A series of hydroxyethylpiperazine HIV-1 protease inhibitors containing various monocyclic or bicyclic thienylmethyl substituents as Py ligands were prepared. They were found to exhibit extremely high potency in the enzyme inhibition assay. These inhibitors also proved to be highly effective against