ChemInform Abstract: Tricyclic Ureas: A New Class of HIV-1 Protease Inhibitors

Autor:	Jeffrey C. Pelletier, Wei Han, C. Nicholas Hodge
Rok vydání:	2010
Předmět:	chemistry.chemical_classification Protease biology Molecular model Chemistry Stereochemistry Pinacol medicine.medical_treatment General Medicine chemistry.chemical_compound HIV-1 protease medicine Side chain biology.protein Stereoselectivity Proline Tricyclic
Zdroj:	ChemInform. 30
ISSN:	1522-2667 0931-7597
Popis:	A new class of tricyclic ureas containing a conformationally constrained proline was designed with the aid of molecular modeling. Efficient stereoselective intermolecular pinacol coupling represented the highlight of the synthesis. These rigid cyclic ureas are active towards HIV-1 protease, with 9 being the most potent compound (Ki = 9 nM) despite interacting with only three side chain binding pockets of HIV protease.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::1702ce14f5f452f9d1ac49cf057a9684 https://doi.org/10.1002/chin.199917166 Zobrazit plný text záznamu Plný text