Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists

Autor:	Jaclyn R. Patterson, Scott K. Thompson, Harvey E. Fries, Eugene T. Grygielko, Walter Trizna, Tram H. Hoang, Jeffrey D. Bray, Nicholas J. Laping, Douglas J. Minick, Melanie Nord, Lindsay E. Glace, Rakesh Nagilla, Marlys Hammond, Sharada Manns, David G. Washburn
Rok vydání:	2009
Předmět:	Agonist medicine.drug_class Stereochemistry Clinical Biochemistry Triazole Pharmaceutical Science Tetrazoles Biochemistry Chemical synthesis Partial agonist chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Progesterone receptor medicine Structure–activity relationship Animals Tetrazole Amino Acids Molecular Biology chemistry.chemical_classification Organic Chemistry Amino acid Rats chemistry Molecular Medicine Receptors Progesterone
Zdroj:	Bioorganicmedicinal chemistry letters. 19(10)
ISSN:	1464-3405
Popis:	Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands behaved as potent partial agonists, while the 1,2,4-triazole ligands behaved as potent full agonists.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b908a6958d1dc4b3fe1c567457b4850 https://pubmed.ncbi.nlm.nih.gov/19376703 Zobrazit plný text záznamu Full Text from ScienceDirect