CHEM 175-Medicnal Chemistry Drug Activiny asigment In a study by Chen Chen et al
ID: 963967 • Letter: C
Question
CHEM 175-Medicnal Chemistry Drug Activiny asigment In a study by Chen Chen et al published in 2009 in the Joumal of Medicinal Chemistry, the synthesis, SAR and pharmacokinetics of human gonadotropin-releasing hormone receptor nRH-R) antagonists are reported. GnRH-R is a G-protein-coupled receptor that stimulates secrction of gonadotropins GnRIH-R antagonists lower gonadal sex hormone levels and can be to treat discases such as endometriosis and prostate cancer. A major focus of the study presented in this paper the i was to optimize the drug-receptor binding while minimizing inhibition of ey trochrome Pase oxidase (CYP3A4). an enzyme responsible for metabolizing more than 50% of small molecule drugs markcted Compound 4a (NBI-42902) has been identified aspotent and orally active k antagonist. 4a wa receptor binding affinity but a reduced tendency to inhibit CYPBA4 Table I summarizes the 2 GnRH-R as used as a lead compound to dev elop kGnRl-R antagonists wi -GnRIH-R antagonists with similar amino-2pheny lethy luracils synthesized in this study Table 1. SAR of the Aeuso-2-phem lethyal . 47-12 x 0'a.ou ) Fje".. HF056 2s H CF-050 050 4b H 1.247 16- 0.44 36 H CF CHCH COOH 1b CHCH CHCOOH HC 090 1 11 )2 11 nt num ,Desen uned by competua for rtyr, DLeuwela/hs..NE. Moyeneda, roc ofa threshold ab des aribed in Expenics ental Procedures 'Not deerminesd bc
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