التفاصيل البيبلوغرافية
العنوان:
Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux
المؤلفون:
Samer Chmait , Adrie D. Jones , Amy Porter , Kristin L. Andrews , Xiaoning Zhao , Jennifer R. Allen , Shannon Rumfelt , Wenge Zhong , Essa Hu , James R. Falsey , Robert M. Rzasa , Steven W. Louie , James J. S. Treanor , Ning Chen
المصدر:
Bioorganic & Medicinal Chemistry Letters . 22:7371-7375
بيانات النشر:
Elsevier BV, 2012.
سنة النشر:
2012
مصطلحات موضوعية:
Models, Molecular , Phosphodiesterase Inhibitors , Stereochemistry , Clinical Biochemistry , Pharmaceutical Science , Crystallography, X-Ray , Biochemistry , Structure-Activity Relationship , Drug Discovery , Humans , Potency , Structure–activity relationship , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Molecular Biology , P-glycoprotein , chemistry.chemical_classification , Dose-Response Relationship, Drug , Molecular Structure , biology , Phosphoric Diester Hydrolases , Drug discovery , Organic Chemistry , Phosphodiesterase , Enzyme , chemistry , biology.protein , Molecular Medicine , PDE10A , Efflux , Ethers
الوصف:
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies revealed two novel binding modes to the catalytic site of the PDE10A enzyme.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c902b8d3ff73465c5b07e532310cd1d https://doi.org/10.1016/j.bmcl.2012.10.078
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....6c902b8d3ff73465c5b07e532310cd1d
قاعدة البيانات:
OpenAIRE
