title: Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
abstract: A series of benzoylpyrimidines derived from the anilinepyrimidine CRF(1) antagonists were synthesized. Several synthetic routes were developed to explore the SAR of this series of compounds. Compounds such as 8d (K(i) = 15 nM) exhibited high binding affinities at the human CRF(1) receptor.
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmacology, Neurocrine Bioscience, Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Webb
authors.forename: Terry
authors.initials: T
authors.lastname: Moran
authors.forename: Charles Q
authors.initials: CQ
authors.lastname: Huang
authors.forename: James R
authors.initials: JR
authors.lastname: McCarthy
authors.forename: Dimitri E
authors.initials: DE
authors.lastname: Grigoriadis
authors.forename: Chen
authors.initials: C
authors.lastname: Chen
mesh_terms: D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003001:Cloning, Molecular; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013816:Thermodynamics; D000099052:CRF Receptor, Type 1
chemical_list: D001565:Benzoates; D011743:Pyrimidines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1