Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

J P Beck; M A Curry; R J Chorvat; L W Fitzgerald; P J Gilligan; R Zaczek; G L Trainor

doi:10.1016/s0960-894x(99)00159-6

Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

Bioorg Med Chem Lett. 1999 Apr 19;9(8):1185-8. doi: 10.1016/s0960-894x(99)00159-6.

Authors

J P Beck¹, M A Curry, R J Chorvat, L W Fitzgerald, P J Gilligan, R Zaczek, G L Trainor

Affiliation

¹ DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Wilmington, DE 19880-0500, USA.

PMID: 10328310
DOI: 10.1016/s0960-894x(99)00159-6

Abstract

A series of thiazolo[4,5-d]pyrimidine thiones and -ones was prepared and discovered to have good binding affinity to the CRH-R1 receptor, thus showing promise as a new class of potential anxiolytics and/or antidepressants.

MeSH terms

Cell Line
Humans
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacokinetics*
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship
Thiones / chemical synthesis*
Thiones / pharmacokinetics*

Substances

Pyrimidines
Receptors, Corticotropin-Releasing Hormone
Thiones