Ontology highlight
ABSTRACT:
SUBMITTER: Southers JA
PROVIDER: S-EPMC4007832 | biostudies-other | 2010 Aug
REPOSITORIES: biostudies-other
Southers James A JA Bauman Jonathan N JN Price David A DA Humphries Paul S PS Balan Gayatri G Sagal John F JF Maurer Tristan S TS Zhang Yan Y Oliver Robert R Herr Michael M Healy David R DR Li Mei M Kapinos Brendon B Fate Gwendolyn D GD Riccardi Keith A KA Paralkar Vishwas M VM Brown Thomas A TA Kalgutkar Amit S AS
ACS medicinal chemistry letters 20100513 5
As part of a strategy to deliver short-acting calcium-sensing receptor (CaSR) antagonists, the metabolically labile thiomethyl functionality was incorporated into the zwitterionic amino alcohol derivative 3 with the hope of increasing human clearance through oxidative metabolism, while delivering a pharmacologically inactive sulfoxide metabolite. The effort led to the identification of thioanisoles 22 and 23 as potent and orally active CaSR antagonists with a rapid onset of action and short phar ...[more]