AI Article Synopsis
- Researchers conducted detailed studies on the structure-activity and structure-kinetic relationships of CRTh2 antagonists, focusing on bicyclic heteroaromatic compounds.
- Their findings identified several effective molecules that showed strong binding, high cellular potency, and prolonged receptor residence times.
- A minor modification in the bicyclic structure significantly increased the dissociation half-lives, and the best compounds exhibited favorable pharmacokinetic properties.
Article Abstract
Extensive structure-activity relationship (SAR) and structure-kinetic relationship (SKR) studies in the bicyclic heteroaromatic series of CRTh2 antagonists led to the identification of several molecules that possessed both excellent binding and cellular potencies along with long receptor residence times. A small substituent in the bicyclic core provided an order of magnitude jump in dissociation half-lives. Selected optimized compounds demonstrated suitable pharmacokinetic profiles.
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| http://dx.doi.org/10.1016/j.bmcl.2014.08.029 | DOI Listing |
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