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Bioorg Med Chem Lett. 2012 Oct 1;22(19):6205-11. doi: 10.1016/j.bmcl.2012.08.018. Epub 2012 Aug 14.

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.

Author information

1
AstraZeneca R&D Södertälje, S-151 85 Södertälje, Sweden.

Abstract

Benzothiazole amides were identified as TRPV1 antagonists from high throughput screening using recombinant human TRPV1 receptor and structure-activity relationships were explored to pinpoint key pharmacophore interactions. By increasing aqueous solubility, through the attachment of polar groups to the benzothiazole core, and enhancing metabolic stability, by blocking metabolic sites, the drug-like properties and pharmokinetic profiles of benzothiazole compounds were sufficiently optimized such that their therapeutic potential could be verified in rat pharmacological models of pain.

PMID:
22939234
DOI:
10.1016/j.bmcl.2012.08.018
[Indexed for MEDLINE]

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