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Updated: May 19, 2026

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Published on: December 31, 2013
Potent and orally efficacious benzothiazole amides as TRPV1 antagonists
Yevgeni Besidski1, William Brown, Johan Bylund
1AstraZeneca 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.
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