The design and synthesis of a novel series of indole derived selective ET(A) antagonists. |
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| Authors: | David J Rawson Kevin N Dack Roger P Dickinson Kim James |
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| Affiliation: | Department of Discovery Chemistry, Pfizer Central Research, Sandwich, Kent CT13 9NJ, UK. david_rawson@sandwich.pfizer.com |
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| Abstract: | Conformational constraint has been used as the key design element in the identification of a series of potent and selective ET(A) antagonists. The most potent antagonist, 32, (ET(A) IC(50)=0.55nM) is 722-fold selective over the ET(B) receptor, as measured by binding experiments. |
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