Carboxyl-promoted enhancement of selectivity for the β3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces β3 binding selectivity

DOI: 10.1016/S0960-894X(97)00266-7

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1583 - 1588 (1997)

Update date:2022-08-04

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Authors:

Sher, Philip M.

Mathur, Arvind

Fisher, Liesl G.

Wu, Gang

Skwish, Stephen

Michel, Inge M.

Seiler, Steven M.

Dickinson, Kenneth E. J.

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Article abstract of DOI:10.1016/S0960-894X(97)00266-7

Carboxyl and other negatively charged groups were found to be most effective at producing human β₃ adrenergic receptor binding selectivity in 1 (BRL 37344) and related compounds. The sulfonic acid analog 7 (EMS-187413) is a novel and potent β₃ adrenergic agonist that binds selectively, and thus has an in vitro profile that compares favorably with that of BRL 37344.

Full text of DOI:10.1016/S0960-894X(97)00266-7

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