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The design and synthesis of BMS-248360 yielded a potent and orally active dual antagonist of both AT1 and ETA receptors, representing a new approach to treating hypertension.
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The discovery of BMS-248360 provides a novel dual AT(1) and ET(A) receptor antagonist as a potential new approach to treating hypertension.
The ET(A) receptor antagonist (2) (N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)-[1,1'-biphenyl]-2-sulfonamide, BMS-193884) shares the same biphenyl core as a large number of AT(1) receptor antagonists, including irbesartan (3). Thus, it was hypothesized that merging the structural elements of 2 with those of the biphenyl AT(1) antagonists (e.g., irbesartan) would yield a compound with dual activity for both receptors. This strategy led to the design, synthesis, and discovery of (15) (4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(3,4-dimethyl-5-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-[1,1'-biphenyl]-2-sulfonamide, BMS-248360) as a potent and orally active dual antagonist of both AT(1) and ET(A) receptors. Compound 15 represents a new approach to treating hypertension.
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Murugesan et al. (2002) studied Hypertension. BMS-248360 (Compound 15) was evaluated. The design and synthesis of BMS-248360 yielded a potent and orally active dual antagonist of both AT1 and ETA receptors, representing a new approach to treating hypertension.
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