2. Academic Validation
  3. Discovery and structure-activity relationships of a novel series of benzopyran-based K(ATP) openers for urge urinary incontinence

Discovery and structure-activity relationships of a novel series of benzopyran-based K(ATP) openers for urge urinary incontinence

  • Bioorg Med Chem. 2009 Jan 15;17(2):855-66. doi: 10.1016/j.bmc.2008.11.055.
Xuqing Zhang 1,  Yuhong Qiu,  Xiaojie Li,  Sheela Bhattacharjee,  Morgan Woods,  Patricia Kraft,  Scott G Lundeen,  Zhihua Sui
Affiliations

Affiliation

  • 1 Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, LLC, 665 Stockton Drive, Exton, PA 19341, USA. xzhang5@prdus.jnj.com
PMID: 19101153 DOI: 10.1016/j.bmc.2008.11.055
Abstract

A novel series of benzopyran derivatives were synthesized and evaluated as K(ATP) channel openers. Structure-activity relationships were investigated around 4-position of the benzopyran nucleus. Optimization of 4-substituent with some heterocyclic rings led to compound 13b bearing a benzo[d]isoxazol-3-one moiety as a potent and selective K(ATP) channel opener in vitro. In two anesthetized rat models of myogenic bladder overactivity, compound 13b was found to inhibit spontaneous bladder contractions.

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