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Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor |
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| Authors: | Winters Michael P Crysler Carl Subasinghe Nalin Ryan Declan Leong Lynette Zhao Shuyuan Donatelli Robert Yurkow Edward Mazzulla Marie Boczon Lisa Manthey Carl L Molloy Christopher Raymond Holly Murray Lynne McAlonan Laura Tomczuk Bruce |
| Affiliation: | Johnson & Johnson Pharmaceutical Research and Development, 665 Stockton Drive, Exton, PA 19341, USA. mwinter4@prdus.jnj.com |
| Abstract: | A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure-activity relationships are reported for these series. One potent orally bioavailable inhibitor had excellent PK properties and was active in a lung injury model in hyperoxia-exposed newborn rats. |
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