Pharmacophoric 2-hydroxyalkyl benzenesulfonamide: a single-step synthesis from benzenesulfonamide via hemiaminal.
作者信息
Singh Sunil K, Shivaramakrishna S, Saibaba V, Rao K Srinivas, Ganesh K Ravi, Vasudev R, Kumar P Praveen, Babu J Moses, Vyas K, Rao Y Koteswar, Iqbal J
机构信息
Discovery Chemistry, Discovery Research, Dr. Reddy's Laboratories Ltd., Bollaram Road, Miyapur, Hyderabad 500 049, India.
出版信息
Eur J Med Chem. 2007 Apr;42(4):456-62. doi: 10.1016/j.ejmech.2006.09.021. Epub 2006 Nov 13.
ortho-Acylation attempt of benzenesulfonamide afforded the corresponding hemiaminal as major product. The in situ reduction of the reaction mixture, reported herein, directly provided 2-hydroxyalkyl benzenesulfonamide, an important pharmacophoric element for designing drug-like scaffolds. Its application is demonstrated through designing a novel series of 1,5-diarylpyrazoles for cyclooxygenase-2 (COX-2) inhibition.
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