N-acylated sulfonamide sodium salt: a prodrug of choice for the bifunctional 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamide class of COX-2 inhibitors |
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| Authors: | Singh Sunil Kumar Vobbalareddy Saibaba Kalleda Srinivasa Rao Casturi Seshagiri Rao Mullangi Ramesh Ramanujam Rajagopalan Yeleswarapu Koteswar Rao Iqbal Javed |
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| Affiliation: | Discovery Chemistry, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500 049, India. sunilkumarsingh@drreddys.com |
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| Abstract: | Synthesis and biological evaluation of possible prodrugs of COX-2 inhibitors involving sulfonamide and hydroxymethyl groups of 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamides are described. Out of many options, the sodium salt of N-propionyl sulfonamide demonstrated much improved pharmacological profiles and physicochemical properties suitable for oral as well as parenteral administration. |
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