Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5265469 | Tetrahedron Letters | 2012 | 7 Pages |
Abstract
AgNO3 facilitated the intramolecular ring closure of o-(1-alkynyl)benzenesulfonamides via a regioselective C-N bond forming reaction leading to the formation of 3-substituted benzothiazine derivatives. A number of compounds were prepared in good yields by using this inexpensive and safe methodology. All the compounds synthesized were evaluated for their cyclooxygenase (COX) inhibiting properties in vitro. A number of compounds that do not contain an enolic hydroxyl group showed selectivities toward COX-2 over COX-1 inhibition. This was further supported by the predictive binding mode of two compounds with COX-1 and -2 proteins through molecular docking studies.
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Authors
D. Rambabu, P.V.N.S. Murthy, K.R.S. Prasad, Ajit Kandale, Girdhar Singh Deora, M.V. Basaveswara Rao, Manojit Pal,