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Pal, M. et al.

Pal, Madan, Padakanti, Pattabiraman, Kalleda, Vanguri, Mullangi, Mamidi, Casturi, Malde, Gopalakrishnan, Yeleswarapu,

Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.

A series of 1,5-diarylpyrazoles having a substituted benzenesulfonamide moiety as pharmacophore was synthesized and evaluated for cyclooxygenase ( COX-1/ COX-2) inhibitory activities. Through SAR and molecular modeling, it was found that fluorine substitution on the benzenesulfonamide moiety along with an electron-donating group at the 4-position of the 5-aryl ring yielded selectivity as well as potency for COX-2 inhibition in vitro. Among such compounds 3-fluoro-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide 3 displayed interesting pharmacokinetic properties along with antiinflammatory activity in vivo. Among the sodium salts tested in vivo, 10, the propionyl analogue of 3, showed excellent antiinflammatory activity and therefore represents a new lead structure for the development of injectable COX-2 specific inhibitors.[1]

References

Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. Pal, M., Madan, M., Padakanti, S., Pattabiraman, V.R., Kalleda, S., Vanguri, A., Mullangi, R., Mamidi, N.V., Casturi, S.R., Malde, A., Gopalakrishnan, B., Yeleswarapu, K.R. J. Med. Chem. (2003) [Pubmed]

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