RESUMO
The present work describe the synthesis of a novel series of celecoxib derivatives (6a-m) and they were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, IV and IX which are involved in a variety of diseases such as glaucoma, retinitis pigmentosa, epilepsy and tumors etc. These compounds showed interesting inhibitory activity for these isoforms, with several low nanomolar derivatives identified against all these enzymes. The in-vivo anti-inflammatory activity of the synthesized compounds were evaluated using Celecoxib as reference standard by paw Oedema model on albino Wistar. Most of the compounds showed higher in-vivo anti-inflammatory activity compared to Celecoxib.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Inibidores da Anidrase Carbônica/farmacologia , Anidrases Carbônicas/metabolismo , Edema/tratamento farmacológico , Pirazóis/farmacologia , Sulfonamidas/farmacologia , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Inibidores da Anidrase Carbônica/síntese química , Inibidores da Anidrase Carbônica/química , Relação Dose-Resposta a Droga , Humanos , Isoenzimas/antagonistas & inibidores , Isoenzimas/metabolismo , Masculino , Estrutura Molecular , Pirazóis/síntese química , Pirazóis/química , Ratos , Ratos Sprague-Dawley , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química , BenzenossulfonamidasRESUMO
The title compound, C(9)H(9)ClN(2)O(5)S, is of inter-est as a precursor to biologically active substituted quinolines and related compounds. The structure displays inter-molecular C-Hâ¯O inter-actions. Each mol-ecule is linked to two adjacent neighbours via weak centrosymmetric dimer-forming inter-actions, forming chains in the [101] direction.
RESUMO
The title compound, C(7)H(7)ClN(2)O(4)S, is of inter-est as a precursor to biologically active substituted quinolines. Its structure resembles those of the previously reported N-phenyl-methane sulfonamide and its 4-nitro, 4-fluoro and 4-bromo derivatives, with slightly different geometric parameters. An intra-molecular N-Hâ¯O hydrogen bond gives rise to a six-membered ring. Inter-molecular C-Hâ¯O contacts stabilize the crystal packing.
RESUMO
In the mol-ecule of the title compound, C(10)H(9)N(3)O(2), the pyrazole ring is approximately coplanar with the amino and carboxyl groups. The phenyl group is twisted by 48.13â (3)° relative to this plane. An intra-molecular N-Hâ¯O hydrogen bond stabilizes the planar conformation of the mol-ecule. The mol-ecules are linked into two-dimensional sheets by two strong inter-molecular N-Hâ¯N and O-Hâ¯O hydrogen bonds. The latter forms the classic carboxylic acid dimer motif.