Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:5.99.1.3 (topoisomerase)
 9,911 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The synthesis of novel series of structurally related 4-pyrazolyl benzenesulfonamide derivatives is described. All the newly synthesized compounds were examined for their anti-inflammatory activity using cotton pellet induced granuloma and carrageenan induced rat paw edema bioassays. In addition the inhibitory activities of cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2), ulcerogenic effect and acute toxicity were determined. Furthermore, all the compounds were evaluated for their in vitro antimicrobial activity against Eischerichia coli, Staphylococcus aureus and Candida albicans. Docking poses for compounds 6b and 7b separately in the active site of the human COX-2 enzyme and DNA-gyrase B were also obtained. The results revealed that compounds 3c, 4b, 4c, 5c, 6b and 7b exhibited comparable or better anti-inflammatory activity compared to indomethacin and celecoxib with no or minimal ulcerogenic effect and high safety margin. Compounds 3b, 3c, 4b, 4c, 5a-c, 6a, 6b and 7a-c displayed appreciable antibacterial activity against both E. coli and S. aureus compared with ampicillin. Compounds 5a-c and 7a had antibacterial activity against E. coli similar to ampicillin whereas compounds 3b, 3c, 4b, 4c, 6a and 7b displayed considerable activity against the microorganism. Compounds 3a, 3c, 4c, 5a-c, 6b and 7a-c had appreciable activity against S. aureus. Overall, compounds 4c, 6b and 7b are the most distinctive derivatives in the present study because of their remarkable anti-inflammatory potency and significant antibacterial activity. Furthermore, compounds 6b and 7b exhibited good selective inhibitory activity against COX-2 enzyme. Therefore, such compounds would represent a suitable template for the design of anti-inflammatory antimicrobial candidates with reasonable COX-2 selectivity.
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PMID:Synthesis and biological evaluation of novel pyrazole derivatives as anti-inflammatory antimicrobial agents. 1927 9

The synthesis of a novel series of 4-thiazolylpyrazolyl derivatives is described in the present report. All the newly synthesized compounds were examined for their anti-inflammatory activity using cotton pellet-induced granuloma and carrageenan-induced rat paw edema bioassays. Their inhibitory activities of cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2), ulcerogenic effect and acute toxicity were also determined. Furthermore, all compounds were evaluated for their in vitro antimicrobial activity against Escherichia coli, Staphylococcus aureus and Candida albicans. A docking pose for compounds 8b, 10a and 10b separately in the active site of the human COX-2 enzyme and DNA-gyrase B was also obtained. The results revealed that compounds 8b, 10a and 10b exhibited good anti-inflammatory activity with no or minimal ulcerogenic effect and good safety margin. Compounds 10a and 10b were found to be the most potent anti-inflammatory agents in the present study. Meanwhile, 10a and 10b displayed higher selective inhibitory activity towards COX-2 compared to indomethacin. Moreover, compounds 10a and 10b exhibited promising antibacterial against both E. coli and S. aureus. Docking studies for 8b, 10a and 10b with COX-2 (PDB ID: 1CX2) and DNA-gyrase B (PDB ID: 1EI1) showed good binding profile.
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PMID:Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. 2097 Feb 23