Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents

2019 ◽  
Vol 171 ◽  
pp. 25-37 ◽  
Author(s):  
Eman M. Ahmed ◽  
Asmaa E. Kassab ◽  
Afaf A. El-Malah ◽  
Marwa S.A. Hassan
Keyword(s):  
Biological Evaluation ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: Multi-target compounds with dual antimicrobial and anti-inflammatory activities

2020 ◽  
Author(s):  
Ahmed Shaker ◽  
Eman K. A. Abdelall ◽  
Khaled R. A. Abdellatif ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Active Site ◽  
High Selectivity ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
E Coli ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Abstract Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA , E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii , respectively with safe therapeutic dose. Compounds 7a-k, 8a-c and 9a-c showed good anti-inflammatory activity with high selectivity toward COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site correlated with results of in vitro COX-2 inhibition assays.

scholarly journals Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: Multi-target compounds with dual antimicrobial and anti-inflammatory activities

2019 ◽  
Author(s):  
Ahmed Shaker ◽  
Eman K. A. Abdelall ◽  
Khaled R. A. Abdellatif ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Active Site ◽  
High Selectivity ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
E Coli ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Abstract Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA , E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii , respectively with safe therapeutic dose. Compounds 7a-k, 8a-c and 9a-c showed good anti-inflammatory activity with high selectivity toward COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site correlated with results of in vitro COX-2 inhibition assays.

scholarly journals Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: Multi-target compounds with dual antimicrobial and anti-inflammatory activities

2020 ◽  
Author(s):  
Ahmed Shaker ◽  
Eman K. A. Abdelall ◽  
Khaled R. A. Abdellatif ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Active Site ◽  
High Selectivity ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
E Coli ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Abstract Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA , E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii , respectively with safe therapeutic dose. Compounds 7a-k, 8a-c and 9a-c showed good anti-inflammatory activity with high selectivity toward COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site correlated with results of in vitro COX-2 inhibition assays.

Molecular hybrid design, synthesis and biological evaluation of N-phenyl sulfonamide linked N-acyl hydrazone derivatives functioning as COX-2 inhibitors: new anti-inflammatory, anti-oxidant and anti-bacterial agents

2017 ◽  
Vol 41 (22) ◽  
pp. 13516-13532 ◽  
Author(s):  
Vasubabu Gorantla ◽  
Rambabu Gundla ◽  
Surender Singh Jadav ◽  
Sreenivasa Reddy Anugu ◽  
Jithendra Chimakurthy ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Hybrid Design ◽  
Design Synthesis ◽  
Acyl Hydrazone ◽  
Anti Oxidant ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

The design, synthesis and biological evaluation of the anti-inflammatory activities of novel N-phenyl sulfonamide linked N-acylhydrazones (NPS–NAH) have been reported.

scholarly journals Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl)indole derivatives: Multi-target compounds with dual antimicrobial and anti-inflammatory activities

2020 ◽  
Author(s):  
Ahmed M. M. Shaker ◽  
Eman K. A. Abdelall ◽  
Khaled R. A. Abdellatif ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Active Site ◽  
High Selectivity ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
E Coli ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Abstract Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA , E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii , respectively with safe therapeutic dose. Compounds 7a-k, 8a-c and 9a-c showed good anti-inflammatory activity with high selectivity toward COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site correlated with results of in vitro COX-2 inhibition assays.

Selective COX-2 inhibitors. Part 2: Synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides

2008 ◽  
Vol 16 (5) ◽  
pp. 2697-2706 ◽  
Author(s):  
Shwu-Jiuan Lin ◽  
Wei-Jern Tsai ◽  
Wen-Fei Chiou ◽  
Tsang-Hsiung Yang ◽  
Li-Ming Yang
Keyword(s):  
Biological Evaluation ◽  
Cox 2 ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Design, synthesis, and biological evaluation of substituted 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles as selective COX-2 inhibitors

2006 ◽  
Vol 14 (8) ◽  
pp. 2507-2517 ◽  
Author(s):  
Latifeh Navidpour ◽  
Hamed Shafaroodi ◽  
Khosrou Abdi ◽  
Mohsen Amini ◽  
Mohammad H. Ghahremani ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Cox 2 ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation
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