Discovery of 2-Phenyl-3-sulfonylphenyl-indole derivatives as a new class of selective COX-2 inhibitors

2003 ◽  
Vol 11 (24) ◽  
pp. 5539-5544 ◽  
Author(s):  
Wenhui Hu ◽  
Zongru Guo ◽  
Xiang Yi ◽  
Changbin Guo ◽  
Fengming Chu ◽  
...  
Keyword(s):  
Indole Derivatives ◽  
New Class ◽  
Cox 2 ◽  
Cox 2 Inhibitors

2, 3-Diaryl-5-ethylsulfanylmethyltetrahydrofurans as a new class of COX-2 inhibitors and cytotoxic agents

2008 ◽  
Vol 6 (15) ◽  
pp. 2706 ◽  
Author(s):  
Palwinder Singh ◽  
Anu Mittal ◽  
Satwinderjeet Kaur ◽  
Wolfgang Holzer ◽  
Subodh Kumar
Keyword(s):  
Cytotoxic Agents ◽  
New Class ◽  
Cox 2 ◽  
Cox 2 Inhibitors

COX-2 Inhibitors: A New Class of Antiangiogenic Agents

1999 ◽  
Vol 889 (1 CANCER PREVEN) ◽  
pp. 84-86 ◽  
Author(s):  
JAIME L. MASFERRER ◽  
ALANE KOKI ◽  
KAREN SEIBERT
Keyword(s):  
Antiangiogenic Agents ◽  
New Class ◽  
Cox 2 ◽  
Cox 2 Inhibitors

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.

A New Class of Acyclic 2-Alkyl-1,2-diaryl (E)-Olefins as Selective Cyclooxygenase-2 (COX-2) Inhibitors.

ChemInform ◽  
2005 ◽  
Vol 36 (1) ◽  
Author(s):  
Md. Jashim Uddin ◽  
P. N. Praveen Rao ◽  
Md. Abdur Rahim ◽  
Robert McDonald ◽  
Edward E. Knaus
Keyword(s):  
Cyclooxygenase 2 ◽  
New Class ◽  
Cox 2 ◽  
Cox 2 Inhibitors

Design of acyclic triaryl olefins: a new class of potent and selective cyclooxygenase-2 (COX-2) inhibitors

2004 ◽  
Vol 14 (8) ◽  
pp. 1953-1956 ◽  
Author(s):  
Md.Jashim Uddin ◽  
P. N. Praveen Rao ◽  
Edward E Knaus
Keyword(s):  
Cyclooxygenase 2 ◽  
New Class ◽  
Cox 2 ◽  
Cox 2 Inhibitors
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