Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents

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.

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

10.21203/rs.2.17036/v1 ◽

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.

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

10.21203/rs.2.17036/v2 ◽

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.

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Synthesis and Biological Evaluation of Some Novel Thieno[2,3-d] pyrimidine Derivatives as Potential Anti-inflammatory and Analgesic Agents

Medicinal Chemistry ◽

10.2174/1573406411309080012 ◽

2013 ◽

Vol 9 (8) ◽

pp. 1099-1112 ◽

Cited By ~ 4

Author(s):

Alaa El-Tombary ◽

Soad El-Hawash ◽

Nargues Habib ◽

Raafat Soliman ◽

Ibrahim El-Ashmawy ◽

...

Keyword(s):

Biological Evaluation ◽

Pyrimidine Derivatives ◽

Analgesic Agents ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of thieno [2′,3′:4,5]pyrimido[1,2-b][1,2,4]triazines and thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidines as anti-inflammatory and analgesic agents

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2012.12.003 ◽

2013 ◽

Vol 62 ◽

pp. 341-351 ◽

Cited By ~ 78

Author(s):

Hayam M. Ashour ◽

Omaima G. Shaaban ◽

Ola H. Rizk ◽

Ibrahim M. El-Ashmawy

Keyword(s):

Biological Evaluation ◽

Analgesic Agents ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

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

10.21203/rs.2.17036/v4 ◽

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.

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