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Novel N-methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced cardio vascular risks.
- Source :
- Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2023, Vol. 38 Issue 1, p246-266, 21p
- Publication Year :
- 2023
-
Abstract
- Three novel series of N-methylsulfonylindole derivatives 3a&b, 4a–e, and 5a–e were synthesised. Different biological activities of the synthesised compounds were studied. Antimicrobial activity showed that, compounds 4b, 4e and 5d had selective antibacterial activity against the Gram-negative bacteria, Salmonella enterica and/or E. coli. The anti-oxidant activity of the synthesised compounds was evaluated by DPPH radical scavenging activity. In vitro anti-inflammatory activity was estimated. Compounds 4d, 4e, 5b, and 5d showed the highest anti-inflammatory activity. The COX-1, COX-2 and 5-LOX inhibitory activities were measured using enzyme immune assay (EIA) kits. Due to the dual COX-2/5-LOX inhibitory activity of compound 5d, its cardiovascular profile was determined by measuring cardiac biomarkers (LDH, CK-MB, and Tn-I). Besides, the histopathological study of the heart muscle and stomach were examined for the most active COX-2 inhibitors 4e and 5d. Finally, a molecular modelling study and pharmacokinetic properties were obtained using different computational methods. [ABSTRACT FROM AUTHOR]
- Subjects :
- CHEMICAL synthesis
ESCHERICHIA coli
MYOCARDIUM
ANTIOXIDANTS
GRAM-negative bacteria
Subjects
Details
- Language :
- English
- ISSN :
- 14756366
- Volume :
- 38
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Journal of Enzyme Inhibition & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 174161072
- Full Text :
- https://doi.org/10.1080/14756366.2022.2145283