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Title of Journal: Arch Pharm Res

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Abbravation: Archives of Pharmacal Research

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Pharmaceutical Society of Korea

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DOI

10.1007/bf00319916

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1976-3786

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New antiinflammatory thiazolylcarbonylthiosemic

Authors: Brînduşa Tiperciuc Alina Pârvu Radu Tamaian Cristina Nastasă Ioana Ionuţ Ovidiu Oniga
Publish Date: 2013/03/16
Volume: 36, Issue: 6, Pages: 702-714
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Abstract

The objective of this study was to investigate the antiinflammatory and antioxidant activity of new thiazolylcarbonylthiosemicarbazides and thiazolylazole derivatives as potential iNOS inhibitors The in vivo antiinflammatory effects of the new thiazole compounds were studied in a turpentine oil induced inflammation model Their antiinflammatory activity was assessed by evaluating the acute phase bone marrow response phagocytes’ activity NO synthesis and antioxidant capacity The new thiazole compounds have antiinflammatory effects by lowering bone marrow acute phase response and oxidative stress The best antiinflammatory and antioxidant effect was found for thiazolylcarbonylthiosemicarbazides Th18 thiazolyl134oxadiazole Th20 and thiazolyl134thiadiazole Th21 Virtual screening of thiazole derivatives against the oxygenase domain of chain A from 2Y37 revealed that all twentytwo compounds bind the active site of inducible nitric oxide synthase iNOS Based on the virtual screening and on the results obtained above the activity may be due to their capacity to reduce the NO synthesis by blocking the bind of lArg in the active site of iNOS the compounds binding the synthase by hydrogen bonds between the NH 2 and/or 4 of thiosemicarbazide fragment Th28 or N2/N3 from azole cycles and by the thiol function Th922

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