Biological evaluation and molecular docking. studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity
dc.authorid | TASKIN-TOK, Tugba/0000-0002-0064-8400 | |
dc.authorid | Tumer, Tugba/0000-0002-1740-4867 | |
dc.authorid | AY, Mehmet/0000-0002-1095-1614 | |
dc.authorid | Celik, Ayhan/0000-0003-1355-9252 | |
dc.authorid | Comert Onder, Ferah/0000-0002-4037-1979 | |
dc.authorid | Gungor, Tugba/0000-0001-5261-1856 | |
dc.contributor.author | Turner, Tugba B. | |
dc.contributor.author | Onder, Ferah Comert | |
dc.contributor.author | Ipek, Hande | |
dc.contributor.author | Gungor, Tugba | |
dc.contributor.author | Savranoglu, Seda | |
dc.contributor.author | Tok, Tugba Taskin | |
dc.contributor.author | Celik, Ayhan | |
dc.date.accessioned | 2025-01-27T20:49:46Z | |
dc.date.available | 2025-01-27T20:49:46Z | |
dc.date.issued | 2017 | |
dc.department | Çanakkale Onsekiz Mart Üniversitesi | |
dc.description.abstract | A series of nitro substituted benzamide derivatives were synthesized and evaluated for their potential anti-inflammatory activities in vitro. Firstly, all compounds (1-6) were screened for their inhibitory capacity on LPS induced nitric oxide (NO) production in RAW264.7 macrophages. Compounds 5 and 6 demonstrated significantly high inhibition capacities in a dose-dependent manner with IC50 values of 3.7 and 53 mu M, respectively. These two compounds were also accompanied by no cytotoxicity at the studied concentrations (max 50 mu M) in macrophages. Molecular docking analysis on iNOS revealed that compounds 5 and 6 bind to the enzyme more efficiently compared to other compounds due to having optimum number of nitro groups, orientations and polarizabilities. In addition, 5 and 6 demonstrated distinct regulatory mechanisms for the expression of the iNOS enzyme at the mRNA and protein levels. Specifically, both suppressed expressions of COX-2, IL-1 beta and TNF-alpha significantly, at 10 and 20 mu M. However, only compound 6 significantly and considerably decreased LPS-induced secretion of IL-1 beta and TNF-alpha. These results suggest that compound 6 may be a multi-potent promising lead compound for further optimization in structure and as well as for in vivo validation studies. (C) 2016 Published by Elsevier B.V. | |
dc.description.sponsorship | Scientific and Technological Research Council of Turkey in the scope of two different projects (TUBITAK) [110T754, 113Z706]; Canakkale Onsekiz Mart University, Scientific Research Project [FYL-2015-434] | |
dc.description.sponsorship | This work was partially supported by the Scientific and Technological Research Council of Turkey in the scope of two different projects (TUBITAK, Project numbers: 110T754 and 113Z706). Studies related with bioactivity part were partially supported by Canakkale Onsekiz Mart University, Scientific Research Project (FYL-2015-434). | |
dc.identifier.doi | 10.1016/j.intimp.2016.12.009 | |
dc.identifier.endpage | 139 | |
dc.identifier.issn | 1567-5769 | |
dc.identifier.issn | 1878-1705 | |
dc.identifier.pmid | 27988460 | |
dc.identifier.scopus | 2-s2.0-85006007454 | |
dc.identifier.scopusquality | Q1 | |
dc.identifier.startpage | 129 | |
dc.identifier.uri | https://doi.org/10.1016/j.intimp.2016.12.009 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12428/25308 | |
dc.identifier.volume | 43 | |
dc.identifier.wos | WOS:000393242800016 | |
dc.identifier.wosquality | Q2 | |
dc.indekslendigikaynak | Web of Science | |
dc.indekslendigikaynak | Scopus | |
dc.indekslendigikaynak | PubMed | |
dc.language.iso | en | |
dc.publisher | Elsevier | |
dc.relation.ispartof | International Immunopharmacology | |
dc.relation.publicationcategory | info:eu-repo/semantics/openAccess | |
dc.rights | info:eu-repo/semantics/closedAccess | |
dc.snmz | KA_WoS_20250125 | |
dc.subject | Nitro substituted benzamides | |
dc.subject | Anti-inflammatory | |
dc.subject | Nitric oxide | |
dc.subject | iNOS | |
dc.subject | Molecular docking | |
dc.title | Biological evaluation and molecular docking. studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity | |
dc.type | Article |