In vitro anti-leishmanial activities and structure-activity relationship analysis of new antimony(III) complexes
    
Yazarlar (3)
Doç. Dr. Turgay TUNÇ Kırşehir Ahi Evran Üniversitesi, Türkiye
Hatice Ertabaklar
Aydın Adnan Menderes Üniversitesi, Türkiye
Nurcan Karacan
Gazi Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı INDIAN JOURNAL OF CHEMISTRY SECTION A-INORGANIC BIO-INORGANIC PHYSICAL THEORETICAL & ANALYTICAL CHEMISTRY
Dergi ISSN 0376-4710 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 11-2020
Cilt / Sayı / Sayfa 59 / 11 / 1609–1617 DOI 10.56042/ijca.v59i11.27269
Makale Linki http://op.niscair.res.in/index.php/IJCA/article/view/27269/465478273
Özet
New fourteen antimony(III) complexes of general formula [SbLnCl3] (where n= 1 or 2, L =2-aminopyridine, 5-methyl-2-aminopyridine, 2-aminopyrimidine, 4,6-dimethoxy-2-aminopyrimidine, 2-benzyl-2-thiopseudeourea,2-guanidinobenzimidazole, 2-amino-5-thiol-4,6-dimethoxypyrimidine, 2-amino-5-(1H-tetrazol-5-ylthio)-4,6-dimethoxypyrimidine, N-2-pyrimidine, 2-piperidinecarboxamide, N-2-pyrimidine, 2-pyrrolidinecarboxamide, 2-amino-5-(1H-tetrazol-5-iltiyo)-4,6-dimethoxypyrimidine-2-pyrrolidinecarboxamide and N-2-pyrimidine, 5-chloro-2-thiophenecarboxamide, N-2-benzothiazol-2-pyrrolidinecarboxaamide, N,N-(1,2-phenyl)dipyrrolidine-2-carboxamide) have been synthesized and their anti-leishmanial activity have been assessed in vitro against Leishmania tropica promastigotes. The best complex, Sb(2-guanidinobenzimidazole)Cl-3 is demostrated 3.16% growth inhibition at a concentration of 31.25 mu g/mL. In general, antimony(III) complexes containing pyrimidine ligands has showed higher anti-leishmanial activity than antimony(III) complexes bearing pyridine ligands, and electron-donating substituents decrease the anti-leishmanial activity. All complexes have been optimised with DFT/B3LYP/LANL2DZ method in the gas phase. Several descriptors are tested to fmd a quantitative correlation between anti-leishmanial activity and structural properties of the complexes by best multiple linear regression method. Good correlations are obtained with minimum net atomic charge for a C atom and maximum bond order of a Cl atom. The developed QSAR equation is internally validated.
Anahtar Kelimeler
Antimony(III) complexes | Anti-leishmanial activity | Structure-activity relationship