Original
In vitro anti-leishmanial and anti-fungal effects of new SbIII carboxylates
1 Department of Chemistry, Kohat University of Science & Technology, Kohat 26000, Khyber Pakhtunkhwa, Pakistan
2 Department of Chemistry, The Islamia University of Bahawalpur, Bahawlpur, Punjab, Pakistan
3 Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan
4 Institute of Pharmaceutical Sciences, Kohat University of Science and Technology, Kohat 26000, Khyber Pakhtunkhwa, Pakistan
5 Department of Chemistry, Gomal University, Dera Ismail Khan, Khyber Pakhtunkhwa, Pakistan
Organic and Medicinal Chemistry Letters 2011, 1:2 doi:10.1186/2191-2858-1-2
Published: 18 July 2011Abstract
Ring opening of phthalic anhydride has been carried out in acetic acid with glycine, β-alanine, L-phenylalanine, and 4-aminobenzoic acid to yield, respectively, 2-{[(carboxymethyl)amino]carbonyl}benzoic acid (I), 2-{[(2-carboxyethyl)amino]carbonyl}benzoic acid (II), 2-{[(1-carboxy-2-phenylethyl)amino]carbonyl}benzoic acid (III), and 2-[(4-carboxyanilino)carbonyl]benzoic acid (IV). Compounds I-IV have been employed as ligands for Sb(III) center (complexes V-VIII) in aqueous medium. FTIR and 1H NMR spectra proved the deprotonation of carboxylic protons and coordination of imine group and thereby tridentate behaviour of the ligands as chelates. Elemental, MS, and TGA analytic data confirmed the structural hypothesis based on spectroscopic results. All the compounds have been assayed in vitro for anti-leishmanial and anti-fungal activities against five leishmanial strains L. major (JISH118), L. major (MHOM/PK/88/DESTO), L. tropica (K27), L. infantum (LEM3437), L. mex mex (LV4), and L. donovani (H43); and Aspergillus Flavus, Aspergillus Fumigants, Aspergillus Niger, and Fusarium Solani. Compound VII exhibited good anti-leishmanial as well as anti-fungal impacts comparable to reference drugs.
