Effect of derivatization of sulfamethoxazole and trimethoprim with copper and zinc on their medicinal value

Abstract

Cu(II) and Zn(II) complexes of Schiff bases obtained by condensation of sulfamethoxazole with salicylaldehyde/pyridoxal were prepared and characterized by microanalytical, thermogravimetric, magnetic, and spectroscopic data. The Cu (II) and Zn (II) complexes of salicylidenesulfamethoxazole were found to be five coordinate while all others were six coordinate. The electron paramagnetic resonance spectral lines exhibited rhombic distortion from axial symmetry, with g k [ g \ [ g e , in the case of the Cu (II) complexes. The geometry of the complexes appears to be square-pyramidal or octahedral. All the compounds under investigation possess antibacterial activity against the strains tested. The antibacterial activity showed the following trend: Cu (II) complexes [ Zn (II) complexes [ Schiff base ligands [ parent drugs. All the copper complexes were found to be active against kaolin paw edema whereas the parent drugs were inactive.

Structural characterization of new Schiff bases of sulfamethoxazole and sulfathiazole, their antibacterial activity and docking computation with DHPS protein structure

“…Severe side effects of sulfonamides and induction of resistance have prompted worldwide effort to find new generation drugs [13]. To improve drug activity and reduce toxicity the researchers have already engaged in the design, synthesis and to explore the drug-protein interaction of functionalized sulfonamides and their complexes [14][15][16][17].…”

Structures, antimicrobial activity, DNA interaction and molecular docking studies of sulfamethoxazolyl-azo-acetylacetone and its nickel(II) complex

“…The hypersensitivity is assumed to be the result of oxidative metabolites of SMX such as SMX-hydroxylamine (SMX-NHOH) and SMX-nitroso (SMX-NO) [15]. In order to overcome these difficulties and to improve drug activity, functionalized sulfonamides and their metal complexes [16,17] are in clinical trials. Azo dyes of sulfa drugs are well known for their antiseptic activity [18].…”

Synthesis, Characterization and Biological Evaluation of Schiff Base (N-4-(thiophene-2-yl-methyleneamino)-2,6-dimethylpyrimidine-4-yl)benzenesulfonamide and its Complexes with Cu(II), Ni(II), Co(II), Fe(II), Mn(II), Zn(II) Ions

“…Many drugs have improved pharmacological properties when forms Schiff base metal complexes. The Schiff base metal chelates have gained attention in fields like medicine and pharmaceutical because of wide spectrum of biological activities such as anti-inflammatory drugs, antimicrobial, antifungal, antispasmodic, tuberculosis, anticancer, anthelmintic, antioxidant and so forth [3][4][5][6][7][8][9][10].…”