%0 Journal Article
%T Sparfloxacin-Metal Complexes as Urease Inhibitors: Their Synthesis, Characterization, Antimicrobial, and Antienzymatic Evaluation
%A Somia Gul
%A Najma Sultana
%A M. Saeed Arayne
%A Sana Shamim
%A Mahwish Akhtar
%A Ajmal Khan
%J Journal of Chemistry
%D 2013
%I Hindawi Publishing Corporation
%R 10.1155/2013/306385
%X Four new metal complexes (S12¨CS15) of SPFX (third-generation quinolones) via heavy metals have been synthesized in good yield and characterized by physicochemical and spectroscopic methods including TLC, IR, NMR, and elemental analyses. Sparfloxacinato ligand binds with metals through pyridone and oxygen atom of carboxylic group. The biological actives of complexes have been tested against four Gram-positive and seven Gram-negative bacteria and six different fungi. Statistical analysis of antimicrobial data was done by one-way ANOVA, Dunnett¡¯s test; it was observed that S13, S14, and S15 were found to be most active complexes. Antifungal data confirm that all four synthesized complexes are most active and show significant activity against F. solani with respect to parent drug and none of complexes show activity against A. parasiticus, A. effuris, and S. cervicis. To study inhibitory effects of newly formed complexes, enzyme inhibition studies have been conducted against urease, ¦Á-chymotrypsin, and carbonic anhydrase. Enzymatic activity results of these complexes indicated them to be good inhibitors of urease enzyme while all complexes show mild activities against carbonic anhydrase enzyme. Further research may prove the promising role of these synthesized complexes as urease inhibitors. 1. Introduction For infectious diseases, multiple therapies are usually required and so the possibility of drug-drug interactions increased. Careful consideration of concomitant drug therapy is needed. Literature survey reveals that fluoroquinolones showed several important interactions with many drugs [1]. Usually fluoroquinolones are prescribed for many diseases including respiratory and urinary tract infections. Sparfloxacin (SPFX) is an orally active synthetically broadspectrum third-generation quinolones use for upper respiratory tract infection. Metals are considered essential to a human body in performing physiologically important and vital functions, in the body [2]. The action of many drugs is dependent on coordination with metal ions or/and the inhibition on the formation of metalloenzymes [3]. The proposed mechanism of the interaction is chelation between the 4-oxo and adjacent carboxyl group of quinolone and metal cations [4¨C8]. Literature survey reveals that concurrent administration of magnesium and aluminium containing antacid with ciprofloxacin resulted in a nearly complete loss of activity of the drug [9] and patients who orally administrated fluoroquinolones should avoid mixtures containing multivalent cations, because quinolones binds with these metals
%U http://www.hindawi.com/journals/jchem/2013/306385/