4886-44-6Relevant articles and documents
Computer-aided optimization of phosphinic inhibitors of bacterial ureases
Vassiliou, Stamatia,Kosikowska, Paulina,Grabowiecka, Agnieszka,Yiotakis, Athanasios,Kafarski, Pawe,Berlicki, Lukasz
experimental part, p. 5597 - 5606 (2010/10/20)
Urease inhibitors can be considered as a tool to control the damaging effect of ureolytic bacteria infections in humans which occur commonly in the developed countries. Computer-aided optimization of the aminomethylphosphinate structures by modifying both their N- and P-termini led to the invention of a novel group of inhibitors of bacterial ureases. Introduction of P-hydroxymethyl group into the molecule resulted in considerable increase of the inhibitory activity against enzymes purified from Bacillus pasteurii and Proteus vulgaris as compared with their P-methyl counterparts described previously. The designed compounds represent a competitive reversible class of urease inhibitors. The most potent, N-methyl-aminomethyl-P-hydroxymethylphosphinic acid, displayed Ki = 360 nM against P. vulgaris enzyme.
Organophosphorus osteotropic cyclopodands.
Mollier, H.,Vincens, M.,Vidal, M.,Pasqualini, R.,Duet, M.
, p. 787 - 795 (2007/10/02)
Various phosphorus containing ligands (including phosphonic acids, phosphinic acids and phosphine oxide derivatives) have been synthesized and complexed to technetium.The species derived from benzene-1,2,4,5-tetra(methylenephosphonic) acid (BTMP) and 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetra-(methylenephosphonic) acid (TTMP) which are osteotropic vectors have demonstrated excellent tracing properties on animal tests.These tracers however were less effective upon human tests.The differences in their respective biological activities led us to investigate their physicochemical properties in solution. Key Words: organophosphorus cyclopodands / phosphonic acid / technetium / complexes / osteotropic tracers
