2074-67-1Relevant academic research and scientific papers
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.
Synthesis, reactivity and stereochemistry of new phosphorus heterocycles with 5- or 6-membered rings
Cristau, Henri-Jean,Pirat, Jean-Luc,Virieux, David,Monbrun, Jér?me,Ciptadi, Ciptadi,Bekro, Yves-Alain
, p. 2472 - 2481 (2007/10/03)
Syntheses of novel phosphorus heterocycles containing α-amino or α-hydroxyphosphonic or phosphinic acids motifs are developed. 2,3-dihydro-1,3-oxaphospholes (1) and 1,4,2-oxazaphosphinanes (2) exhibit a reactive part, respectively the enolether moiety and the P-H bond, which allows various structural modifications: (i) for 1a, by introduction of amino substituents, (ii) for 2a, by hydroxy- or aminoalkylation, by Michael addition or by P-arylation. These reactions present generally a good or even an excellent kinetic diastereoselectivity which can often be predicted by molecular models of the transition states.
Optimal conditions for preparing chloromethylphosphonic dichloride
Nazarov,Muslinkin
, p. 1043 - 1047 (2007/10/03)
A procedure was developed for preparing chloromethylphosphonic dichloride, involving available raw materials and common process equipment. The optimal operation conditions were determined. This procedure can be used for production of chloromethylphosphonic dichloride both in laboratory and under industrial conditions.
Inhibitors of retroviral proteases
-
, (2008/06/13)
The present invention relates to compounds of the formula I STR1 in which A, Q, R2, R3, R4 and the corresponding radicals with an * are defined as indicated in the description, a process for the preparation thereof, and th
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
A New Method for the Preparation of Bis(1-hydroxyalkyl)phosphinic Acid
Majewski, Piotr
, p. 555 - 557 (2007/10/02)
Bis(1-hydroxyalkyl)phosphinic acids 6 have been conveniently obtained by addition of bis(trimethylsiloxy)phosphine 1 to aldehydes or ketones 2 in the presence of chlorotrimethylsilane and triethylamine, followed by ethanolysis of the resulting trimethylsi
Bis(aminomethyl)phosphinic acid
-
, (2008/06/13)
Method for synthetizing bis(aminomethyl)phosphinic acid and its salts are disclosed. This acid corresponds to the formula STR1 and possesses plant-growth retarding activity.
