874819-71-3Relevant articles and documents
Design, synthesis, and biological evaluation of phosphoramide derivatives as urease inhibitors
Dominguez, Maria J.,Sanmartin, Carmen,Font, Maria,Palop, Juan A.,San Francisco, Sara,Urrutia, Oscar,Houdusse, Fabrice,Garcia-Mina, Jose M.
experimental part, p. 3721 - 3731 (2010/03/05)
The design, synthesis, and biological evaluation of phosphoramide derivatives as urease inhibitors to reduce the loss of ammonia has been carried out. Forty phosphorus derivatives were synthesized and their inhibitory activities evaluated against that of jack bean urease. In addition, in vivo assays have been carried out. All of the compounds were characterized by IR, 1H NMR, MS, and elemental microanalysis. In some cases, detailed molecular modeling studies were carried out, and these highlighted the interaction between the enzyme active center and the compounds and also the characteristics related to their activity as urease inhibitors. According to the IC50 values for in vitro inhibitory activity, 12 compounds showed values below 1 μM and 8 of them represent improvements of activity in comparison to the commercial urease inhibitor N-n-butylthiophosphorictriamide (NBPT) (100 nM) (AGROTAIN). On the basis of the activity results and the conclusions of the molecular modeling study, a structural model for new potential inhibitors has been defined.
N-PHENYLPHOSPHORIC ACID TRIAMIDES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS AGENTS FOR REGULATING OR INHIBITING ENZYMATIC UREA HYDROLYSIS
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Page/Page column 16, (2008/06/13)
The invention relates to N-phenylphosphonic acid triamides of general formula (I), to a method for the production thereof and to their use as agents for regulating or inhibiting enzymatic urea hydrolysis. In formula (I), X represents oxygen or sulfur; Rs