107148-17-4Relevant academic research and scientific papers
Design, synthesis, and evaluation of novel organophosphorus inhibitors of bacterial ureases
Vassiliou, Stamatia,Grabowiecka, Agnieszka,Kosikowska, Paulina,Yiotakis, Athanasios,Kafarski, Pawe?,Berlicki, Lukasz
supporting information; experimental part, p. 5736 - 5744 (2009/08/16)
A new group of organophosphorus inhibitors of urease, P-methyl phosphinic acids was discovered by using the structure based inhibitor design approach. Several derivatives of the lead compound, aminomethyl(P-methyl)phosphinic acid, were synthesized successfully. Their potency was evaluated in vitro against urease from Bacillus pasteurii and Proteus vulgaris. The studied compounds constitute a group of competitive, reversible inhibitors of bacterial ureases. Obtained thiophosphinic analogues of the most effective structures exhibited kinetic characteristics of potent, slow binding urease inhibitors, with K i = 170 nM (against B. pasteurii enzyme) for the most active N-(N′-benzyloxycarbonylglycyl)aminomethyl(P-methyl)phosphinothioic acid.
Design and synthesis of phosphinic acids that triply inhibit endothelin converting enzyme, angiotensin converting enzyme and neutral endopeptidase 24.11
McKittrick, Brian A.,Stamford, Andrew W.,Weng, Xiaoyu,Ma, Ke,Chackalamannil, Samuel,Czarniecki, Michael,Cleven, Renee M.,Fawzi, Ahmad B.
, p. 1629 - 1634 (2007/10/03)
We have synthesized a series of phosphinic acids as inhibitors of the metalloprotease endothelin converting enzyme (ECE). Potent ECE inhibitors 4g and 4o were identified. These compounds are members of a novel class of ECE inhibitors that are also potent inhibitors of angiotensin converting enzyme and neutral endopeptidase.
