200941-05-5Relevant academic research and scientific papers
Probing for a hydrophobic a binding register in prostate-specific membrane antigen with phenylalkylphosphonamidates
Maung, Jack,Mallari, Jeremy P.,Girtsman, Teri A.,Wu, Lisa Y.,Rowley, Jennifer A.,Santiago, Nicholas M.,Brunelle, Alan N.,Berkman, Clifford E.
, p. 4969 - 4979 (2007/10/03)
A series of phenylalkylphosphonamidate derivatives of glutamic acid were synthesized and evaluated for their inhibitory potencies against PSMA. The greatest inhibitory potency was observed for the inhibitors 1f (n = 5) and 1g (n = 6) suggesting the presen
Evaluation of phosphorus-containing inhibitors of γ-glutamyl hydrolase
Rodriguez, Chester E.,Holmes, H. Michael,Mlodnosky, Karyn L.,Lam, Vinh Q.,Berkman, Clifford E.
, p. 1521 - 1524 (2007/10/03)
Several putative, phosphorus-containing inhibitors of γ-glutamyl hydrolase were synthesized and evaluated for inhibitory activity. The phosphonamidoic acids were shown to be weak competitive inhibitors while both a phosphoramidate diester and a phosphonamidate ester were shown to be potent time-dependent inactivators, presumably through irreversible phosphorylation of an active site nucleophile.
A convenient two-step one-pot synthesis of phosphonamidates
Mlodnosky, Karyn L.,Holmes, H. Michael,Lam, Vinh Q.,Berkman, Clifford E.
, p. 8803 - 8806 (2007/10/03)
Phosphonamidates are formed in high yield from a one-pot sequential reaction of a phosphonyl dichloride with an alcohol and then an amine in the presence of catalytic 1H-tetrazole. Undesired disubstitution of the phoshphonyl dichloride by the alcohol or the amine is minimal due to the presence of tetrazole.
