- Probing for a hydrophobic a binding register in prostate-specific membrane antigen with phenylalkylphosphonamidates
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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
- Maung, Jack,Mallari, Jeremy P.,Girtsman, Teri A.,Wu, Lisa Y.,Rowley, Jennifer A.,Santiago, Nicholas M.,Brunelle, Alan N.,Berkman, Clifford E.
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p. 4969 - 4979
(2007/10/03)
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- Phosphonic peptide inhibitors of bacterial collagenases
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The invention relates to novel derivatives of peptides usable as inhibitors of bacterial collagenases.These derivatives comply with the formula: STR1 in which R 1 is an optionally substituted aryl or aralkyl group or the group STR2 with R 6 being the side chain of an α-amino acid and R 7 R 8 a protective group or a radical derived from an amino acid or a protected peptide, R 2 is derived from proline, hydroxyproline, thiazolidine or dehydroproline, R 3 is H or an alkyl, and R 4 is the side chain of an amino acid and R 5 and R'' 5 are H, a metal, an alkyl or benzyl.The derivatives in which R'' 5 is a metal or hydrogen can be used as inhibitors of bacterial collagenases.
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- PHOSPHONATE AND PHOSPHONAMIDE ENDOPEPTIDASE INHIBITORS
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Compounds of the formula STR1 wherein Y is O or NH and X is STR2 will inhibit the action of neutral endopeptidase. As a result, such compounds produce diuresis, natriuresis, and lower blood pressure as well as being useful in the treatment of congestive heart failure, relieving pain, and diarrhea when administered to a mammalian host.
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