David James Beecham Pha Hunter

TL;DR: The synthesis of a series of N-phosphonalkyl dipeptides 6 is described, devised that allowed the preparation of single diastereoisomers and the assignment of stereochemistry and potency was enhanced by introducing bicyclic aromatic P2' substituents.

TL;DR: A series of peptidomimetic aminophosphonic acid derivatives was synthesized and evaluated in vitro for inhibition of human fibroblast collagenase activity and incorporation of a bromonaphthalimidoethyl moiety at the P1 position led to potent inhibitors, such as 14a.

TL;DR: In this article, a process for their preparation and their use as collagenase inhibitors are described, in which Rℓ is hydrogen or hydroxy; R₁ is hydrogen, alkyl, -CH₂-Z where Z is optionally substituted phenyl or heteroaryl.

TL;DR: In this article, a process for their preparation and their use as collagenase inhibitors is described, and a number of novel compounds of the formula (I) are described. But none of them are described in detail.

TL;DR: The synthesis of a series of N-phosphonalkyl dipeptides was described in this paper, which were at least 10-fold more potent than their corresponding N-carboxyalkyl analogues.