Author/Authors :
John Bird، نويسنده , , Gregory P. Harper، نويسنده , , Ian Hughes، نويسنده , , David J. Hunter، نويسنده , , Eric H. Karran، نويسنده , , Roger E. Markwell، نويسنده , , Anette J. Miles-Williams، نويسنده , , Shahzad S. Rahman، نويسنده , , Robert W. Ward، نويسنده ,
Abstract :
A series of thiol-, aminophosphonic acid-, and hydroxamic acid-containing collagenase inhibitors, with lactam and azalactam P2′/P3′ substituents has been prepared and evaluated in vitro as inhibitors of human fibroblast collagenase. The most potent inhibitor was the hydroxamic acid 17a (IC50 12 nM). Introduction of a basic amino function into the lactam ring had little effect on potency, but greatly enhanced aqueous solubility.
