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Bioorg Med Chem Lett ; 12(13): 1727-30, 2002 Jul 08.
Article in English | MEDLINE | ID: mdl-12067547

ABSTRACT

The solid-phase synthesis of substituted 1,2,4-triazoles tethered to a 4-mercaptopyrrolidine core 1 is described. This novel class of non-peptidic, Zn(2+) metallo-protease inhibitors was found to have inhibitory activity for the endothelin converting enzyme (ECE-1). The SAR of the substitution pattern in 1 is discussed.


Subject(s)
Aspartic Acid Endopeptidases/antagonists & inhibitors , Protease Inhibitors/chemistry , Protease Inhibitors/chemical synthesis , Pyrrolidines/chemistry , Pyrrolidines/chemical synthesis , Triazoles/chemistry , Triazoles/chemical synthesis , Endothelin-Converting Enzymes , Humans , Inhibitory Concentration 50 , Metalloendopeptidases/antagonists & inhibitors , Protease Inhibitors/pharmacology , Pyrrolidines/pharmacology , Structure-Activity Relationship , Triazoles/pharmacology
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