1.
Bioorg Med Chem Lett
; 17(24): 6707-13, 2007 Dec 15.
Article
in English
| MEDLINE
| ID: mdl-17977724
ABSTRACT
The cis-3-amino-4-(2-cyanopyrrolidide)-pyrrolidine template has been shown to afford low nanomolar inhibitors of human DPP-IV that exhibit a robust PK/PD profile. An X-ray co-crystal structure of 5 confirmed the proposed mode of binding. The potent single digit DPP-IV inhibitor 53 exhibited a preferred PK/PD profile in preclinical animal models and was selected for additional profiling.
Subject(s)
Benzene/chemistry , Cyanides/chemistry , Dipeptidyl-Peptidase IV Inhibitors , Protease Inhibitors/chemical synthesis , Protease Inhibitors/pharmacology , Pyrroles/chemistry , Pyrroles/pharmacology , Amination , Animals , Dipeptidyl Peptidase 4/chemistry , Dipeptidyl Peptidase 4/metabolism , Dogs , Drug Design , Humans , Inhibitory Concentration 50 , Models, Molecular , Molecular Structure , Protease Inhibitors/chemistry , Rats , Stereoisomerism , Structure-Activity Relationship
2.
J Am Mosq Control Assoc
; 8(2): 196, 1992 Jun.
Article
in English
| MEDLINE
| ID: mdl-1359008
ABSTRACT
Culiseta impatiens is reported for the first time from Maryland. Collections from the southwestern border of Fort George G. Meade extend the range of this species over 400 km farther south than previous records. Multiple collections from 4 separate traps during 2 years indicate a population of Cs. impatiens is probably established in the collection area.
