1.
Bioorg Med Chem Lett
; 17(24): 6707-13, 2007 Dec 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17977724
RESUMO
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.
Assuntos
Benzeno/química , Cianetos/química , Inibidores da Dipeptidil Peptidase IV , Inibidores de Proteases/síntese química , Inibidores de Proteases/farmacologia , Pirróis/química , Pirróis/farmacologia , Aminação , Animais , Dipeptidil Peptidase 4/química , Dipeptidil Peptidase 4/metabolismo , Cães , Desenho de Fármacos , Humanos , Concentração Inibidora 50 , Modelos Moleculares , Estrutura Molecular , Inibidores de Proteases/química , Ratos , Estereoisomerismo , Relação Estrutura-Atividade
2.
J Am Mosq Control Assoc
; 8(2): 196, 1992 Jun.
Artigo
em Inglês
| MEDLINE
| ID: mdl-1359008
RESUMO
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.
