Discovery of AX8312, an N-alkyl-Gly-boro-Pro Derivative that Accelerates Recovery from Neutropenia in the Mouse

Emme C. K. Lin,Kevin R. Shreder,Melissa C. Zhang,Yi Hu,Lisa Morera,Min Wu,Melissa S. Wong,Lifu Ma,Doris Chun,Sergio Corral,John W. Kozarich

LETTERS IN DRUG DESIGN & DISCOVERY（2008）

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摘要

A screen of N-alkyl-Gly-boro-Pro DPP inhibitors using an acute murine model revealed that N-adamantyl and N-cycloalkyl groups greater in size than cyclobutyl significantly induced G-CSF. Treatment of neutropenic mice with the most efficacious compound, AX8312 (N-(1-adamantyl)-Gly-boro-Pro), resulted in a faster and greater neutrophil recovery versus vehicle-treated mice.

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关键词

N-alkyl-Gly-boro-Pro,G-CSF,neutropenia,cytokine,AX8312

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