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1. chinaXiv:201711.02425 [pdf]

Discovery of novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on a pharmacokinetic property-driven optimization

Hui Xie; Saogao Zeng; Lili Zeng; Xiaobing Lan; Guicheng Zhang; Li Liu; Xin Lu; Na Chen; Zhiyuan Li; Zengzhao Tu; Hongjiang Xu; Ling Yang; Xiquan Zhang; Wenhui Hu
Subjects: Biology >> Ecology

Followed pharmacological evaluation exposed an extensive hepatic first pass effect within our recently disclosed DPP-IV inhibitors bearing thienopyrimidine scaffold. Through scaffold replacement with pyrrolopyrimidine, compound 1a had substantially improved the metabolic stability (from 6.6% to 65.07%), yet with severely poor absorptive property. Further modification by incorporation with varied substituents and structure conversion yielded both permeable and metabolic stable compounds. The whole pharmacokinetic- property based optimization had succeeded in balancing overall properties and resulted in the compound 1j, that with excellent efficacy to be a potential anti-diabetic candidate.

submitted time 2017-11-17 Hits1117Downloads674 Comment 0

2. chinaXiv:201711.02427 [pdf]

Discovery of multiple lead compounds as M2 inhibitors through the screening of a focused library of scaffold-hops

Wenhui Hu; Shaogao Zeng; Chufang Li; Zhiyuan Li; Ling Chen
Subjects: Biology >> Ecology

It is urgent to discover new anti-influenza drugs considering the threat of so called swine flu and Spanish flu. Though Adamantane derivatives are the only M2 inhibitors as anti-influenza virus A drugs, they are limited to use in the US due to drug resistant. Herein we reported that multiple lead compounds as M2 inhibitors were rapidly generated through the screening of focused library designed with scaffold-hopping strategy based on Amantadine.

submitted time 2017-11-17 Hits1215Downloads653 Comment 0

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