Ontology highlight
ABSTRACT:
SUBMITTER: Li Z
PROVIDER: S-EPMC5304296 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Li Zhe Z Partridge James J Silva-Garcia Abel A Rademacher Peter P Betz Andreas A Xu Qing Q Sham Hing H Hu Yunjin Y Shan Yuqing Y Liu Bin B Zhang Ying Y Shi Haijuan H Xu Qiong Q Ma Xubo X Zhang Li L
ACS medicinal chemistry letters 20161206 2
A series of macrocyclic analogues were designed and synthesized based on the cocrystal structure of small molecule plasma kallikrein (pKal) inhibitor, <b>2</b>, with the pKal protease domain. This led to the discovery of a potent macrocyclic pKal inhibitor <b>29</b>, with an IC<sub>50</sub> of 2 nM for one olefinic isomer and 42.3 nM for the other olefinic isomer. ...[more]