Novel carboxylated pyrroline-2-one derivatives bearing a phenylhydrazine moiety: Design, synthesis, antifungal evaluation and 3D-QSAR analysis
作者:Min Chen、Lizhi Zhang、Aimin Lu、Xiaobin Wang、Weijie Si、Jinghua Yan、Chunlong Yang
DOI:10.1016/j.bmcl.2020.127519
日期:2020.11
Aiming to discover novel high-efficient antifungal leads that possess an innovative action mechanism, twenty-three carboxylated pyrroline-2-one derivatives, bearing a phenylhydrazine moiety, were rationally designed and firstly prepared in this letter. The in vitro bioassays showed that most of the compounds possessed excellent antifungal effects with the EC50 values of less than 1 μg/mL against the
Inhibitors of HCV replication of formula I
including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R′ are, each independently, —CR
1
R
2
R
3
, aryl, heteroaryl or heteroC
4-6
cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl.
The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
申请人:Genentech, Inc.
公开号:US20180065983A1
公开(公告)日:2018-03-08
Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure:
or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.