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Design, Synthesis and Biological Evaluation of Some 2‐ A zetidinone Derivatives as Potential Antihyperlipidemic Agents
Author(s) -
Arya Nikhilesh,
Dwivedi Jaya,
Khedkar Vijay M.,
Coutinho Evans C.,
Jain Kishor S.
Publication year - 2013
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300262
Subject(s) - chemistry , combinatorial chemistry , biological activity , stereochemistry , pharmacology , biochemistry , in vitro , biology
In an effort to develop new molecules with improved antihyperlipidemic activity, eight new 2‐azetidinone analogs ( 4a – 4h ) of ezetimibe were designed through in silico docking experiments with the crystal structure of the Niemann‐Pick C1‐like 1 protein (NPC1L1). Synthesis and further antihyperlipdemic evaluation of this series in the Triton WR 1339 induced hyperlipidemic rat model showed some of the molecules to exhibit significant lipid‐lowering effects comparable to ezetimibe. Correlation between the observed biological activity and the in silico molecular docking scores of the compounds was observed.