Synthesis of L-Phenylalanine Derivatives as the Inhibitors against the SARS-CoV 3CL Protease
Date Issued
2006
Date
2006
Author(s)
Chen, Chun-Lin
DOI
zh-TW
Abstract
Severe Acute Respiratory Syndrome (SARS) first occurred in Guandong (China) in November of 2002. In only a few months, nearly 1000 lives were claimed. The fatality rate of SARS coronavirus infection is rather high, estimated to be 10%.
We found the phenylalanine derivatives possessed good inhibitory activities. The compound prepared from 2-chloro-4-nitroaniline, L-phenylalanine, and 4-(dimethylamino)benzoic acid is the most potent inhibitor, showing an IC50 of 0.06 μM. The boronate analog of L-phenylalanine also showed inhibitory activities. We currently conduct the hydrolysis to remove the pinanediol moiety in order to get the boronic acid compounds as the transition state mimics of phenylalinine, and evaluate their anti-SARS activity.
Subjects
冠狀病毒
抑制劑
SARS
inhibitor
Type
thesis
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