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Study Data from COMSATS Institute of Information Technology Provide New Insights into Carboxylic Ester Hydrolases

June 20, 2014

By a News Reporter-Staff News Editor at Health & Medicine Week -- Investigators publish new report on Enzymes and Coenzymes. According to news reporting from Abbottabad, Pakistan, by NewsRx journalists, research stated, "The present study reports the synthesis of cinnamide derivatives and their biological activity as inhibitors of both cholinesterases and anticancer agents. Controlled inhibition of brain acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) may slow neurodegeneration in Alzheimer's diseases (AD)."

The news correspondents obtained a quote from the research from the COMSATS Institute of Information Technology, "The anticholinesterase activity of phenylcinnamide derivatives was determined against Electric Eel acetylcholinesterase (EeAChE) and horse serum butyrylcholinesterase (hBChE) and some of the compounds appeared as moderately potent inhibitors of EeAChE and hBChE. The compound 3-(2-(Benzyloxy)phenyl)-N-(3,4,5-trimethoxyphenyl)acrylamide (3i) showed maximum activity against EeAChE with an IC50 0.29 +/- 0.21 mu M whereas 3-(2-chloro-6-nitrophenyl)-N-(3,4,5-trimethoxyphenyl)acrylamide (3k) was proved to be the most potent inhibitor of hBChE having IC50 1.18 +/- 1.31 mu M. To better understand the enzyme-inhibitor interaction of the most active compounds toward cholinesterases, molecular modelling studies were carried out on high-resolution crystallographic structures. The anticancer effects of synthesized compounds were also evaluated against cancer cell line (lung carcinoma)."

According to the news reporters, the research concluded: "The compounds may be useful leads for the design of a new class of anticancer drugs for the treatment of cancer and cholinesterase inhibitors for Alzheimer's disease (AD)."

For more information on this research see: Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases. European Journal of Medicinal Chemistry, 2014;78():43-53. European Journal of Medicinal Chemistry can be contacted at: Elsevier France-Editions Scientifiques Medicales Elsevier, 23 Rue Linois, 75724 Paris, France. (Elsevier -; European Journal of Medicinal Chemistry -

Our news journalists report that additional information may be obtained by contacting A. Saeed, COMSATS Inst Informat Technol, Dept. of Pharmaceut Sci, Abbottabad 22060, Pakistan. Additional authors for this research include P.A. Mahesar, S. Zaib, M.S. Khan, A. Matin, M. Shahid and J. Iqbal (see also Enzymes and Coenzymes).

Keywords for this news article include: Asia, Pakistan, Abbottabad, Cholinesterases, Enzymes and Coenzymes, Carboxylic Ester Hydrolases

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Source: Health & Medicine Week

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