Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain

Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain Publisher Pubmed

Pourshojaei Y¹ ; Gouranourimi A¹ ; Hekmat S¹ ; Asadipour A² ; Rahmaninezhad S¹ ; Moradi A³ ; Nadri H³ ; Moghadam FH³ ; Emami S⁴ ; Foroumadi A^{2, 5} ; Shafiee A¹

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medicinal Sciences, Tehran, 14176, Iran
2. Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medicinal Sciences, Kerman, Iran
3. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
4. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
5. Drug Design and Development Research Center, Tehran University of Medicinal Sciences, Tehran, Iran

Source: European Journal of Medicinal Chemistry Published:2015

Abstract

A series of 3-(4-(aminoalkoxy)benzylidene)-chroman-4-ones 7a-r were designed and synthesized as analogs of homoisoflavonoids which are well known natural products with diverse pharmacological properties related to Alzheimer's disease. The in vitro anti-cholinesterase activity of designed compounds 7a-r against AChE and BuChE, revealed that compounds bearing piperidinylethoxy residue showed potent activity against AChE at sub-micromolar level (IC50 values = 0.122-0.207 μM), more potent than reference drug tacrine. The structure-activity relationships study of piperidinylethoxy series demonstrated that the selectivity and physicochemical properties of compounds could be optimized by selection of a proper substituent on the C-7 position of chroman ring, while the high potency of the molecule against AChE was reserved. © 2015 Elsevier Masson SAS.

Style	Citing Format
MLA	Pourshojaei Y, et al.. "Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain." European Journal of Medicinal Chemistry, vol. 97, no. , 2015, pp. 181-189.
APA	Pourshojaei Y, Gouranourimi A, Hekmat S, Asadipour A, Rahmaninezhad S, Moradi A, Nadri H, Moghadam FH, Emami S, Foroumadi A, Shafiee A (2015). Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain. European Journal of Medicinal Chemistry, 97(), 181-189.
Chicago	Pourshojaei Y, Gouranourimi A, Hekmat S, Asadipour A, Rahmaninezhad S, Moradi A, Nadri H, et al.. "Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain." European Journal of Medicinal Chemistry 97, no. (2015): 181-189.
Harvard	Pourshojaei Y et al. (2015) 'Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain', European Journal of Medicinal Chemistry, 97(), pp. 181-189.
Vancouver	Pourshojaei Y, Gouranourimi A, Hekmat S, Asadipour A, Rahmaninezhad S, Moradi A, et al.. Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain. European Journal of Medicinal Chemistry. 2015;97():181-189.
BibTex	@article{ author = {Pourshojaei Y and Gouranourimi A and Hekmat S and Asadipour A and Rahmaninezhad S and Moradi A and Nadri H and Moghadam FH and Emami S and Foroumadi A and Shafiee A}, title = {Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain}, journal = {European Journal of Medicinal Chemistry}, volume = {97}, number = {}, pages = {181-189}, year = {2015} }
RIS	TY - JOUR AU - Pourshojaei Y AU - Gouranourimi A AU - Hekmat S AU - Asadipour A AU - Rahmaninezhad S AU - Moradi A AU - Nadri H AU - Moghadam FH AU - Emami S AU - Foroumadi A AU - Shafiee A TI - Design, Synthesis and Anticholinesterase Activity of Novel Benzylidenechroman-4-Ones Bearing Cyclic Amine Side Chain JO - European Journal of Medicinal Chemistry VL - 97 IS - SP - 181 EP - 189 PY - 2015 ER -

Science Communicator Platform

Authors

Authors Affiliations

Abstract