Synthesis of stemofoline analogues as acetylcholinesterase inhibitors

Thirty-two new stemofoline analogues were prepared from didehydrostemofoline for studies as AChE inhibitors. C-3 Side-chain modified amino, carbamate, triazole and oxazole stemofoline derivatives were prepared. In general the amine derivatives were found to be stronger inhibitors of AChE than their...

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Main Authors:	Kwankamol Sastraruji, Thanapat Sastraruji, Alison T. Ung, Renate Griffith, Araya Jatisatienr, Stephen G. Pyne
Format:	Journal
Published:	2018
Subjects:	Biochemistry, Genetics and Molecular Biology Chemistry Pharmacology, Toxicology and Pharmaceutics
Online Access:	https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84863853821&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/51359
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Institution:	Chiang Mai University

id	th-cmuir.6653943832-51359
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spelling	th-cmuir.6653943832-513592018-09-04T06:13:13Z Synthesis of stemofoline analogues as acetylcholinesterase inhibitors Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Renate Griffith Araya Jatisatienr Stephen G. Pyne Biochemistry, Genetics and Molecular Biology Chemistry Pharmacology, Toxicology and Pharmaceutics Thirty-two new stemofoline analogues were prepared from didehydrostemofoline for studies as AChE inhibitors. C-3 Side-chain modified amino, carbamate, triazole and oxazole stemofoline derivatives were prepared. In general the amine derivatives were found to be stronger inhibitors of AChE than their alcohol analogues that we previously reported. Compounds 5 and 26, with small C-3 side-chain substituents, were two of the most active inhibitors. Preliminary molecular docking studies suggested that these compounds may inhibit AChE by binding horizontally along the passage of the active-site gorge and block access to acetylcholine. © 2012 Elsevier Ltd. All rights reserved. 2018-09-04T06:00:46Z 2018-09-04T06:00:46Z 2012-09-02 Journal 14645416 00404020 2-s2.0-84863853821 10.1016/j.tet.2012.06.047 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84863853821&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/51359
institution	Chiang Mai University
building	Chiang Mai University Library
country	Thailand
collection	CMU Intellectual Repository
topic	Biochemistry, Genetics and Molecular Biology Chemistry Pharmacology, Toxicology and Pharmaceutics
spellingShingle	Biochemistry, Genetics and Molecular Biology Chemistry Pharmacology, Toxicology and Pharmaceutics Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Renate Griffith Araya Jatisatienr Stephen G. Pyne Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
description	Thirty-two new stemofoline analogues were prepared from didehydrostemofoline for studies as AChE inhibitors. C-3 Side-chain modified amino, carbamate, triazole and oxazole stemofoline derivatives were prepared. In general the amine derivatives were found to be stronger inhibitors of AChE than their alcohol analogues that we previously reported. Compounds 5 and 26, with small C-3 side-chain substituents, were two of the most active inhibitors. Preliminary molecular docking studies suggested that these compounds may inhibit AChE by binding horizontally along the passage of the active-site gorge and block access to acetylcholine. © 2012 Elsevier Ltd. All rights reserved.
format	Journal
author	Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Renate Griffith Araya Jatisatienr Stephen G. Pyne
author_facet	Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Renate Griffith Araya Jatisatienr Stephen G. Pyne
author_sort	Kwankamol Sastraruji
title	Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
title_short	Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
title_full	Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
title_fullStr	Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
title_full_unstemmed	Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
title_sort	synthesis of stemofoline analogues as acetylcholinesterase inhibitors
publishDate	2018
url	https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84863853821&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/51359
_version_	1681423755555897344

Synthesis of stemofoline analogues as acetylcholinesterase inhibitors

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