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:	Sastraruji K., Sastraruji T., Ung A., Griffith R., Jatisatienr A., Pyne S.
Format:	Journal
Published:	2017
Online Access:	https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84863853821&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/42778
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Institution:	Chiang Mai University

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spelling	th-cmuir.6653943832-427782017-09-28T06:38:58Z Synthesis of stemofoline analogues as acetylcholinesterase inhibitors Sastraruji K. Sastraruji T. Ung A. Griffith R. Jatisatienr A. Pyne S. 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. 2017-09-28T06:38:58Z 2017-09-28T06:38:58Z 2012-09-02 Journal 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/6653943832/42778
institution	Chiang Mai University
building	Chiang Mai University Library
country	Thailand
collection	CMU Intellectual Repository
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	Sastraruji K. Sastraruji T. Ung A. Griffith R. Jatisatienr A. Pyne S.
spellingShingle	Sastraruji K. Sastraruji T. Ung A. Griffith R. Jatisatienr A. Pyne S. Synthesis of stemofoline analogues as acetylcholinesterase inhibitors
author_facet	Sastraruji K. Sastraruji T. Ung A. Griffith R. Jatisatienr A. Pyne S.
author_sort	Sastraruji K.
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	2017
url	https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84863853821&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/42778
_version_	1681422253975142400

Synthesis of stemofoline analogues as acetylcholinesterase inhibitors

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