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Special Issue "Asymmetric Synthesis and Medicinal Chemistry"

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A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 January 2010)

Special Issue Editor

Guest Editor
Prof. Dr. Oliver Reiser

Institut für Organische Chemie, Universität Regensburg, Universitätsstr. 31, 93053 Regensburg, Germany
Website | E-Mail
Phone: 49-9419434631
Fax: +49 (0)941 943 4121
Interests: asymmetric catalysis; stereoselective synthesis; natural product; synthesis; unnatural amino acids; foldamers

Special Issue Information

Dear Colleagues,

Any new drug that¹s chiral is likely to be developed and marketed as a single enantiomer. You win more than you lose with single enantiomers.

This statement from an article in Chem. Eng. News emphasized in 2003 the importance of enantiopure pharmaceuticals. Asymmetric Synthesis and Medicinal Chemistry are areas closely related to each other, and very often fundamental contributions in the development of new asymmetric processes initially disclosed on small scale are transfered in a most impressive way into industrial applications, showing the relevance of those fields for academia and industry alike.

I would like to invite contributions to this special issue of Pharamceuticals "Asymmetric Synthesis and Medicinal Chemistry" as an opportunity to showcase the creativity of leading scientists to tackle the challenges in the development of chiral drugs.

Prof. Dr. Oliver Reiser
Guest Editor

Published Papers (1 paper)

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Research

Open AccessArticle Synthesis and Neuroprotective Action of Optically Pure Neoechinulin A and Its Analogs
Pharmaceuticals 2010, 3(4), 1063-1069; doi:10.3390/ph3041063
Received: 21 December 2009 / Revised: 5 January 2010 / Accepted: 29 March 2010 / Published: 31 March 2010
Cited by 3 | PDF Full-text (207 KB) | HTML Full-text | XML Full-text
Abstract
We developed an efficient, stereoselective synthetic method for the diketopiperazine moiety of neoechinulin A and its derivatives. The intramolecular cyclization at 80 ºC proceeded with minimal racemization of the stereogenic center at C-12 on neoechinulin A, even though the cyclization at 110 ºC
[...] Read more.
We developed an efficient, stereoselective synthetic method for the diketopiperazine moiety of neoechinulin A and its derivatives. The intramolecular cyclization at 80 ºC proceeded with minimal racemization of the stereogenic center at C-12 on neoechinulin A, even though the cyclization at 110 ºC caused partial racemization. In contrast with these results, the cyclization on diketopiperazine of 8,9-dihydroneoechinulin A derivatives did not cause epimerization of the stereogenic centers, even at 110 °C. We examined the structure-activity relationships for the cytoprotective activity against cytotoxicity induced by 3-morpholinosydnonimine (SIN-1) in nerve growth factor (NGF)-differentiated PC12 cells. The C-8/C-9 double bond, but not the stereogenic center derived from alanine, was found to play a key role in the cytoprotective activity. Full article
(This article belongs to the Special Issue Asymmetric Synthesis and Medicinal Chemistry)
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