http://www.mdpi.com/journal/pharmaceuticals/special_issues/asymmetr/ 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 Submission Information All papers should be submitted to pharmaceuticals@mdpi.com. To be published continuously until the deadline and papers will be listed together at the special issue website. Submitted papers should not have been published nor be under consideration for publication elsewhere. All papers are refereed through a peer-review process. A guide for authors is available on the Instructions for Authors page. Pharmaceuticals is a new international, peer-reviewed, quarterly open access journal published by MDPI. Article Processing Charges (APC) for publication in this open access journal are waived for well-prepared manuscripts submitted by 30 June 2010. English correction or formatting fees of 250 CHF (Swiss Francs) will be charged in certain cases for those paper accepted for publication, that require extensive additional formatting and/or English corrections. http://www.mdpi.com/1424-8247/3/4/1063/ 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. http://www.mdpi.com/1424-8247/3/4/1063/ Wed, 31 Mar 2010 00:00:00 CEST Pharmaceuticals 2010-03-31 3 4 Article 1063 1069 1424-8247 Synthesis and Neuroprotective Action of Optically Pure Neoechinulin A and Its Analogs 2010-03-31 doi: 10.3390/ph3041063 Aoki Ohnishi Kimoto Fujieda Kuramochi Takeuchi Nakazaki Watanabe Sugawara Arai Kobayashi