Journal ArticleDOI
Structure of FK506, a novel immunosuppressant isolated from Streptomyces
Hirokazu Tanaka,Akio Kuroda,Hiroshi Marusawa,Hiroshi Hatanaka,Toru Kino,Toshio Goto,Masashi Hashimoto,Toru Taga +7 more
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This article is published in Journal of the American Chemical Society.The article was published on 1987-08-01. It has received 523 citations till now. The article focuses on the topics: Streptomyces tsukubaensis & Streptomyces.read more
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Patent
Synthetic process for fk-506 type macrolide intermediates
TL;DR: In this article, a process for the conversion of FK-506 (I,R = allyl;1) to FK525 (XV) and analogous 23-membered ring macrolides differing in the C.1-N.7 segment of the molecule (e.g. XVI) is presented.
Patent
Process for synthesis of FK-506 and tricarbonyl intermediates
Todd K. Jones,Sander G. Mills,David Askin,Robert A. Reamer,Richard Desmond,David M. Tschaen,Ralph P. Volante,Ichiro Shinkai +7 more
TL;DR: In this article, a process for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof is described.
Journal ArticleDOI
Drug Syntheses Beyond the Rule of 5
TL;DR: It is concluded that structural simplification, planning of synthetic routes regarding incorporation of stereocenters and macrocylisation, as well as incorporation of structural knowledge and consideration of chameleonic properties in design should facilitate drug discovery in bRo5 space.
Journal ArticleDOI
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities
Marco Robello,Elisabetta Barresi,Emma Baglini,Silvia Salerno,Sabrina Taliani,Federico Da Settimo +5 more
TL;DR: In this paper, the α-ketoamide motif is used as a privileged structure in drug discovery and a brief analysis of its physical-chemical features and synthetic procedures to obtain it is presented.
Journal ArticleDOI
Maintenance Immunosuppression: New Agents and Persistent Dilemmas
TL;DR: Tacrolimus and mycophenolate mofetil appear to increase graft survival in pancreas-kidney recipients but their efficacy in another high-risk group, African-American recipients, has not yet been clearly shown, however, the trend toward improved graft survive in African- American recipients treated with tacrolimous is encouraging.