Showing papers by "Kunisuke Izawa published in 2016"
TL;DR: Compounds Currently in Phase II−III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas is presented.
Abstract: Compounds Currently in Phase II−III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas Yu Zhou,† Jiang Wang,† Zhanni Gu,† Shuni Wang,† Wei Zhu,† Jose ́ Luis Aceña,*,‡,§ Vadim A. Soloshonok,*,‡,∥ Kunisuke Izawa,* and Hong Liu*,† †Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China ‡Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizab́al 3, 20018 San Sebastiań, Spain Department of Organic Chemistry, Autońoma University of Madrid, Cantoblanco, 28049 Madrid, Spain IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, 48013 Bilbao, Spain Hamari Chemicals Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka, Japan 533-0024
1,740 citations
TL;DR: A review of the recent progress in identification of purely chemical, small-molecule drugs of considerable potential to be used as effective therapeutics for prevention, diagnosis, and treatment of EBOV profiles three compounds – favipiravir, BCX-4430, and brincidofovir – identified by the World Health Organization as high-priority targets.
32 citations
TL;DR: Excellent yields and diastereoselectivity coupled with reliable and easy scalability render this method of immediate use for practical synthesis of (1R,2S)-vinyl-ACCA.
Abstract: Asymmetric synthesis of (1R,2S)-1-amino-2-vinylcyclopropanecarboxylic acid (vinyl-ACCA) is in extremely high demand due to the pharmaceutical importance of this tailor-made, sterically constrained α-amino acid. Here we report the development of an advanced procedure for preparation of the target amino acid via two-step SN2 and SN2' alkylation of novel axially chiral nucleophilic glycine equivalent. Excellent yields and diastereoselectivity coupled with reliable and easy scalability render this method of immediate use for practical synthesis of (1R,2S)-vinyl-ACCA.
32 citations
TL;DR: In this paper, the authors highlight the recent progress in identification of purely chemical, small-molecule drugs of considerable potential to be used as effective therapeutics for prevention, diagnosis, and treatment of EBOV.
Abstract: The current epidemic of Ebola virus (EBOV) hemorrhagic fever in sub-Saharan West-African countries, in terms of severity, is second only to the human immunodeficiency virus (HIV). Besides the strong pathogenicity of EBOV, the unprecedented fatality rates (up to 90 %) are partially the result of a near total absence of any proper vaccines and therapeutics to combat the EBOV epidemic. This review highlights the recent progress in identification of purely chemical, small-molecule drugs of considerable potential to be used as effective therapeutics for prevention, diagnosis, and treatment of EBOV. In particular, we profile three compounds – favipiravir, BCX-4430, and brincidofovir – identified by the World Health Organization as high-priority targets. The detailed syntheses and modes of antiviral activity of these drugs are critically discussed. The major goal of this review is to encourage the chemistry community to focus research on this area of high social impact.