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Hidaka, Koshi*; Kimura, Toru*; Abdel-Rahman, H. M.*; Nguyen, J.-T.*; McDaniel, K. F.*; Kohlbrenner, W. E.*; Molla, A.*; Adachi, Motoyasu; Tamada, Taro; Kuroki, Ryota; et al.
Journal of Medicinal Chemistry, 52(23), p.7604 - 7617, 2009/07
Times Cited Count：20 Percentile：44.99(Chemistry, Medicinal)A series of HIV protease inhibitor based on the allophenylnorstatine structure with various P2' moieties were synthesized. Among these analogues, we discovered that a small allyl group would maintain potent enzyme inhibitory activity compared to that of the 
-methylbenzyl moiety in clinical candidate 1 (KNI-764, also known as JE-2147, AG-1776 or SM-319777). Introduction of an anilinic amino group to 2 (KNI-727) improved water-solubility and anti-HIV-1 activity. X-ray crystallographic analysis of 13k (KNI-1689) with a 
-methallyl group at P2' position revealed hydrophobic interactions with Ala28, Ile84, and Ile50' similar to that of 1. The presence of an additional methyl group on the allyl group in compound 13k significantly increased anti-HIV activity over 1, while providing a rational drug design for structural minimization and improving membrane permeability.
Tani, Norio; Adachi, Toshikazu*; Igarashi, Susumu*; Watanabe, Yasuhiro; Someya, Hirohiko*; Sato, Hikaru*; Kishiro, Junichi
IEEE Transactions on Applied Superconductivity, 14(2), p.409 - 412, 2004/06
Times Cited Count：18 Percentile：62.45The 3-GeV synchrotron proposed in the JAERI/KEK Joint Project (J-PARC) is a rapid-cycling synchrotron (RCS), which accelerates a high-intensity proton beam from 400-MeV to 3-GeV at a repetition rate of 25-Hz. The 3-GeV synchrotron is used to produce pulsed spallation neutrons and muons. It also works as an injector for a 50-GeV synchrotron. The 3-GeV synchrotron consists of 24 dipole magnets, 60 quadrupole magnets, 18 sextupole magnets and 52 steering magnets. Since the magnets for the 3-GeV synchrotron are required to have a large aperture in order to realize the large beam power of 1 MW, there is a larger fringe field at a pole end than a usual synchrotron magnet. Therefore, it is important to estimate the magnetic field and the effect of multipole component at the fringe field. In this paper, we report the results of the field calculation and mechanical design of RCS magnets.
Tani, Norio; Adachi, Toshikazu*; Someya, Hirohiko*; Watanabe, Yasuhiro; Sato, Hikaru*; Kishiro, Junichi
IEEE Transactions on Applied Superconductivity, 14(2), p.421 - 424, 2004/06
Times Cited Count：14 Percentile：56.04The 3-GeV synchrotron proposed in the JAERI/KEK Joint Project (J-PARC) is a rapid-cycling synchrotron (RCS), which accelerates a high-intensity proton beam from 400-MeV to 3-GeV at a repetition rate of 25-Hz. The 3-GeV synchrotron is used to produce pulsed spallation neutrons and muons. Since the magnets for the 3-GeV synchrotron are required to have a large aperture in order to realize the large beam power of 1 MW, there is a larger fringe field at a pole end than a usual synchrotron magnet. In addition, 25-Hz ac field induces an eddy current in magnet components, magnet end plates and etc. The eddy current induced in the end plates is expected to be large. Therefore, it is important to investigate an effect of large leakage field and eddy current to the beam motion around the magnet end part. We have measured the eddy loss and the eddy field at the edges of the dipole and quadrupole magnets. In this paper, we report the comparison between the results of the measurements and the two-dimensional eddy current model developed for this study.
Funatsu, Takahiro*; Adachi, Hikaru*; Shimizu, Norikazu*; Sato, Toshinori; Yamachi, Hiroshi*
no journal, ,
no abstracts in English
