Synthesis, Crystal Structure and Biological Evaluation of 4, 5, 6, 7-tetrahydropravastatin as HMG-CoA Reductase Inhibitor

被引：1
|
作者：
Li, Jing [1 ]
Li, Huan [1 ]
Zhang, Lei [1 ]
机构：
[1] S China Univ Technol, Sch Biosci & Bioengn, Guangzhou Higher Educ Mega Ctr, Guangzhou 510006, Guangdong, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2011年 / 8卷 / 09期
关键词：
Crystal structure; HMG-CoA reductase; hydrogenation; pravastatin; 4; 5; 6; 7-tetrahydropravastatin; COENZYME-A REDUCTASE; THERAPY;
D O I：
10.2174/157018011797200876
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
4, 5, 6, 7-Tetrahydropravastatin and its sodium salt as the hydrogenated derivatives of pravastatin were evaluated as HMG-CoA reductase inhibitor in vitro and in vivo, and they exhibited similar antihyperlipidaemic activity to pravastatin. The results could be regarded as a particular case to the reported SARs of statins up to now.
引用
收藏
页码：884 / 888
页数：5
相关论文
共 50 条
  • [41] HMG-CoA reductase inhibitor cerivastatin inhibits interleukin-6 expression and secretion in human adipocytes
    van Harmelen, V
    Skurk, T
    Röhrig, K
    Hauner, H
    HORMONE AND METABOLIC RESEARCH, 2003, 35 (08) : 466 - 470
  • [42] COMPARATIVE-EVALUATION OF THE SAFETY AND EFFICACY OF HMG-COA REDUCTASE INHIBITOR MONOTHERAPY IN THE TREATMENT OF PRIMARY HYPERCHOLESTEROLEMIA
    HSU, I
    SPINLER, SA
    JOHNSON, NE
    ANNALS OF PHARMACOTHERAPY, 1995, 29 (7-8) : 743 - 759
  • [43] A new and efficient synthesis of the HMG-CoA reductase inhibitor pitavastatin (vol 90, pg 1069, 2007)
    Acemoglu, Murat
    Brodbeck, Andre
    Garcia, Angel
    Grimler, Dominique
    Hassel, Marc
    Riss, Bernhard
    Schreiber, Robert
    HELVETICA CHIMICA ACTA, 2007, 90 (07) : 1447 - 1447
  • [44] Synthesis and biological evaluations of condensed pyridine and condensed pyrimidine-based HMG-CoA reductase inhibitors
    Suzuki, M
    Iwasaki, H
    Fujikawa, Y
    Sakashita, M
    Kitahara, M
    Sakoda, R
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (10) : 1285 - 1288
  • [45] HMG-COA REDUCTASE INHIBITORS .1. SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF ARYL SUBSTITUTED CYCLOALKENES
    NEUENSCHWANDER, K
    REGAN, J
    SCOTESE, A
    KOSMIDER, B
    BRUNO, J
    AMIN, D
    GUSTAFSON, S
    WEINACHT, J
    PERRONE, M
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1990, 200 : 125 - MEDI
  • [46] Hepatoselectivity of statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors
    Park, William K. C.
    Kennedy, Robert M.
    Larsen, Scott D.
    Miller, Steve
    Roth, Bruce D.
    Song, Yuntao
    Steinbaugh, Bruce A.
    Sun, Kevin
    Tait, Bradley D.
    Kowala, Mark C.
    Trivedi, Bharat K.
    Auerbach, Bruce
    Askew, Valerie
    Dillon, Lisa
    Hanselman, Jeffrey C.
    Lin, Zhiwu
    Lu, Gina H.
    Robertson, Andrew
    Sekerke, Catherine
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (03) : 1151 - 1156
  • [47] Synthesis and HMG-CoA reductase inhibition of 2-cyclopropyl-4-thiophenyl-quinoline mevalonolactones
    Zhao, Shikui
    Zhou, Weicheng
    Liu, Jun
    BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (23) : 7915 - 7923
  • [48] Development of an Early Enabling Synthesis for PF-03052334-02: A Novel Hepatoselective HMG-CoA Reductase Inhibitor
    Bowles, Daniel M.
    Boyles, David C.
    Choi, Chulho
    Pfefferkom, Jeffrey A.
    Schuyler, Stephanie
    ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2011, 15 (01) : 148 - 157
  • [49] MEASUREMENT OF STEROL SYNTHESIS AND TISSUE DISTRIBUTION OF A LIVER SELECTIVE HMG-COA REDUCTASE INHIBITOR, CI-981
    FERGUSON, E
    MCNALLY, W
    BOCAN, TMA
    UHLENDORF, PD
    KRAUSE, BR
    SLISKOVIC, DR
    OBRIEN, P
    ROTH, BD
    NEWTON, RS
    FASEB JOURNAL, 1991, 5 (05): : A1253 - A1253
  • [50] DEFICIENT INTESTINAL CHOLESTEROL-SYNTHESIS IS INHERITED IN SITOSTEROLEMIA - SITOSTEROL IS NOT A FEEDBACK INHIBITOR OF INTESTINAL HMG-COA REDUCTASE
    NGUYEN, LB
    SALEN, G
    SHEFER, S
    BULLOCK, J
    CLINICAL RESEARCH, 1992, 40 (02): : A418 - A418
12345