Synthesis and structure-activity relationships of novel compounds for the inhibition of TNF-α production

被引:0
|
作者
Joon Seok Park
Kyong Up Baik
Ho Jung Son
Jae Ho Lee
Se Jong Lee
Jae Youl Cho
Jisoo Park
Eun Sook Yoo
Young Seok Byun
Myung Hwan Park
机构
[1] R&D Center,
[2] Daewoong Pharm. Co. Ltd.,undefined
来源
关键词
2-[3-(Cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone; TNF-α production inhibitor; PDE 4 inhibition; Structure-activity relationship;
D O I
暂无
中图分类号
学科分类号
摘要
This study describes the synthesis,in vitro evaluation and molecular modeling study of novel compounds for the inhibition of TNF-α production. Among these compounds, 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (9) was selected as a lead compound and its pyridine derivative10 was more potent in activity and safer than rolipram.
引用
收藏
页码:332 / 337
页数:5
相关论文
共 50 条
  • [31] Synthesis and structure-activity relationships of serotonin derivatives effect on α-glucosidase inhibition
    Takahashi, Toshiyuki
    Miyazawa, Mitsuo
    MEDICINAL CHEMISTRY RESEARCH, 2012, 21 (08) : 1762 - 1770
  • [32] Synthesis and structure-activity relationships of phenylpropanoid amides of serotonin on tyrosinase inhibition
    Takahashi, Toshiyuki
    Miyazawa, Mitsuo
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (07) : 1983 - 1986
  • [33] SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF DISODIUM CROMOGLYCATE AND SOME RELATED COMPOUNDS
    CAIRNS, H
    COX, JSG
    MINSHULL, R
    FITZMAUR.C
    LORD, GH
    LEE, TB
    KING, J
    JOHNSON, PB
    HUNTER, D
    JOURNAL OF MEDICINAL CHEMISTRY, 1972, 15 (06) : 583 - +
  • [34] Inhibition of zinc metallopeptidases by flavonoids and related phenolic compounds: Structure-activity relationships
    Parellada, J
    Suarez, G
    Guinea, M
    JOURNAL OF ENZYME INHIBITION, 1998, 13 (05): : 347 - 359
  • [35] Total synthesis of a natural antioxidant and structure-activity relationships of related compounds
    Jinno, S
    Otsuka, N
    Okita, T
    Inouye, K
    CHEMICAL & PHARMACEUTICAL BULLETIN, 1999, 47 (09) : 1276 - 1283
  • [36] Synthesis and structure-activity relationships of teixobactin
    Karas, John A.
    Chen, Fan
    Schneider-Futschik, Elena K.
    Kang, Zhisen
    Hussein, Maytham
    Swarbrick, James
    Hoyer, Daniel
    Giltrap, Andrew M.
    Payne, Richard J.
    Li, Jian
    Velkov, Tony
    ANNALS OF THE NEW YORK ACADEMY OF SCIENCES, 2020, 1459 (01) : 86 - 105
  • [37] SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF BACTERIOCINS
    Vederas, J.
    BIOPOLYMERS, 2009, 92 (04) : 303 - 303
  • [38] Ketonethiosemicarbazones: Structure-activity relationships for their melanogenesis inhibition
    Thanigaimalai, Pillaiyar
    Lee, Ki-Cheul
    Sharma, Vinay K.
    Roh, Eunmiri
    Kim, Youngsoo
    Jung, Sang-Hun
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (12) : 3527 - 3530
  • [39] STRUCTURE-ACTIVITY RELATIONSHIPS OF PODOLACTONES AND RELATED COMPOUNDS
    GALBRAITH, MN
    HORN, DHS
    ITO, S
    KODAMA, M
    SASSE, JM
    AGRICULTURAL AND BIOLOGICAL CHEMISTRY, 1972, 36 (13): : 2393 - 2396
  • [40] Design, synthesis and structure-activity relationships of novel uracil compounds as potent GNRH receptor antagonists.
    Zhu, YF
    Struthers, S
    Saunders, J
    Gao, YH
    Gross, T
    Connors, P
    Reinhart, G
    Ling, N
    Chen, C
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 223 : B137 - B137