Synthesis and BK channel-opening activity of 2-amino-1,3-thiazole derivatives

被引：3
|
作者：
Qi, Xiao-Lei [1 ]
Jo, Heeji [2 ,3 ]
Wang, Xue-Ying [1 ]
Ji, Tong-Tong [1 ]
Lin, Hai-Xia [1 ]
Park, Chul-Seung [2 ,3 ]
Cui, Yong-Mei [1 ]
机构：
[1] Shanghai Univ, Coll Sci, Innovat Drug Res Ctr, Dept Chem, Shanghai 200444, Peoples R China
[2] Gwangju Inst Sci & Technol GIST, Sch Life Sci, Gwangju 61005, South Korea
[3] Gwangju Inst Sci & Technol GIST, Natl Leading Res Lab, Gwangju 61005, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2021年 / 43卷
关键词：
BK channels; Openers; Synthesis; Thiazole; SAR; ACTIVATED POTASSIUM CHANNELS; SMOOTH-MUSCLE; K+ CHANNELS; PHARMACOLOGICAL ACTIVATION; TRANSMITTER RELEASE; SKELETAL-MUSCLE; BETA-SUBUNIT; BLADDER; CONTRACTILITY; EXCITABILITY;
D O I：
10.1016/j.bmcl.2021.128083
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2-amino-5-arylmethyl-or 5-heteroarylmethyl-1,3-thiazole derivatives were synthesized and evaluated for BK channel-opening activities in cell-based fluorescence assay and electrophysiological recording. The assay results indicated that the activities of the investigated compounds were influenced by the physicochemical properties of the substituent at benzene ring.
引用
收藏
页数：6
相关论文
共 50 条
  • [1] STRUCTURE OF 2-AMINO-1,3-THIAZOLE
    CARANONI, C
    REBOUL, JP
    ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE, 1982, 38 (APR): : 1255 - 1259
  • [2] Design, synthesis, and BK channel-opening activity of hexahydrodibenzazepinone derivatives
    Tashima, Toshihiko
    Toriumi, Yoshimi
    Mochizuki, Yumi
    Nonomura, Taro
    Nagaoka, Satoru
    Furukawa, Katsuo
    Tsuru, Hiromichi
    Adachi-Akahane, Satomi
    Ohwada, Tomohiko
    BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (23) : 8014 - 8031
  • [3] SYNTHESIS AND CHARACTERIZATION OF NOVEL 1,3-THIAZOLE AND 2-AMINO-1,3,4-THIADIAZOLE DERIVATIVES
    Er, Mustafa
    Sahin, Ayse
    Tahtaci, Hakan
    MACEDONIAN JOURNAL OF CHEMISTRY AND CHEMICAL ENGINEERING, 2014, 33 (02) : 189 - 198
  • [4] Synthesis and Structural Characterization of a Tetranuclear Copper Complex with 2-Amino-1,3-thiazole
    邓玉恒
    丁彦峰
    刘娟
    单晓晨
    结构化学, 2010, 29 (12) : 1818 - 1823
  • [5] Synthesis and Structural Characterization of a Tetranuclear Copper Complex with 2-Amino-1,3-thiazole
    Deng Yu-Heng
    Ding Yan-Feng
    Liu Juan
    Shan Mao-Chen
    CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2010, 29 (12) : 1818 - 1823
  • [6] Synthesis and antioxidant activity of 2-amino-4-phenyl-1,3-thiazole derivatives
    Rzaeva, IA
    Sadigova, SE
    Vekilova, TM
    Farzaliev, VM
    Magerramov, AM
    Allakhverdiev, MA
    PETROLEUM CHEMISTRY, 2005, 45 (06) : 436 - 440
  • [7] The synthesis and BK channel-opening activity of N-acylaminoalkyloxime derivatives of dehydroabietic acid
    Cui, Yong-Mei
    Liu, Xin-Lan
    Zhang, Wen-Ming
    Lin, Hai-Xia
    Ohwada, Tomohiko
    Ido, Katsutoshi
    Sawada, Kohei
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (02) : 283 - 287
  • [8] Reaction of N-aryl-3-oxobutanethioamides with 2-amino-1,3-thiazole and 2-amino-1,3-benzothiazole
    Britsun, V. N.
    Borisevich, A. N.
    Esipenko, A. N.
    Lozinskii, M. O.
    RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2007, 43 (01) : 103 - 107
  • [9] Condensation of 2-Amino-1,3-thiazole Salts and Benzo Analogs with Trifluoroacetylacetone
    Shulga, S., I
    Simurova, N., V
    Shulga, O. S.
    RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2021, 57 (03) : 364 - 368
  • [10] PARAMETERS, SPACE GROUP AND POWDER DIAGRAM OF 2-AMINO-1,3-THIAZOLE
    CARANONI, C
    CAPELLA, L
    JOURNAL OF APPLIED CRYSTALLOGRAPHY, 1982, 15 (FEB) : 106 - 107
12345