Design, Synthesis and Biological Evaluation of Lipophilic Analogs of Anethol Trithione

被引：2
|
作者：
Li, Xiao-Cen [2 ]
Fan, Wei [2 ]
Hai, Li [2 ]
Qian, Shan [2 ]
Xiao, Qui-Qi [1 ]
Guan, Mei [1 ]
机构：
[1] Sichuan Univ, W China Hosp, Chengdu 610041, Sichuan, Peoples R China
[2] Sichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Sichuan, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 10期
关键词：
Synthesis; Anethol trithione; Lipophilicity; Bioavailability; Prodrugs;
D O I：
10.2174/1570180811007010747
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
16 ADT carboxylate esters were prepared and tested for their chemical characteristics, stability, bioavailability, potency and toxicity. Considering the good bioavailability, 3a was selected for the pharmacology test, and the result showed that the potency of 3a was remarkably higher than that of ATT. Additionally, 3a was also chosen for the acute toxicity test. The result indicated that the prodrug 3a was more safer than ATT. The study suggested the feasibility to improve the bioavailability of ATT by using prodrug strategy.
引用
收藏
页码：747 / 753
页数：7
相关论文
共 50 条
  • [31] Synthesis and biological activity of lipophilic analogs of the cationic antimicrobial active peptide anoplin
    Chionis, Kostas
    Krikorian, Dimitrios
    Koukkou, Anna-Irini
    Sakarellos-Daitsiotis, Maria
    Panou-Pomonis, Eugenia
    JOURNAL OF PEPTIDE SCIENCE, 2016, 22 (11-12) : 731 - 736
  • [32] Design and synthesis of sulfur-containing pseudilin analogs and their biological activity evaluation
    Wang, Jili
    Zhou, Yaqing
    Chen, Can
    Wang, Zhiyi
    Wu, Xin
    Zhou, Xin
    Sun, Yong
    Wu, Wenhai
    Zhang, Aidong
    PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY, 2025, 208
  • [33] Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents
    Elicio, Pablo D.
    Chao, Maria N.
    Galizzi, Melina
    Li, Catherine
    Szajnman, Sergio H.
    Docampo, Roberto
    Moreno, Silvia N. J.
    Rodriguez, Juan B.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 69 : 480 - 489
  • [34] Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARα
    Mizuno, Cassia S.
    Ma, Guoyi
    Khan, Shabana
    Patny, Akshay
    Avery, Mitchell A.
    Rimando, Agnes M.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (07) : 3800 - 3808
  • [35] Design, synthesis, and biological evaluation of tetrazole analogs as protein arginine deiminase inhibitors
    Subramanian, Venkataraman
    Knight, Jason S.
    Kaplan, Mariana J.
    Thompson, Paul R.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 247
  • [36] Design, synthesis and biological evaluation of nitrate ester analogs of SCP-1
    Das, Madhurima
    Bazan, Nicolas
    Trudell, Mark
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2018, 256
  • [37] Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation
    Pecnard, Shannon
    Provot, Olivier
    Levaique, Helene
    Bignon, Jerome
    Askenatzis, Laurie
    Saller, Francois
    Borgel, Delphine
    Michallet, Sophie
    Laisne, Marie-Catherine
    Lafanechere, Laurence
    Alami, Mouad
    Hamze, Abdallah
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 209
  • [38] Design, synthesis and biological evaluation of Novel Curcumin Analogs with anticipated anticancer activity
    Fawzy, Iten M.
    Youssef, Khairia M.
    Ismail, Nasser S. M.
    Gullbo, J.
    Abouzid, Khaled A. M.
    FUTURE JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 1 (01) : 22 - 31
  • [39] Design, Synthesis and Biological Evaluation of Novel Indole-Thalidomide Hybrids Analogs
    Zahran, M. A. -H.
    El Kosey, S.
    Mehany, A. B.
    Gebreil, M. H.
    EGYPTIAN JOURNAL OF CHEMISTRY, 2020, 63 (11): : 4175 - 4184
  • [40] Design, synthesis and biological evaluation of comformation restricted analogs of FTY720
    Huang, Tao
    Kharel, Yugesh
    Lynch, Kevin R.
    Macdonald, Timothy L.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2012, 243
12345