Design, synthesis and biological evaluation of GY3-based derivatives for anti-type 2 diabetes activity.
A series of indole carboxylic acid derivatives were designed and synthesized. Their anti-type 2 diabetes activity was evaluated in HepG2 cell and db/db mice. The results showed that compounds 8c, 17a, 17b, 15a and 15b could significantly increase glucose consumption in HepG2 cell. Furthermore, compound 8c was able to lower the blood glucose level and induce less weight gain in db/db mice.
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China.
Lingling
L
Fan
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China.
Jianta
J
Wang
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China.
Xiao
X
Ma
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China.
Wan
W
Xiao
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China.
Zhiyan
Z
Li
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China.
Gang
G
Zhong
College of Pharmacy, Guiyang Medical University, Guiyang 550004, China. Electronic address: tlei1974@hotmail.com.
Lei
L
Tang
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China. Electronic address: fwhs@zju.edu.cn.
Haoshu
H
Wu
D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D015195:Drug Design; D056945:Hep G2 Cells; D006801:Humans; D007210:Indoleacetic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008817:Mice, Mutant Strains; D015394:Molecular Structure
C526371:1-(4-chlorobenzoyl)-5-hydroxy-2-methyl-3-indoleacetic acid; D007210:Indoleacetic Acids
Anti-type 2 diabetes activity; Design; Indole carboxylic acid derivatives; Synthesis