[Synthesis and insulinotropic activity of 2-benzylidenesuccinic acid derivatives].
OBJECTIVE
To design and synthesize new compounds of prandial glucose regulator with more simple structure.


METHODS
The target compounds were synthesized from diethyl succinate and benzaldehyde or 4-fluorobenzaldehyde by four-step reactions. Thus 18 compounds were synthesized. Their structures were comfirmed by NMR, MS and IR.


RESULTS
Seventeen compounds had different hypoglycemic activity in mice, among them, 9 compounds had higher hypoglycemic activity and 6 compounds had character of prandial glucose regulator.


CONCLUSIONS
Part of the compounds have higher hypoglycemic activity deserve to be further investigated.
Gao
Li-mei
LM
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Yang
Peng
P
Song
Dan-qing
DQ
D000818:Animals; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001786:Blood Glucose / Q000378:metabolism; D002219:Carbamates / Q000138:chemical synthesis / Q000737:chemistry; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000737:chemistry; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry; D054833:Isoindoles; D051379:Mice; D015394:Molecular Structure; D000077715:Nateglinide; D010649:Phenylalanine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship; D013386:Succinates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D001597:Benzylidene Compounds; D001786:Blood Glucose; D002219:Carbamates; D003510:Cyclohexanes; D007004:Hypoglycemic Agents; D007211:Indoles; D054833:Isoindoles; D010880:Piperidines; D013386:Succinates; D000077715:Nateglinide; D010649:Phenylalanine; C072379:repaglinide; C087255:mitiglinide