[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.
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Li-mei
LM
Gao
Peng
P
Yang
Dan-qing
DQ
Song
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