Synthesis, resolution, and antiplatelet activity of 3-substituted 1(3H)-isobenzofuranone.
A series of 3-substituted-1(3H)-isobenzofuranone 6a-g and 7a-g were synthesized from phthalic anhydride. The compound 6a-g was resolved. The antiplatelet activities of these compounds were evaluated using in vitro experiment of platelet aggregation. The levels of antiplatelet activity were displayed as following sequence: l-isomer >dl-isomer>d-isomer, respectively. The alkylphthalide is more active than the corresponding alkenephthalide. All these compounds were less active than n-butylphthalide (NBP, 6c) and Aspirin (Asp).
Yang
Hua
H
Research Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, Changsha 410013, PR China.
Hu
Gao-Yun
GY
Chen
Jun
J
Wang
Yi
Y
Wang
Zhong-Hua
ZH
D004353:Drug Evaluation, Preclinical; D005663:Furans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D005663:Furans; D010975:Platelet Aggregation Inhibitors