title: Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs.
abstract: Fifty-two 2-benzoylaminobenzoate analogs were synthesized and subjected to anti-platelet aggregation assay using arachidonic acid (AA), collagen (Col), thrombin (Thr), and U46619 as inducers. The results revealed that most of 2-benzoylaminobenzoic acid derivatives showed a selectively inhibitory effect on AA-induced platelet aggregation. As a result of the 2-benzoylaminobenzoic acid derivatives (18, 44, and 46), there were no inhibitory effects on platelet aggregation induced by U46619, but these elicited an inhibitory effect on thromboxane B(2) formation at 1.0microM. These 2-benzoylaminobenzoate analogs were therefore proposed as cyclooxygenase inhibitors.
authors.affiliation: Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung 807, Taiwan. pewehs@kmu.edu.tw
authors.forename: Pei-Wen
authors.initials: PW
authors.lastname: Hsieh
authors.forename: Shin-Zan
authors.initials: SZ
authors.lastname: Chiang
authors.forename: Chin-Chung
authors.initials: CC
authors.lastname: Wu
authors.forename: Yi-Ching
authors.initials: YC
authors.lastname: Lo
authors.forename: Yu-Tzu
authors.initials: YT
authors.lastname: Shih
authors.forename: Yang-Chang
authors.initials: YC
authors.lastname: Wu
mesh_terms: D062365:Aminobenzoates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D062365:Aminobenzoates; D010975:Platelet Aggregation Inhibitors