title: Design, Synthesis and Pharmacological Evaluation of Novel Piperlongumine derivatives as Potential Antiplatelet Aggregation Candidate.
abstract: A series of novel piperlongumine derivatives (4a-i, 6a-i) were designed and synthesized. The inhibitory activities of platelet aggregation induced by ADP and AA in vitro have been evaluated by bron turbidimetry and liver microsomal incubated assay. The assay results show that compounds 4e and 6e exhibited remarkable potency to that of the positive control piplartine and aspirin.
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Yujun
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Bengbu Medical College, Bengbu, 233030, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Wang
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Jiaming
authors.initials: J
authors.lastname: Li
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Yanchun
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Weijun
authors.initials: W
authors.lastname: Huang
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Zuo
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Huicai
authors.initials: H
authors.lastname: Liu
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Di
authors.initials: D
authors.lastname: Xie
authors.affiliation: Department of Medicinal Chemistry, Anhui University of Chinese Medicine, 103 Meishan Road, Hefei, 230031, China.
authors.forename: Panhu
authors.initials: P
authors.lastname: Zhu
mesh_terms: D000244:Adenosine Diphosphate / Q000494:pharmacology; D000255:Adenosine Triphosphate / Q000494:pharmacology; D001241:Aspirin / Q000494:pharmacology; D001792:Blood Platelets / Q000378:metabolism*; D004148:Dioxolanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D006801:Humans; D010881:Piperidones / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004148:Dioxolanes; D010881:Piperidones; D010975:Platelet Aggregation Inhibitors; C498077:piperlongumine; D000244:Adenosine Diphosphate; D000255:Adenosine Triphosphate; D001241:Aspirin
keywords: antiplatelet aggregation; piperlongumine derivatives; thienopyridine