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Investigation of Platelet Aggregation Inhibitory Activity by Phenyl Amides and Esters of Piperidinecarboxylic Acids by Modesto de Candia; Luciana Summo; Antonio Carrieri; Cosimo Altomare; Adele Nardecchia; Saverio Cellamare; Angelo Carotti is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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A series of anilides and phenyl esters of piperidine-3-carboxylic acid (nipecotic acid) were synthesized and tested for the ability to inhibit aggregation of human platelet rich-plasma triggered by adenosine 5'-diphosphate (ADP) and adrenaline. As a rule, amides were about two times more active than the corresponding esters, and derivatives bearing substituents at the para position of the phenyl ring were significantly more active than the meta-substituted ones. Among the tested compounds, 4-hexyloxyanilide of nipecotic acid (18a) was found to be the most active one, its IC(50) value being close to that of the most active bis-3-carbamoylpiperidines reported in literature (ca. 40 micro M) and aspirin (ca. 60 microM) in ADP- and adrenaline-induced aggregation, respectively. Compared with the isomeric 4-hexyloxyanilides of piperidine-2-carboxylic (pipecolinic) and piperidine-4-carboxylic (isonipecotic) acids, compound 18a showed higher activity, and a Hansch-type quantitative structure-activity relationship (QSAR) study highlighted lipophilicity and increase in electron density of the phenyl ring as the properties which mainly increase the antiplatelet activity (r(2)=0.74, q(2)=0.64).

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Author

Modesto de Candia; Luciana Summo; Antonio Carrieri; Cosimo Altomare; Adele Nardecchia; Saverio Cellamare; Angelo Carotti

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2003

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)