Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin

Clara Cena; Marco L Lolli; Loretta Lazzarato; Elena Guaita; Giuseppina Morini; Gabriella Coruzzi; Stuart P McElroy; Ian L Megson; Roberta Fruttero; Alberto Gasco

doi:10.1021/jm020969t

Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin

Clara Cena
, Marco L Lolli
, Loretta Lazzarato
, Elena Guaita
, Giuseppina Morini
, Gabriella Coruzzi
, Stuart P McElroy
, Ian L Megson
, Roberta Fruttero
, Alberto Gasco

科研成果: Article › 同行评审

101 引用（Scopus）

摘要

A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.

源语言	English
页（从-至）	747-54
页数	8
期刊	Journal of Medicinal Chemistry
卷	46
期	5
DOI	https://doi.org/10.1021/jm020969t
出版状态	Published - 2003

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10.1021/jm020969t

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title = "Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin",

abstract = "A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.",

author = "Clara Cena and Lolli, \{Marco L\} and Loretta Lazzarato and Elena Guaita and Giuseppina Morini and Gabriella Coruzzi and McElroy, \{Stuart P\} and Megson, \{Ian L\} and Roberta Fruttero and Alberto Gasco",

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T1 - Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin

AU - Cena, Clara

AU - Lolli, Marco L

AU - Lazzarato, Loretta

AU - Guaita, Elena

AU - Morini, Giuseppina

AU - Coruzzi, Gabriella

AU - McElroy, Stuart P

AU - Megson, Ian L

AU - Fruttero, Roberta

AU - Gasco, Alberto

PY - 2003

Y1 - 2003

N2 - A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.

AB - A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.

U2 - 10.1021/jm020969t

DO - 10.1021/jm020969t

M3 - Article

C2 - 12593655

SN - 0022-2623

VL - 46

SP - 747

EP - 754

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 5

ER -

Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin

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