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Design, Synthesis and pharmacological evaluation of new compounds 1,2,5-oxadiazole-2-oxide useful as preventive of atherothrombosis.

Grant number: 11/15520-4
Support Opportunities:Scholarships in Brazil - Master
Effective date (Start): March 01, 2012
Effective date (End): November 30, 2013
Field of knowledge:Health Sciences - Pharmacy - Medicines Analysis and Control
Principal Investigator:Jean Leandro dos Santos
Grantee:Luiz Antonio Dutra
Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil


In Brazil, cardiovascular diseases account for the increased mortality rate in all regions, representing 30% of all deaths in the country in individuals between 30 and 69 years. Among cardiovascular diseases, atherosclerosis is highly prevalent. The disease is progressive and characterized by the accumulation of lipids and fibrous components in arteries leading to the formation of atheromas. These decrease or block the caliber of the vessels causing ischemic events. There is a close association between atherosclerosis and atherothrombosis. After the rupture or erosion of atherosclerotic plaque is extravasated prothrombotic contents into the circulation leading to platelet adhesion and aggregation, thrombin generation, fibrin and thrombus formation. Due to the essential activity of platelets in thromboembolic disease, antiplatelet drugs have important therapeutic value as a preventive atherothrombosis in reducing morbidity and mortality due to atherothrombotic disease. The AAS is one of the most used antiplatelet drugs in the prevention of atherothrombosis. The drug inhibits the formation of thromboxane (platelet aggregation inducer and vasoconstrictor properties holder). However, AAS use has limitations as a series of induction of gastric ulcers, weak inhibition of platelet function, blocking only one pathway mediated by thromboxane interpaciente variable and response ("resistance") with weak inhibition of aggregation in some patients. Once therapy with aspirin has limitations and undesirable effects, the use of tools such as molecular changes, such as the hybridization is a strategy for discovery of more effective antiplatelet drugs. In this context, through the agency of different pathways: inhibition of thromboxane associated with the donation of nitric oxide by spaced subunit N-acyl hydrazone, is being sought synthetically compounds with antiplatelet activity are optimized for the original prototype AAS.

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
DUTRA, LUIZ ANTONIO; DE ALMEIDA, LETICIA; PASSALACQUA, THAIS G.; REIS, JULIANA SANTANA; TORRES, FABIO A. E.; MARTINEZ, ISABEL; PECCININI, ROSANGELA GONCALVES; CHIN, CHUNG MAN; CHEGAEV, KONSTANTIN; GUGLIELMO, STEFANO; et al. Leishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivatives. Antimicrobial Agents and Chemotherapy, v. 58, n. 8, p. 4837-4847, . (11/15520-4, 12/50359-2)
DUTRA, LUIZ ANTONIO; GUANAES, JESSICA FRADE O.; JOHMANN, NADINE; LOPES PIRES, MARIA ELISA; CHIN, CHUNG MAN; MARCONDES, SISI; DOS SANTOS, JEAN LEANDRO. Synthesis, antiplatelet and antithrombotic activities of resveratrol derivatives with NO-donor properties. Bioorganic & Medicinal Chemistry Letters, v. 27, n. 11, p. 2450-2453, . (15/19531-1, 11/15520-4, 15/21271-8, 14/03945-9)
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
DUTRA, Luiz Antonio. Planejamento, síntese e avaliação farmacológica de novos compostos 1,2,5-oxadiazol-2-n-óxido úteis como preventivos de aterotrombose. 2013. Master's Dissertation - Universidade Estadual Paulista (Unesp). Faculdade de Ciências Farmacêuticas. Araraquara Araraquara.

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