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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Antiplatelet activity and TNF- release inhibition of phthalimide derivatives useful to treat sickle cell anemia

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Author(s):
Chelucci, Rafael C. [1] ; de Oliveira, Isabela J. [1] ; Barbieri, Karina P. [1] ; Lopes-Pires, Maria E. [2] ; Polesi, Marisa C. [1] ; Chiba, Diego E. [1] ; Carlos, Iracilda Z. [1] ; Marcondes, Sisi [2] ; Dos Santos, Jean L. [1] ; Chung, ManChin [1]
Total Authors: 10
Affiliation:
[1] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, Araraquara, SP - Brazil
[2] State Univ Campinas UNICAMP, Fac Med Sci, Campinas, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: MEDICINAL CHEMISTRY RESEARCH; v. 28, n. 8, p. 1264-1271, AUG 2019.
Web of Science Citations: 0
Abstract

Sickle Cell Anemia (SCA) is one of the most prevalent hereditary hematological diseases worldwide. The disease is characterized by chronic inflammation, hypercoagulable state, and pro-thrombotic profile, which lead the vaso-occlusive process. In this work, we described the antiplatelet activity and the ability to reduce tumor necrosis factor-alpha (TNF-) levels of phthalimide derivatives. All compounds inhibited platelet aggregation induced by collagen and adenosine diphosphate, at levels ranging from 26.0 to 74.2% and 30.7 to 79.6%, respectively. The compounds exhibited reduced bleeding time compared to acetylsalicylic acid (ASA). Moreover, compounds 4c and 10c inhibited TNF- levels at 73.5% and 65.0%, respectively. These findings suggest that phthalimide derivatives 4c and 10c are promising lead compounds useful to prevent vaso-occlusion and inflammation associated with the sickle cell anemia. {[}GRAPHICS] . (AU)

FAPESP's process: 15/19531-1 - Targeting histone deacetylase (HDAC-1 and HDAC-2) as mechanisms to induce fetal hemoglobin in sickle cell disease
Grantee:Jean Leandro dos Santos
Support Opportunities: Regular Research Grants
FAPESP's process: 13/23461-3 - Planning, synthesis and pharmacological evaluation of hybrid compounds with potential activity in the treatment of Alzheimer's Disease
Grantee:Rafael Consolin Chelucci
Support Opportunities: Scholarships in Brazil - Doctorate