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Design, synthesis and biological evaluation of new derivatives of Lapdesf FTD-AO and Lapdesf FTD-TAU series with potential activity in the treatment of Alzheimer's Disease

Grant number: 16/08470-4
Support type:Scholarships in Brazil - Doctorate
Effective date (Start): August 01, 2016
Effective date (End): June 30, 2019
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Chung Man Chin
Grantee:Diego Eidy Chiba
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Associated scholarship(s):17/13524-9 - Design, synthesis and biological evaluation of new derivatives of LAPDESF FTD-AO and LAPDESF FTD-TAU series with potential activity in the treatment of Alzheimer's Disease, BE.EP.DR

Abstract

Alzheimer's disease (AD) is the main and most common cause of senile dementia, responsable for 50-75% of diagnosed cases. In developed countries, AD is the fourth cause of death, only behind of cardiovascular disease, cancer and stroke. The projection of the World Health Organization (WHO) is that by 2050 the number of elderly will increase 21% in the world. AD is a progressive neurodegenerative disease, in which patients diagnosed show an extensive loss of synapses and neurons in the hippocampus and frontal and temporal cortex, compromising gradually his cognitive functions such as memory, learning ability, thinking, besides of the impairment of communication skills and performance of daily activities. Currently there is no treatment able to cure or modify effectively the disease, only medications (tacrine, donepezil, rivastigmine, galantamine and memantine) that improve some symptoms manifested by patients. It is therefore of great importance to find and develop new therapeutic approaches and new drugs able to delay or prevent the progression of the disease. Because of the described, this project aims to obtain two series of novel drug candidates with anti-inflammatory / neuroprotective activities, using molecular hybridization of lipoic acid or ferulic acid with phtalimide derivatives (first series containing phenyl group and the second series containing the amino acid taurine), mainly by exploiting the properties of TNF-± inhibition, microtubule stabilizing and antioxidant. The reduction in the process of neuroinflammation and oxidative stress associated with aging and DA biomarkers, such as the formation of senile plaques and neurofibrillary tangles, contributes to synaptic plasticity, cognition and memory, which mitigate the effects associated with neuronal loss in AD patients

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)
SANTOS FERNANDES, GUILHERME FELIPE; BERNARDES SILVA, GABRIEL DALIO; PAVAN, ALINE RENATA; CHIBA, DIEGO EIDY; CHIN, CHUNG MAN; DOS SANTOS, JEAN LEANDRO. Epigenetic Regulatory Mechanisms Induced by Resveratrol. NUTRIENTS, v. 9, n. 11 NOV 2017. Web of Science Citations: 18.
PAVAN, ALINE RENATA; BERNARDES DA SILVA, GABRIEL DALIO; JORNADA, DANIELA HARTMANN; CHIBA, DIEGO EIDY; DOS SANTOS FERNANDES, GUILHERME FELIPE; CHIN, CHUNG MAN; DOS SANTOS, JEAN LEANDRO. Unraveling the Anticancer Effect of Curcumin and Resveratrol. NUTRIENTS, v. 8, n. 11 NOV 2016. Web of Science Citations: 38.
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
CHIBA, Diego Eidy. Planejamento, síntese e avaliação biológica de novos derivados da série LAPDESF FTD-AO com potencial atividade no tratamento da Doença de Alzheimer. 2019. Doctoral Thesis - Universidade Estadual Paulista "Júlio de Mesquita Filho" Faculdade de Ciências Farmacêuticas..

Please report errors in scientific publications list by writing to: cdi@fapesp.br.