Novel and potential anti-Alzheimer's agents: from design to preclinical studies

• Grant number: 13/50788-3
• Support Opportunities: Regular Research Grants
• Duration: January 01, 2014 - April 30, 2016
• Field of knowledge: Health Sciences - Pharmacy
• Convênio/Acordo: Consejo Superior de Investigaciones Cientificas (CSIC)
• Principal Investigator: Ivone Carvalho
• Grantee: Ivone Carvalho
• Principal researcher abroad: Ana Martinez Gil
• Institution abroad: Instituto de Química Médica (IQM), Spain
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Associated research grant: 12/14114-5 - Design, synthesis and evaluation of dual binding sites acetylcholinesterase inhibitors as potential anti-Alzheimer's drug candidates, AP.R

Abstract

Alzheimer's disease (AD) is a process involving progressive and irreversible decline of cognitive functíons which lead to disorganization of the behavior and psychotic symptoms being their incidence exponentially associated to the increase of life expectancy. The World Health Organization estimates that in 20 years, mental illness and neurological disorders will be the second cause of death worldwide and more than 50 millions of AD patients are expected all over the world. Today, there is no effective therapy for delay or stop the neuronal loss, being an urgent need for current societies. Alzheimer's disease drug therapy research is a priority for our world where a global effort should be done. The present proposal is designed to provide two main goals: the first one is strategic and a global platform for drug discovery in AD is here proposed as reference and help for many countries in South America and other communities in the world. The second goal is to provide new drug candidates for AD that can meet the criteria to be transferred to the pharmaceutical industry for further development to clinical trials. Joint efforts from multidisciplinary teams belonging to the Pharmaceutical Sciences Faculty from USP and the Medicinal Chemistry Institute of CSIC (IQM-CSIC) can provide experience and strategic vision to successfully accomplish these goals. (AU)

Scientific publications

(4)

(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)

CHIERRITO, TALITA P. C.; PEDERSOLI-MANTOANI, SUSIMAIRE; ROCA, CARLOS; SEBASTIAN-PEREZ, VICTOR; MARTINEZ-GONZALEZ, LORETO; PEREZ, DANIEL I.; PEREZ, CONCEPCION; CANALES, ANGELES; JAVIER CANADA, F.; CAMPILLO, NURIA E.; et al. Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 145, p. 431-444, FEB 10 2018. (14/10414-0, 13/50788-3, 12/14114-5, 12/04054-5)

MANTOANI, SUSIMAIRE P.; CHIERRITO, TALITA P. C.; VILELA, ADRIANA F. L.; CARDOSO, CARMEN L.; MARTINEZ, ANA; CARVALHO, IVONE. Novel Triazole-Quinoline Derivatives as Selective Dual Binding Site Acetylcholinesterase Inhibitors. Molecules, v. 21, n. 2, FEB 2016. (13/50788-3, 13/01710-1, 12/14114-5, 12/04054-5)

DE ANDRADE, PETERSON; MANTOANI, SUSIMAIRE P.; GONCALVES NUNES, PAULO SERGIO; MAGADAN, CARLOS ROCA; PEREZ, CONCEPCION; XAVIER, DANILO JORDAO; SAKAMOTO HOJO, ELZA TIEMI; CAMPILLO, NURIA E.; MARTINEZ, ANA; CARVALHO, IVONE. Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer's disease. Bioorganic & Medicinal Chemistry, v. 27, n. 6, p. 931-943, MAR 15 2019. (12/14114-5, 14/04868-8, 13/50788-3)

CHIERRITO, TALITA P. C.; PEDERSOLI-MANTOANI, SUSIMAIRE; ROCA, CARLOS; REQUENA, CARLOS; SEBASTIAN-PEREZ, VICTOR; CASTILLO, WILLIAN O.; MOREIRA, NATALIA C. S.; PEREZ, CONCEPCION; SAKAMOTO-HOJO, ELZA T.; TAKAHASHI, CATARINA S.; et al. From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 139, p. 773-791, OCT 20 2017. (12/14114-5, 13/50788-3, 12/04054-5)