Design and synthesis of triazolyl-flavone hybrids: Investigation of biological activities against leishmaniasis and Chagas disease.

• Grant number: 17/01249-3
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• Start date: September 01, 2017
• End date: September 14, 2021
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Elizabeth Igne Ferreira
• Grantee: Pone Kamdem Boniface
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Based on the urgent need of new leads/drug candidates for Chagas disease and leishmaniasis, and taking into account that some flavones have promising antiparasitic activity and that the triazole is a group found in many anti-infective compounds, the aim of the project is to synthesize triazolyl-flavone hybrids with the purpose of obtaining compounds potentially active in leishmaniasis and Chagas disease. So, monotriazolyl- and bistriazolyl-flavone hybrids with and without sugar moieties(D-mannose, D-galactose and D-ribose, directing groups for selectivity) will be synthesized. Antileishmanial and trypanomicide activity of the synthesized compounds will be determined,as well as permeability studies of the synthesized compounds in order to appraise their bioavailability, and cytotoxicity of the synthesized compounds will be carried out.

Scientific publications

(6)

(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)

BONIFACE, PONE KAMDEM; FERREIRA, ELIZABETH IGNE. Flavonoids as efficient scaffolds: Recent trends for malaria, leishmaniasis, Chagas disease, and dengue. Phytotherapy Research, v. 33, n. 10, AUG 2019. (17/01249-3)

BONIFACE, PONE K.; ELIZABETH, I, FERREIRA. Flavones as a Privileged Scaffold in Drug Discovery: Current Developments. CURRENT ORGANIC SYNTHESIS, v. 16, n. 7, p. 968-1001, 2019. (17/01249-3)

PONE, BONIFACE KAMDEM; FERREIRA, ELIZABETH IGNE. Therapeutic Potential of Flavonoid Derivatives for Certain Neglected Tropical Diseases. CURRENT DRUG TARGETS, v. 23, n. 7, p. 3-pg., 2022-01-01. (17/01249-3)

KAMDEM, BONIFACE PONE; KAMTO, EUTROPHE LE DOUX; PAUMO, HUGUES KAMDEM; KATATA-SERU, LEBOGANG MAUREEN; PEGNYEMB, DIEUDONNE EMMANUEL; IGNE, FERREIRA ELIZABETH. Chemical Constituents, Ethnomedicinal Uses, Pharmacology, and Toxicity of Dysphania Ambrosioides (L.) Mosyakin & Clemants, Formerly Chenopodium Ambrosioides L.. NATURAL PRODUCTS JOURNAL, v. 12, n. 3, p. 43-pg., 2022-01-01. (17/01249-3)

BONIFACE, PONE K.; SANO, CINTHYA M.; ELIZABETH, I, FERREIRA. Unveiling the Targets Involved in the Quest of Antileishmanial Leads Using In silico Methods. CURRENT DRUG TARGETS, v. 21, n. 7, p. 681-712, 2020. (17/01249-3)

KAMDEM, BONIFACE PONE; KAMTO, EUTROPHE LE DOUX; SOH, DESIRE; PEGNYEMB, DIEUDONNE EMMANUEL; ZINGUE, STEPHANE; PAUMO, HUGUES KAMDEM; KATATA-SERU, LEBOGANG MAUREEN; ABOU, ABOUBAKAR; ROSINAH, MONTSHO MAIYANE; MBAH, JAMES AJECK; et al. Pharmacological Activity and Mechanisms of Action of Terpenoids from Laurus nobilis L.. NATURAL PRODUCTS JOURNAL, v. 13, n. 7, p. 18-pg., 2023-01-01. (17/01249-3)