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Preparation ánd biological evaluation of curcumin-cinnamaldehyde hybrids às bacterial cell division inhibitors: Methoxychalcones (part 2)

Grant number: 16/08084-7
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): July 01, 2016
Effective date (End): December 31, 2016
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:Luis Octávio Regasini
Grantee:Beatriz de Carvalho Marques
Home Institution: Instituto de Biociências, Letras e Ciências Exatas (IBILCE). Universidade Estadual Paulista (UNESP). Campus de São José do Rio Preto. São José do Rio Preto , SP, Brazil

Abstract

Anti-infective agents are crucial drugs for life expectancy. Several reasons justify the need for new antibacterials, including high bacterial resistance and high mortality caused by infectious diseases. Thus, efforts are need to develop innovative antibacterial drugs. Recently, curcumin and cinnmaldehyde exhibited potent antibacterial activity. The central interest by these natural products is related to their bacterial cell division inhibitory effect, and their interaction with FtsZ protein (Filamentous temperature-sensitive protein Z), which is a vital macromolecule for all bacteria. The current project purposes the synthesis of three series of curcumin-cinnamaldehyde hybrids, which are methoxychalcones and their derivatives. These compounds will be prepared by aldol condensation reactions between ketone derivatives and aldehydes, under basic catalysis, as well as nucleophilic addition of alpha,beta-unsaturated ketones. Compounds will be tested against Gram-positive, Gram-negative bacteria and Mycobacterium species, using sensitive and resistant strains. The toxicity of selected antibacterial compounds will be evaluated on macrophages. The selective index (SI) of compounds will be calculated from IC50 and MBC values, IS = IC50/MBC. IC50 is a half maximal inhibitory concentration to kill macrophages and MBC is a minimum bactericidal concentration. Compounds displayed IS e 10 will be submitted to inhibitory bacterial cell division assays, using FtsZ sedimentation and GTP hydrolysis methods.