Antimicrobial and Cytotoxicity Potential of Acetamido, Amino and Nitrochalcones

T. C. Tristão; F. Campos-Buzzi; R. Corrêa; R.C B. Cruz; V. Cechinel Filho; A. Bella Cruz

doi:10.1055/s-0032-1327610

Arzneimittelforschung, Inhaltsverzeichnis

Arzneimittelforschung 2012; 62(12): 590-594
DOI: 10.1055/s-0032-1327610

Original Article

Antimicrobial and Cytotoxicity Potential of Acetamido, Amino and Nitrochalcones

T. C. Tristão

¹Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil

,

F. Campos-Buzzi

¹Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil

²Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Itajaí, Brazil

,

R. Corrêa

¹Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil

²Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Itajaí, Brazil

,

R.C B. Cruz

²Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Itajaí, Brazil

,

V. Cechinel Filho

¹Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil

²Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Itajaí, Brazil

,

A. Bella Cruz

¹Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil

²Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Itajaí, Brazil

› Institutsangaben

Abstract

Background:

Chalcones constitute one of the major classes of natural products belonging to the flavonoid family, and they have been reported as having a range of important therapeutic activities, including some chalcones are effective as antimicrobial agents. Currently, the search for new structures with antimicrobial activity has been intensified due to the emergence of many strains resistant to antibiotics currently used to treat infectious diseases.

Method:

3 chalcone series (amino, acetamido and nitrochalcones) were prepared (23 compounds) and evaluated for their antimicrobial and cytotoxic potential. The effects of substituents on their respective activities also was evaluated.

Results & Conclusion:

The results showed that 4 aminochalcones (2, 4, 8, 9), 3 acetoamidochalcones (10, 14, 18) and 3 nitrochalcones (20, 22, 23), exhibited antifungal effects. The aminochalcones were more toxic than the acetamidochalcones, while the nitrochalcones did not present any toxic effect. It was verified that there seems to be structure-activity correlation in some electron-donating and withdrawing substituents groups in rings A and B of the synthetized chalcone analogues and its antifungal and cytotoxic activity.

Key words

antibacterial - antifungal - Artemia salina - QSAR - chalcone

Volltext

Referenzen

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