Biological activity screening of some hydrazone and chalcone derivatives

Küçük Resim Yok

Tarih

2021

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Refik Saydam National Public Health Agency (RSNPHA)

Erişim Hakkı

info:eu-repo/semantics/openAccess

Özet

Objective: Today, the development of resistance to antibiotics is increasing rapidly. Loss of antibiotics effectiveness due to the development of resistance causes serious hazards. Especially methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis create life-threatening conditions in patients with a weak immune system. For this reason, it is important to develop new drug active substances against these microorganisms. In this article, hydrazones and chalcones were synthesized and some biological activities of these compounds such as antimicrobial and antituberculosis were investigated. This study was conducted to investigate new antimicrobial and antituberculous drug-active substances instead of antibiotics that lost their effectiveness due to the rapidly increasing resistance to existing antibiotics. Methods: The compounds were obtained by synthesis of chalcones via Claisen Schmidt condensation and then by reacting these chalcones with hydrazides to form hydrazone. Antimicrobial and antituberculosis activities of the compounds were evaluated by microdilution method and microplate alamar blue assays, respectively. Results: All compounds displayed the same activity against Mycobacterium tuberculosis (MIC: 64 ?g/mL). E4, 4'-Bromo-4-methyl chalcone, displayed the best activity against Meticilline resistant-Staphylococcus aureus (MIC: 16 ?g/mL). The most effective compounds against Enterococcus faecalis isolate and Enterococcus faecalis were found B26 (N-(1-(4fluorophenyl)-3-p-tolylallylidene)thiophene-2-carbohydrazide) and E8 (4'-fluoro-3-methyl chalcone), respectively (MIC: 32 ?g/mL). Conclusion: Hydrazones have been found to be more effective than chalcones against S. aureus ATCC 29213. However, chalcones exhibited a remarkable effect against meticilline resistant-Staphylococcus aureus and Enterococcus faecalis. In terms of tuberculosis bacillus, it did not differ whether the compounds had a chalcone or hydrazone structure. Both chalcones and hydrazones exhibited the same activity against candida species. All compounds were observed to be more effective than gentamicin against methicillin-resistant Staphylococcus aureus. © 2021, Turk Hijyen ve Deneysel Biyoloji Dergisi. All Rights Reserved.

Açıklama

Anahtar Kelimeler

Antimicrobial; Antitubercular; Chalcone; Hydrazone; Microbial Resistance

Kaynak

Turk Hijyen ve Deneysel Biyoloji Dergisi

WoS Q Değeri

Scopus Q Değeri

Q4

Cilt

78

Sayı

2

Künye