New Thiazolone Derivatives: Design, Synthesis, Anticancer and Antimicrobial Activity

Abstract

In order to explore the anticancer and antimicrobial activity associated with the thiazolone framework, several new (Z)-2-((5-(3fluorobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)carboxylic acid derivatives have been synthesized in water as a solvent. All synthesized compounds were evaluated for anticancer and antimicrobial activity in vitro. Amongst these, the 3-methylbutanoic and the 3-or 4-methylpentanoic acid derivatives, the 3-hydroxy-, the 3-(1H-imidazol-4-yl) and the 3-(4-hydroxyphenyl)propanoic acid derivatives and the succinic acid derivative showed high antibacterial and antifungal activity. The unsubstituted propanoic acid derivative exhibited significant antibacterial activity against B. subtilis and significant antifungal activity against fungal strains, i.e., A. flavus. The in vitro anticancer studies revealed that the 3-(hydroxy)-, the 3-(1H-imidazol-4yl)-and the 3-(4-hydroxyphenyl)propanoic acid, or the succinic acid derivatives are the most active compounds against MCF-7 and BT-474 human breast cancer cell lines.

Synthesis, spectroscopy, and theoretical calculations of some 2-thiohydantoin derivatives as possible new fungicides

“…In this work, two derivatives of 2-thiohydantoin, compound A (5-benzylidene-2-thiohydantoin-3-acetic acid) and compound B (5-cinnamylidene-2-thiohydantoin-3-acetic acid), have been synthesised. The antifungal activity of similar compounds was detected [13,32,33], so we expect that compounds synthesised here also can have this property. Studies on their antifungal properties are currently being conducted.…”

Synthesis of substituted pyrimidine using ZnFe2O4 nanocatalyst via one pot multi‐component reaction ultrasonic irradiation

“…With reference to above literature survey, in continuation to our previous research work of pharmaceutical moieties, 30–36 we have focused on synthesis of imidazo[1,2‐ a ]pyrimidine‐3‐carbonitrile derivatives (4a‐j ) using efficient and heterogeneous Zinc Ferrite (ZnFe 2 O 4 ) as nanocatalyzed one‐pot three‐component condensation reaction of benzimidazole ( 1 ) and malononitrile (3) with substituted aromatic aldehyde (2a‐j ) in methanol under ultrasonic irradiations. Author has selected normal spinel catalyst ZnFe 2 O 4 for present synthesis because ammonia molecule preferred to adsorbed on the surface of Zn atom of spinal zinc ferrite and it is used to removal of ammonia 37 .…”

Synthesis of 2-((5-Benzylidene-4-Oxo-4,5-Dihydrothiazol-2-Yl)-Substituted Amino Acids as Anticancer and Antimicrobial Agents

“…[19][20][21][22][23][24] These reports suggested that Rhodanine nuclei were essential to the observed levels of antimicrobial activity. [25][26][27][28] We make a plan to synthesized Rhodanine derivatives as an antimicrobial agent by preparing hybrid molecules having similar features of reported potent antimicrobial agents (Figure 1). Because of the facts mentioned above, Rhodanine derivatives were synthesized, characterized by different spectral analysis techniques and screened for their antimicrobial activity.…”