UDC: 615.276:547.789:542.91

Aim. To accomplish the synthesis and screening of anticancer and antimicrobial activities of 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones 2-10. Methods. The in vitro anticancer activity of compounds 4, 6, 8-10 has been established by DTP(Developmental Therapeutics Program) of the National Cancer Institute. The antibacterial and antifungal activities of synthesized thiazole-based derivatives were evaluated in vitro with the agar diffusion and broth microdilution methods to wards Gram-positive, Gram-negative bacteria and yeasts. For the synthesized compounds, the in silico drug-likeness screening using SwissADME online server is reported. Results. The novel 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones were synthesized from 1-[2-amino-4-methylthiazol-5-yl]ethanones and various aromatic aldehydes in the Claisen–Schmidt condensation. The synthesized compound 9 was moderately active
against the leukemia CCRF-CEM and HL-60(TB), renal cancer UO-31 and breast cancer MCF7 cell lines. The antimicrobial screening led to identification of the active compound 10 against Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. Conclusions. The results obtained herein provide a platform for structure-based optimization of these newly identified thiazole-based compounds for the anticancer and antibacterial drug design. K e y w o r d s: thiazoles, Claisen-Schmidt condensation, anticancer activity, antimicrobial activity, SwissADME

Raoultella terrigena is a rarely found opportunistic pathogen that can cause healthcare-associated infections with high mortality. It is important to differentiate it from Klebsiella species.

Keywords: Klebsiella; Raoultellaterrigena; clinical case; healthcare‐associated infections; literature review; opportunists; phylogenetic analysis; rare pathogen.

The share of Klebsiella pneumoniae in infections has been recently increasing. Multidrug-resistant strains that produce more than one antibiotic resistance mechanism are also increasingly isolated. Contamination of the organs preservation fluid occurs quite often, but the isolated microorganisms are mainly saprophytic bacteria that are part of the skin microbiota (coagulase-negative Staphylococcus, Corynebacterium spp). The following case describes a K. pneumoniae blood infection in a patient after liver transplantation. Susceptibility of the strains to chosen antimicrobials was determined using the automated method. For strain isolated from blood, it was confirmed by loop-mediated isothermal amplification of genetic material. © 2021 Indian Association of Medical Microbiologists

Abstract: The share of Klebsiella pneumoniae in infections has been recently increasing. Multidrug-resistant strains that produce more than one antibiotic resistance mechanism are also increasingly isolated. Contamination of the organs preservation fluid occurs quite often, but the isolated microorganisms are mainly saprophytic bacteria that are part of the skin microbiota (coagulase-negative Staphylococcus, Corynebacterium spp). The following case describes a K. pneumoniae blood infection in a patient after liver transplantation. Susceptibility of the strains to chosen antimicrobials was determined using the automated method. For strain isolated from blood, it was confirmed by loop-mediated isothermal amplification of genetic material.
Keywords: Klebsiella pneumoniae; Liver transplantation; RAPD; 16S rRNA

The Knoevenagel reaction is an essential synthetic tool in the organic and medicinal chemistry of thiazolidin-4-one derivatives. In the present work, the application of ethylenediamine diacetate (EDDA) as an effective catalyst for the interaction of 2-thioxothiazolidin-4-one with 4-(tert-butyl)cyclohexanone is proposed. The structure of novel synthesized 5-[4-(tert-butyl)cyclohexylidene]-2-thioxothiazolidin-4-one (yield 61%) was confirmed by1H-,13C-NMR, LC-MS, IR, and UV spectra. Drug-like properties of the synthesized compound were evaluated in silico using the SwissAdme, and their potential antimicrobial activity against 15 strains of Gram-positive and Gram-negative bacteria as well as yeasts was evaluated in vitro. The synthesized compound possesses satisfactory drug-like parameters and promising antimicrobial properties and presents interest as a prospective intermediate for the forthcoming design of biologically active small molecules. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

Author keywords

Antimicrobial activity; Catalyst; Ethylenediamine diacetate (EDDA); Knoevenagel reaction; Rhodanine