Synthesis and evaluation of biological activity of 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones
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
Vibrio metschnikovii: Current state of knowledge and discussion of recently identified clinical case
Vibrio metschnikovii is a widespread opportunistic pathogen that rarely causes disease in human. It caused graft infection in our case. It is important to differentiate it from another water-transmitted pathogens.
Keywords: Vibrio metschnikovii; case report; graft infection; rare pathogen; vascular surgery.
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
Keywords: Klebsiella pneumoniae; Liver transplantation; RAPD; 16S rRNA