Synthesis of novel thiazolyl-phenyl-thiazole derivatives as promising anti-Candida agents

New imine derivatives, that contain the thiazolyl-phenyl-thiazole scaffold, were synthesized and evaluated as anti-Candida agents. Elemental analysis and FT-IR, MS, [1]H-NMR and [13]C-NMR spectroscopic methods confirmed the structure of the newly synthesized compounds. The in vitro antifungal activity was investigated using the broth microdilution method against different Candida spp, including C. albicans, C. krusei and C. parapsilosis. All synthesized compounds exhibited good antifungal activity. Compound 4f showed the highest inhibitory effect against all tested Candida strains, being more potent than fluconazole. The results revealed that the new compounds have promising antifungal activity, with MIC values, ranging from 3.9 to 31.25Mug/mL and MFC values between 7.81 and 62.5 Mug/mL and could be considered for further development as anti-Candida agents

Biological evaluation and molecular docking of some chromenyl derivatives as potential antimicrobial agents

Various thiosemicarbazones [TSCs] and their heterocyclic thiadiazolines [TDZ] possess important biological effects. In addition, chromenyl derivatives exhibit a wide range of pharmacological activities. Based on these findings and as a continuation of our research on nitrogen and sulfur containing compounds, we investigated a series of previously reported chromenyl-TSCs [1a-j] and chromenyl-TDZs [2a-j] for their in vitro antimicrobial activities against two bacterial and four fungal strains. MIC and MBC/MFC [microg/mL] values of these compounds were evaluated and compared to those of Spectinomycin, Moxifloxacin and Fluconazole, used as reference drugs. For a better understanding of the drug-receptor interactions, all the compounds were further subjected to molecular docking against four targets that were chosen based on the specific mechanism of action of the reference drugs used in the antimicrobial screening. All compounds tested showed equal or higher antibacterial/antifungal activities relative to the used reference drugs. In silico studies [molecular docking] revealed that all the investigated compounds showed good binding energies towards four receptor protein targets and supported their antimicrobial properties