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Relevant academic research and scientific papers

5-nitrofuran-2-yl thiohydrazones as double antibacterial agents synthesis and in vitro evaluation

Background: Applying of "double-drug" strategy to 5-nitrofuran derivatives has been proposed. Methods: A small library of 5-Nitrofuran-2-yl Thiohydrazones was developed, and initial screening demonstrated good activity against bacteria and fungi of ESKAPE panel. Conclusion: The synthesis of the desired thiohydrazones was carried out via condensation of 5-nitrofuran-2-carbaldehyde with thiohydrazides of substituted oxamic acids.

Novel steroidal 1,3,4-thiadiazines: Synthesis and biological evaluation in androgen receptor-positive prostate cancer 22Rv1 cells

A flexible approach to previously unknown spirofused and linked 1,3,4-thiadiazine derivatives of steroids with selective control of heterocyclization patterns is disclosed. (N-Arylcarbamoyl)spiroandrostene-17,6′ [1,3,4]thiadiazines and (N-arylcarbamoyl)17-[1′,3′,4′]thiadiazine-substituted androstenes, novel types of heterosteroids, were prepared from 16β,17β-epoxypregnenolone and 21-bromopregna-5,16-dien-20-one in good to high yields by the treatment with oxamic acid thiohydrazides. The synthesized compounds were screened for antiproliferative activity against the human androgen receptor-positive prostate cancer cell line 22Rv1. Most of (N-arylcarbamoyl)17-[1′,3′,4′]thiadiazine-substituted androstenes exhibit better antiproliferative potency (IC50 = 2.1–6.6 μM) than the antiandrogen bicalutamide. Compounds 7d with IC50 = 3.0 μM and 7j with IC50 = 2.1 μM proved to be the most active in the series under study. Lead synthesized compound 7j downregulates AR expression and activity in 22Rv1 cells. NF-κB activity is also blocked in 7j-treated 22Rv1 cells. Apoptosis is considered as a possible mechanism of 7j-induced cell death.

Hydrazones derived from thiooxamohydrazides and 3-formyl-4-hydroxycoumarin: Synthesis, structures, and fragmentation

Novel hydrazones were obtained from thiooxamohydrazides and 3-3-formyl-4-hydroxycoumarin. According to data from NMR spectroscopy and X-ray diffraction, the coumarin fragment in the compounds obtained exists as 4-hydroxycoumarin or chromane-2,4-dione. When dissolved in dimethyl sulfoxide, these hydrazones undergo fragmentation into derivatives of 1,3,4-thiadiazole and 4-hydroxycoumarin.

Synthesis of oxamic acids thiohydrazides and carbamoyl-1,3,4-thiadiazoles

A convenient preparation method was developed for oxamic acids thiohydrazides by reaction of α-chloroacetamides with a preliminary prepared solution of elemental sulfur and hydrazines. A series of carbamoyl-1,3,4-thiadiazole derivatives was obtained.