New series of thiazole derivatives were synthesized using 5-(aryldiazo)salicylaldehyde thiosemicarbazones 2a–i. Cyclocondensation 2a–i with chloroacetone afforded the corresponding 4-methylthiazole 3a–i. Moreover, cycloalkylation ethyl bromoacetate thiazolidin-4-one 4a–i. The antimicrobial activity new was evaluated.

Herpes simplex and vaccinia viruses and adenovirus types 1, 2, 5, and 7 were tested by plaque suppression methods for sensitivity to halogenated deoxyuridines (5-iodo-, 5-bromo-, 5-chloro-, and 5-fluoro-), cytosine arabinoside, isatin-beta-thiosemicarbazone, and N-methylisatin-beta-thiosemicarbazone. After incubation for 12 days in HeLa cell cultures, vaccinia virus plaques were still readily s...

In this work, Pt(II) complexes of previously synthesized steroidal thiosemicarbazones were and characterized. The ligands their metal studied by analytical spectroscopic data (elemental analysis, IR, 1D-NMR 2D-NMR, HSQC, HMBC, NOESY, COSY), the analysis which enabled complete 1H 13C assignments each compound including E Z isomers. All screened for cytotoxic antimicrobial activity. results demon...

Thiosemicarbazones are Schiff based ligands which have gained importance over the decades as potential drug candidates. When coordinated to metals, they have proved as good anticancer, antimicrobial, antioxidant and antiprotozoal agents. Numerous applications of these ligands in the field of Analytical Chemistry have also been reported. The present review aims to summarize some of the recent ad...

Background Blocking of DNA synthesis through inhibition of ribonucleotide reductase has been proposed to be the main mechanism of anti-neoplastic action for a-N-heterocyclic thiosemicarbazones. Currently the best-studied agent of this class of compounds is triapine (3-amino-2-carboxaldehyde thiosemicarbazone), which has been tested in several phase I and II clinical trials. We synthesized triap...

A set of closely related furylidene thiosemicarbazones was prepared and screened against various clinically important Gram-positive bacteria. One compound containing an ethylene spacer and a 5-nitrofuryl group was found to have promising activity against Clostridium difficile.

We have recently identified a new class of compounds that selectively kill cells that express P-glycoprotein (P-gp, MDR1), the ATPase efflux pump that confers multidrug resistance on cancer cells. Several isatin-beta-thiosemicarbazones from our initial study have been validated and a range of analogues synthesized and tested. A number demonstrated improved MDR1-selective activity over the lead,...

Two novel thiosemicarbazones and eight novel 2-{[1-(5-alkyl/arylalkylpyrazin-2-yl)ethylidene]hydrazono}-1,3-thiazolidin-4-ones were prepared and tested against a panel of eight fungal strains-Candida albicans ATCC 44859, Candida tropicalis 156, Candida krusei E 28, Candida glabrata 20/I, Trichosporon asahii 1188, Aspergillus fumigatus 231, Lichtheimia corymbifera 272, and Trichophyton interdigi...

One of the most promising classes of iron chelators are α-N-heterocyclic thiosemicarbazones with Triapine as the most prominent representative. In several clinical trials Triapine showed anticancer activity against hematological diseases, however, studies on solid tumors failed due to widely unknown reasons. Some years ago, it was recognized that "terminal dimethylation" of thiosemicarbazones c...

We present an efficient procedure for the synthesis of thirty-six N₁,N₄-substituted thiosemicarbazones, including twenty-five ones that are reported for the first time, using a microwave-assisted methodology for the reaction of thiosemicarbazide intermediates with aldehydes in the presence of glacial acetic acid in ethanol and under solvent free conditions. Overall reaction times (20-40 min whe...