Azoles are generally fungistatic, and resistance to fluconazole is emerging in several fungal pathogens. In an attempt to find novel azole antifungal agents with improved activity, a series of tetrazole ring bearing acylhydrazone derivatives were synthesized and screened for their in vitro antifungal activity. The mechanism of their antifungal activity was assessed by studying their effect on t...

To explore the effect of the nature of substitutions on the structural parameters and hydrogen-bond inter-actions in N-acyl-hydrazone derivatives, the crystal structures of three ortho-substituted N-acyl-hydrazone derivatives, namely (E)-N-{2-[2-(2-chloro-benzyl-idene)hydrazin-yl]-2-oxoeth-yl}-4-methyl-benzene-sulfon-amide, C16H16ClN3O3S (I), (E)-N-{2-[2-(2-methyl-benzyl-idene)hydrazin-yl]-2-ox...

Cyclization-carbonylation of α,β-alkynic hydrazones and (o-alkynylphenyl) (methoxymethyl) sulfides with Pd(tfa)2 in DMSO/MeOH afforded methyl pyrazole-4-carboxylates and benzo[b]thiophene-3-carboxylates, respectively, in good yields. A simple change of the ligand (solvent) allowed controlled, effective switching between cyclization-carbonylation-cyclization-coupling (CCC-coupling) reactions and...

Oxidative transformations of the aldehydes, ketones, and their azomethine derivatives such as hydrazones, Schiff bases, azines, and oximes are presented and discussed. The oxidants used have been hydrogen peroxide in the presence of selenium compounds as catalysts, peroxycarboxylic acids, and eerie ammonium nitrate. Some of reported reactions have practical value in the synthesis of phenols, es...

A number of new substituted 1,2,4-triazole {[(1,2,4-triazolyl)ethyl]tetrazolyl} derivatives, their sugar hydrazones, and their acyclic C-nucleoside analogues were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). The synthesized compounds displayed different degrees...

A novel direct transformation of hydrazones to acyloxylated pyrazoles by copper-catalyzed regioselective olefinic C(sp(2))-H bond cycloamination and acyloxylation was performed under mild conditions, which combines the formation of the pyrazole skeleton and installation of an acyloxyl group in a single step, using facile carboxylic acids as the acyloxylation reagents.

2-Substituted azetidin-3-ones can be prepared in good yields and enantioselectivities (up to 85% ee) by a one-pot procedure involving the metalation of the SAMP/RAMP hydrazones of N-Boc-azetidin-3-one, reaction with a wide range of electrophiles, including alkyl, allyl, and benzyl halides and carbonyl compounds, followed by hydrolysis using oxalic acid.

New (tetrazol-5-yl)methylindole derivatives were synthesized from 2-phenylindole. Furthermore, the sugar acetyl hydrazones of the tetrazole derivatives as well as their derived acyclic C-nucleoside analogs were prepared. The synthesized compounds were studied for their anticancer activity against human liver carcinoma cell line (HepG2) and the results showed that arylidine substituted tetrazole...