The 1,3,4-oxadiazole is an aromatic heterocycle valued for its low-lipophilicity in drug development. Substituents at the 2- and/or 5-positions can modulate the heterocycle's electronic and hydrogen bond-accepting capability, while exploiting its use as a carbonyl bioisostere. A new approach to 1,3,4-oxadiazoles is described wherein α-bromo nitroalkanes are coupled to acyl hydrazides to deliver...

Palladium-catalyzed desulfitative and denitrogenative arylation of azoles with arylsulfonyl hydrazides has been achieved. A broad scope of azoles and arylsulfonyl hydrazides has been used to produce arylated azoles in high yields.

ABSTRACT New dimethyl benzoylcarbonohydrazonodithioates were obtained by CS2 addition to arylcarboxylic acid hydrazides and methylation of the formed adduct. The new derivatives were tested for their activity against Mycobacterium tuberculosis. Some compounds exhibited high activity toward sensitive and resistant strains. GRAPHICAL ABSTRACT

A facile and efficient method for synthesis of fenamic acid hydrazides from their acids in one-step reaction under microwave irradiation and solvent-free conditions was developed. Compared with the two-step conventional heating method, the process was simple, the reaction time was very short and the yields were almost quantitative.

Naphthoquinones have been reported to possess a variety of pharmacological properties including antibacterial, antifungal, antiviral, anti-inflammatory, anti-artherosclerotic and anticancer effects. We have successfully synthesized a series of novel naphthoquinone acylhydrazides. The straightforward synthesis of these molecules involves a coupling reaction between 2,3-dichloro-1,4-naphthoquinon...

We report the synthesis of new phosphoramidite building blocks and their use for the modification of oligonucleotides with hydrazides. The reaction of these hydrazide oligonucleotides with active esters and aldehydes is demonstrated for solution conjugation and immobilization. Compared with the established amino modified oligonucleotides, hydrazides show enhanced reactivity at neutral and acidi...

The 1,3,4-oxadiazole is an aromatic heterocycle valued for its low-lipophilicity in drug development. Substituents at the 2and/or 5-positions can modulate the heterocycle's electronic and hydrogen bondaccepting capability, while exploiting its use as a carbonyl bioisostere. A new approach to 1,3,4oxadiazoles is described wherein a-bromo nitroalkanes are coupled to acyl hydrazides to deliver the...

Methyl 3-phenylpropanoate (1), after hydrazination into 3-phenylpropanehydrazide (2), was converted into N-arylidene-3-phenylpropane hydrazides (3a-e), which on cyclization with thioglycolic acid yielded N-(4-oxo-2-arylthiazolidin-3-yl)-3-phenylpropanamides (4a-e). All the proposed structures of newly synthesized compounds were in full agreement with the spectral data. Due to para substitution,...

A systematic investigation on the metal-free, Cope-type hydroamination reactivity of hydrazides and analogues is reported. Optimization of the hydrazide structure resulted in more facile intramolecular reactivity and enabled intermolecular reactions of alkenes, thus providing a direct approach to polysubstituted hydrazides.