There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

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Biological activities of hydrazone derivatives.

Metal based biologically active compounds: design, synthesis, and antibacterial/antifungal/cytotoxic properties of triazole-derived Schiff bases and their oxovanadium(IV) complexes

Synthesis and characterization of novel hydrazide-hydrazones and the study of their structure-antituberculosis activity.

A series of 2,5-disubstituted-1,3,4-thiadiazoles were synthesized, the compounds structures were elucidated and screened for the antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the tested compounds, 2-phenylamino-5-(4-fluorophenyl)-1,3,4-thiadiazole 22 showed the highest inhibitory activity. The relationships between the structures of compounds and their antituberculosis activity were investigated by the Electronic-Topological Method (ETM) and feed forward neural networks (FFNNs) trained with the back-propagation algorithm. As a result of the approach, a system of pharmacophores and anti-pharmacophores has been found that effectively separates compounds of the examination set into groups of active and inactive compounds. The system can be applied to the screening and design of new active compounds possessing skeletons similar to those used in the present study.

1,3,4-thiadiazole derivatives. Synthesis, structure elucidation, and structure-antituberculosis activity relationship investigation.

Synthesis and biological activities of diflunisal hydrazide–hydrazones

A series of hydrazide hydrazones and 1,3,4-oxadiazolines of 4-fluorobenzoic acid hydrazide were prepared and evaluated as potential antimicrobial agents and were tested for their antibacterial and antifungal activities against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. From these compounds, 4-fluorobenzoic acid[(5-nitro-2-furanyl)methylene]hydrazide (1a) showed equal activity with ceftriaxone against S. aureus. In addition, the MIC values of compounds 1c, 1d and 2a for the same strain were in the range of those reported for ceftriaxone according to NCCLS 1997.

Synthesis and antimicrobial activity of some new hydrazones of 4-fluorobenzoic acid hydrazide and 3-acetyl-2,5-disubstituted-1,3,4-oxadiazolines

5-(4-Pyridinyl)-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones and 5-(4-pyridinyl)-4-substituted-3-(benzoylmethyl)thio-4H-1,2,4-triazoles were synthesized. The structures of original nine compounds were confirmed by IR, 1H NMR, mass spectral methods and elemental analysis. The antibacterial, antifungal and antimycobacterial activities, together with those of known intermediate 1,4-disubstituted thiosemicarbazides, were reported.

Synthesis and structure elucidation of some new thioether derivatives of 1,2,4-triazoline-3-thiones and their antimicrobial activities

Some new 1-(4-fluorobenzoyl)-4-alkyl/arylthiosemicarbazide (2a-g), 5-(4-fluorophenyl)4-alkyl/aryl-2,4-dihydr-3H-1,2,4-triazole-3-thio ne (3a-g) derivatives, 3-(benzylthio)-5-(4-fluorophenyl)-4-phenyl-4H-1,2,4-triazole (3h) and 2-acetyl-5-(4-fluorophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thi one (3i) were prepared and tested for their antimycobacterial and anticonvulsant activities. The structure of compounds was confirmed by elemental analyses and spectroscopic techniques. The antimycobacterial activity of the synthesized compounds was investigated against M. fortiutum ATCC 6841 and most of them were found active against the above strain with MIC values of 64 or 32 micrograms/ml. The anticonvulsant activity of the 2d, 3d-i was determined against pentylenetetrazole induced seizures. 3f-i showed anticonvulsant activity (10 to 30% protection).

Evaluation of antimycobacterial and anticonvulsant activities of new 1-(4-fluorobenzoyl)-4-substituted-thiosemicarbazide and 5-(4-fluorophenyl)-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thione derivatives.

Synthesis and Antimicrobial Activity of Some New Hydrazones of 4‐Fluorobenzoic Acid Hydrazide and 3‐Acetyl‐2,5‐disubstituted‐1,3,4‐oxadiazolines.

Although most triazoline-3-thione derivatives (cyclic thiosemicarbazides) are important compounds possessing some biological and pharmacological activities, no literature was found showing their metabolic reactions with hepatic microsomal preparations. We, therefore, planned to study the in vitro microsomal metabolism of a prototype, 4-ethyl-5-(4-fluorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (A). The substrate (A) and its potential metabolites i.e. the corresponding dealkylation (A1), desulphuration (A2) and S-oxidation (A3) products were synthesized and characterized by spectral methods. The substrate and its potential metabolites were separated by a reverse phase HPLC. A was incubated with rat microsomal preparations fortified with NADPH and extracted into DCM; concentrated under a stream of N2 at 20 degrees C and analyzed by HPLC. The results indicated that A was metabolically inert and failed to produce the corresponding desulphuration (triazole-3-one) and S-oxidation (sulphenic acid) metabolites which would lead to pharmacological and toxicological alterations compared to the parent molecule. However, a small amount of dealkylated product (A1) was observed as a metabolite together with two unidentified metabolites.

Nehir Gulerman

Papers

Synthesis and antimicrobial activity of some new hydrazones of 4-fluorobenzoic acid hydrazide and 3-acetyl-2,5-disubstituted-1,3,4-oxadiazolines

Synthesis and structure elucidation of some new thioether derivatives of 1,2,4-triazoline-3-thiones and their antimicrobial activities

Evaluation of antimycobacterial and anticonvulsant activities of new 1-(4-fluorobenzoyl)-4-substituted-thiosemicarbazide and 5-(4-fluorophenyl)-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thione derivatives.

Synthesis and Antimicrobial Activity of Some New Hydrazones of 4‐Fluorobenzoic Acid Hydrazide and 3‐Acetyl‐2,5‐disubstituted‐1,3,4‐oxadiazolines.

Synthesis and in vitro microsomal metabolism of 4-ethyl-5-(4-fluorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione and its potential metabolites.