Organic and Medicinal Chemistry Letters ..

Synthesis of 6-Aryl-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazine-3-thione derivatives (IIa-b)

Reaction of tartaric acid with thiocarbohydrazide (2) ..

The synthesized derivatives were evaluated for their antimycobacterial activity against Mycobacterium bovis BCG and the MIC values have been listed in . As evident from the MIC values, the triazole derivatives Ia-f exhibited moderate activities and among them compound Ib (R = CH3) was the most potent derivative with IC50 value of 31.25 µg/mL. While the triazolopyridazine derivative IIa showed a moderate activity (MIC = 62.5 µg/mL), the p-chloro substituted compound IIb was found to be inactive. Amongst the compounds IIIa-e, Schiff bases of 2-pyridinecarboxaldehyde (3a) and cinnamaldehyde (3e) exhibited the highest activity in the series with MIC value of 62.5 µg/mL.

We have described herein the synthesis of 12 hybrid 1,2,4-triazole Schiff bases ..

Journal of Chemistry is a peer ..

A novel series of Schiff base was successfully synthesized and tested for antifungal activity against three fungal strains and antibacterial activity against two bacterial strains. The results of the biological studies revealed that among the three fungal strains, M. gypseum was found to be more sensitive to the studied 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol. In fact, six (5b, 5c, 5d, 5e, 5m, 5n) among the 17 compounds tested were more effective than the clinical candidate ketoconazole. M. gypseum is a type of fungi which causes dermatomycoses, a type of infection difficult to treat, hence, the studied compounds, specifically, (5b, 5c, 5d, 5e, 5 m, 5n) could be promising lead molecules for development of more potent and safer antifungal drugs for the treatment of dermatomycoses.

ADA581104. Title : Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties. Descriptive Note : Journal article

Equimolar amounts of thiocarbohydrazide and appropriate carboxylic acids (10 mmol of each) were mixed and heated at 165-170 °C for 30 min. Boiling water (20 mL) was added to the solid and the mixture was kept at room temperature for 24 h. The precipitate was filtered and recrystallized from ethanol to afford the title compounds.

03/02/2017 · A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity.


Synthesis and Biological Activity of Substituted ..

Reagents, starting materials and solvents were purchased from common commercial suppliers. The melting points of synthesized compounds were determined by an open capillary method on a Veego digital melting point apparatus. Mass spectral analysis was carried out using Applied Biosystem QTRAP 3200 MS/MS system in ESI mode. The infra-red spectra of the synthesized compounds were recorded on Fourier transformer infra-red spectrophotometer Model Schimadzu 8400S using potassium bromide pellets. 1H NMR spectra were recorded on the Bruker NMR using DMSO-d6, tetramethylsilane as an internal standard.

04/03/2017 · The 1,2,4-triazole and 1,2 ..

The synthesis of 4-amino-5-phenyl-4H-1,2,4-triazole-3-thiol(3a-3c) was carried out from benzoic acid derivatives (1) and thiocarbohydrazide (2) as per the literature.[] Intermediate compound (3) was treated with substituted aromatic aldehydes (4) in the presence of concentrated H2SO4, and yielded Schiff bases (5) The structures of the synthesized compounds were confirmed by NMR, IR, Mass and elemental analysis [Schemes and ].

AND BIOLOGICAL EVALUATION OF TRIAZOLE AND FUSED ..

A series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. The 4-amino-1,2,4-triazole-5-thione analogues (Ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. Reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivatives IIa-b. Finally, condensation of 4-amino-1,2,4-triazole-5-thione with some aldehydes gave Schiff bases IIIa-e. After characterization by different spectroscopic and analytical methods, the derivatives were tested for their inhibitory activity against Mycobacterium bovis BCG. Among the derivatives, compound Ib proved to be the most potent derivatives with MIC value of 31.25 µg/mL. Given the fact that 4-amino-1,2,4-triazole-5-thiones Ia-f were the most active derivatives, it could be suggested that this group of derivatives have the potential to be considered as lead compounds for future optimization efforts.

3-acetic acid with thiocarbohydrazide gave the 4-amino- …

A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistance, new agents should preferably have chemical characteristics that clearly differ from those of existing agents. Thus led to the design and synthesize the new antimicrobial agents. A novel series of Schiff bases based on of 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol scaffold was prepared by heating thiocarbohydrazide and substituted benzoic acid and subsequently, treating with substituted benzaldehydes. Seventeen derivatives were synthesized and were biologically screened for antifungal and antibacterial activity. The newly synthesized derivatives of triazole showed antifungal activity against fungal species, Microsporum gypseum; and antibacterial activity against bacterial species, Staphylococcus aureus. It was observed that none of the compounds tested showed positive results for fungi Candida albicans fungi Aspergillus niger, nor against bacterial strain Escherichia coli. Strong antifungal effects were obtained for the synthesized compounds against M. gypseum and were superior or comparable to standard drug ketoconazole. Similarly, all of the synthesized compounds exhibit strong antibacterial activity against S. aureus and were superior or comparable to standard drug streptomycin. It was found that among the triazole derivatives so synthesized, six of them, showed antifungal activity superior to ketoconazole while one of them, showed antibacterial activity superior to streptomycin. Thus, these can be the potential new molecule as an antimicrobial agent.