Study of direction of cyclization of 1‐azolil‐4‐aryl/alkyl‐thiosemicarbazides

This study presents the synthesis and spectral analysis of new derivatives of 1,2,4-triazole-3-thione and 1,3,4-thiadiazole. New compounds were prepared by cyclization reaction of acyl thiosemicarbazide derivatives in the presence of alkaline and acidic media. All synthesized compounds were screened for their in vitro antibacterial activity by using the agar dilution technique. Six of the compounds had potential activity against Gram-positive bacteria (minimal inhibitory concentration [MIC] = 15.63–500 μg/mL). Some compounds showed good activity especially against Bacillus subtilis ATCC 6633 (MIC = 15.63–250 μg/mL), Staphylococcus aureus ATCC 25923 (MIC = 31.25–250 μg/mL), and Micrococcus luteus ATCC 10240 (MIC = 125–250 μg/mL).Graphical abstract

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“…It was proved that the direction of cyclization is dependent on the nature of substituents and acidic or alkaline media (Siwek et al ., 2010). …”

Section: Resultsmentioning

confidence: 99%

Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives

et al. 2012

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“…MS were recorded on a Bruker microTOF-Q II mass spectrometer (BioSpin, GmbH, Rheinstetten, Germany) using APCI method. The physicochemical characterization of compounds 5 – 7 , 9 , 10 were presented in [19,30,31].…”

Section: Methodsmentioning

confidence: 99%

Discovery of Potent and Selective Halogen-Substituted Imidazole-Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro via Structure-Based Design

et al. 2019

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Employing a simple synthetic protocol, a series of highly effective halogen-substituted imidazole-thiosemicarbazides with anti-Toxoplasma gondii effects against the RH tachyzoites, much better than sulfadiazine, were obtained (IC50s 10.30—113.45 µg/mL vs. ~2721.45 µg/mL). The most potent of them, 12, 13, and 15, blocked the in vitro proliferation of T. gondii more potently than trimethoprim (IC50 12.13 µg/mL), as well. The results of lipophilicity studies collectively suggest that logP would be a rate-limiting factor for the anti-Toxoplasma activity of this class of compounds.

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“…The ligand shows characteristic bands at 3294 and 3066 cm –1 due to ν(N–H) and at 2343 cm –1 due to ν(S–H). The absorption band at 1103 cm –1 should be assigned as ν(C=S) vibrations , , . These results suggest that the 1,2,4‐triazole ligand exhibits thione‐thiol tautomerism (Scheme ).…”

Section: Resultsmentioning

confidence: 88%

Metal(II) Ion Complexes with 5‐(Pyrazin‐2‐yl)‐2,4‐dihydro‐3H‐1,2,4‐triazole‐3‐thione; Synthesis, Structural Characterization, Acid‐base, and Complexing Properties in Solution

Kufelnicki

Jaciubek-Rosińska

Sobiesiak

et al. 2017

Zeitschrift anorg allge chemie

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The study reports the synthesis of complexes Co(HL)Cl 2 (1), Ni(HL)Cl 2 (2), Cu(HL)Cl 2 (3), and Zn(HL) 3 Cl 2 (4) with the title ligand, 5-(pyrazin-2-yl)-1,2,4-triazole-5-thione (HL), and their characterization by elemental analyses, ESI-MS (m/z), FT-IR and UV/Vis spectroscopy, as well as EPR in the case of the Cu II complex. The comparative analysis of IR spectra of the metal ion complexes with HL and HL alone indicated that the metal ions in 1, 2, and 3 are chelated by two nitrogen atoms, N(4) of pyrazine and N(5) of triazole in the thiol tautomeric form, whereas the Zn II ion in 4 is coordinated

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Study of direction of cyclization of 1‐azolil‐4‐aryl/alkyl‐thiosemicarbazides

Abstract: On a four series of 1-azolil-4-aryl/alkyl-

Cited by 20 publications

References 39 publications

Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives

Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives

Discovery of Potent and Selective Halogen-Substituted Imidazole-Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro via Structure-Based Design

Metal(II) Ion Complexes with 5‐(Pyrazin‐2‐yl)‐2,4‐dihydro‐3H‐1,2,4‐triazole‐3‐thione; Synthesis, Structural Characterization, Acid‐base, and Complexing Properties in Solution

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