Synthesis and Antimicrobial Properties of New Thiosemicarbazide, 1,2,4-Triazole, and 1,3,4-Thiadiazole Derivatives of Sulfanylacetic Acid

Popiołek, Łukasz; Kosikowska, Urszula; Dobosz, Maria; Malm, Anna

doi:10.1080/10426507.2011.625511

Cited by 17 publications

(8 citation statements)

References 14 publications

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“…The bioassay of antibacterial and antifungal activities of 245a-i revealed that they have better antifungal than antibacterial activities; also, compounds 245b,c,f,j,k,l showed excellent antifungal activity against Candida albicans with an MIC of 16 μg/mL [93]. [96]. The screening of the antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method revealed that the corresponding hydrazinecarbothioamides showed excellent antioxidant activity, while 1,2,4-triazole-3-thiones showed good antioxidant activity (Scheme 71) [96].…”

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

“…[96]. The screening of the antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method revealed that the corresponding hydrazinecarbothioamides showed excellent antioxidant activity, while 1,2,4-triazole-3-thiones showed good antioxidant activity (Scheme 71) [96]. [96].…”

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

“…The screening of the antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method revealed that the corresponding hydrazinecarbothioamides showed excellent antioxidant activity, while 1,2,4-triazole-3-thiones showed good antioxidant activity (Scheme 71) [96]. [96]. The screening of the antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method revealed that the corresponding hydrazinecarbothioamides showed excellent antioxidant activity, while 1,2,4-triazole-3-thiones showed good antioxidant activity (Scheme 71) [96].…”

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

“…Reaction of 3,4-disubstituted triazolethioles 66a-c with 2-bromoacetophenones gave ((3,4disubstituted-1,2,4-triazole-3-yl)thio)-1-phenyl-ethanones 254a-c in 70-82% yields and ((3,4disubstituted-1,2,4-triazole-3-yl)thio)-1-(4-fluorophenyl)ethanones 255a-c in 72-85% yields [96]. The screening of the antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method revealed that the corresponding hydrazinecarbothioamides showed excellent antioxidant activity, while 1,2,4-triazole-3-thiones showed good antioxidant activity (Scheme 71) [96]. Condensation of 5-chloro-1-phenyl-3-(substituted)-1H-pyrazole-4-carbaldehyde with aminotriazolethiones 11d,e furnished the corresponding Schiff bases 246a,b.…”

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

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Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

et al. 2020

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Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.

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Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

Section: Synthesis Of Spiro-124-triazolethionesmentioning

confidence: 99%

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Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

et al. 2020

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“…Previous studies have shown that the examined compounds show antibacterial activity 13,14 . The inhibitory activities against Grampositive bacteria on the basis of minimal inhibitory concentration (MIC, µg/mL) values showing the following compounds: 6,7,8,9,10 and 16,18 13,14 . …”

Section: Introductionmentioning

confidence: 99%

Determination of lipophilicity of some new 1,2,4-triazole derivatives by RP-HPLC and RP-TLC and calculated methods

Hawrył

Świeboda²,

Gawroński³

et al. 2015

10.5267/j.ccl

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Experimental and computational approaches were used to estimate the lipophilicity of novel 1,2,4-triazole derivatives. These derivatives have been subjected to this research, because they exhibit antimicrobial activity. The chromatographic analysis of RP-HPLC and RP-TLC was carried out using methanol-water or acetonitrile-water as mobile phase. The linear relationships between (or ) values and the concentration of organic modifier were obtained. The lipophilicity was expressed as chromatographically derived descriptors:, , ϕ0 and scores and corresponding to the first principal component. The experimental lipophilicity data have been compared with the computer calculated lipophilicity parameters ( ,ℎ ) of the same molecules. The matrices were created with or 0 and logP and they have been the subject of PCA analysis.

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Antiproliferative Activity and Ultrastructural Changes in Promastigote and Amastigote forms of Leishmania amazonensis Caused by Limonene‐Acylthiosemicarbazide Hybrids

Contato

Kaplum

Scariot

et al. 2023

Chemistry & Biodiversity

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Leishmaniasis is a tropical zoonotic disease. It is found in 98 countries, with an estimated 1.3 million people being affected annually. During the life cycle, the Leishmania parasite alternates between promastigote and amastigote forms. The first line treatment for leishmaniasis are the pentavalent antimonials, such as N-methylglucamine antimoniate (Glucantime®) and sodium stibogluconate (Pentostam®). These drugs are commonly related to be associated with dangerous side effects such as cardiotoxicity, nephrotoxicity, hepatotoxicity, and pancreatitis. Considering these aspects, this work aimed to obtain a new series of limonene-acylthiosemicarbazides hybrids as an alternative for the treatment of leishmaniasis. For this, promastigotes, axenic amastigotes, and intracellular amasti-gotes of Leishmania amazonensis were used in the antiproliferative assay; J774-A1 macrophages for the cytotoxicity assay; and electron microscopy techniques were performed to analyze the morphology and ultrastructure of parasites. ATZÀ S-04 compound showed the best result in both tests. Its IC 50 , in promastigotes, axenic amastigotes and intracellular amastigotes was 0.35 � 0.08 μM, 0.49 � 0.06 μM, and 15.90 � 2.88 μM, respectively. Cytotoxicity assay determined a CC 50 of 16.10 � 1.76 μM for the same compound. By electron microscopy, it was observed that ATZÀ S-04 affected mainly the Golgi complex, in addition to morphological changes in promastigote forms of L. amazonensis.

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Synthesis and Antimicrobial Properties of New Thiosemicarbazide, 1,2,4-Triazole, and 1,3,4-Thiadiazole Derivatives of Sulfanylacetic Acid

Cited by 17 publications

References 14 publications

Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Determination of lipophilicity of some new 1,2,4-triazole derivatives by RP-HPLC and RP-TLC and calculated methods

Antiproliferative Activity and Ultrastructural Changes in Promastigote and Amastigote forms of Leishmania amazonensis Caused by Limonene‐Acylthiosemicarbazide Hybrids

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