New dimensions in triazolo[4,3-a]pyrazine derivatives: The land of opportunity in organic and medicinal chemistry

Jethava, Divya J.; Borad, Mayuri A.; Bhoi, Manoj N.; Acharya, Prachi T.; Bhavsar, Zeel A.; Patel, Hitesh

doi:10.1016/j.arabjc.2020.09.038

Cited by 9 publications

(2 citation statements)

References 79 publications

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“…Triazolo [4,3-a]pyrazine is a privileged building block/scaffold used for the synthesis of biologically active molecules and has received significant attention in the field of synthetic organic chemistry. Triazolo [4,3-a]pyrazine derivatives have a wide range of biological activities, such as antidiabetic [19], anti-platelet aggregations [20], anti-fungal [21], anti-bacterial [22], anti-malarial [23], anti-tubercular [24], and anticonvulsant properties [25], which are important in drug discovery programs. 3-(Trifluoromethyl)-1,2,4-triazolo [4,3-a]pyrazine is the key pharmacophore of sitagliptin phosphate, a new drug for the treatment of type II-diabetes mellitus.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives

Hu,

Dong,

et al. 2023

Molecules

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Infectious diseases pose a major challenge to human health, and there is an urgent need to develop new antimicrobial agents with excellent antibacterial activity. A series of novel triazolo[4,3-a]pyrazine derivatives were synthesized and their structures were characterized using various techniques, such as melting point, 1H and 13C nuclear magnetic resonance spectroscopy, mass spectrometry, and elemental analysis. All the synthesized compounds were evaluated for in vitro antibacterial activity using the microbroth dilution method. Among all the tested compounds, some showed moderate to good antibacterial activities against both Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli strains. In particular, compound 2e exhibited superior antibacterial activities (MICs: 32 μg/mL against Staphylococcus aureus and 16 μg/mL against Escherichia coli), which was comparable to the first-line antibacterial agent ampicillin. In addition, the structure–activity relationship of the triazolo[4,3-a]pyrazine derivatives was preliminarily investigated.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives

Hu,

Dong,

et al. 2023

Molecules

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“…For example, ribavirin is an N-heterocyclic molecule that is used in the treatment of COVID-19 [39]. The reasonable results obtained from bioactivity studies have enabled them to be a family that is frequently used in pharmaceutical chemistry [40]. NHCs, which are known for their high catalytic activity, are easily synthesized and modified [41,42].…”

Section: Introductionmentioning

confidence: 99%

Novel N-Heterocyclic Carbene Silver (I) Complexes: Synthesis, Structural Characterization, Antimicrobial, Antioxidant and Cytotoxicity Potential Studies

Slimani¹,

Dridi²,

Özdemır³

et al. 2022

Carbene

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Nowadays, N-heterocyclic carbene-based silver-complexes Ag(I) have been widely used as an organometallic drug candidate in medicinal and pharmaceutical chemistry researches due to their low toxicity. Due to the success of Ag(I) complexes in biological applications, interest in the synthesis and applications of such compounds is increasing rapidly. Therefore, in this study, a series of unsymmetrical N,N-disubstituted benzimidazolium salts were synthesized as N-heterocyclic carbene (NHC) (2a-2j). The interaction of these benzimidazolium salts having their two nitrogen atoms substituted by bulky groups with Ag2O in DMF has been carried out to afford Ag(I) complexes and characterized by 1H NMR, 13C NMR, FT-IR and elemental analyses. The antimicrobial activity of Ag(I) complexes was tested against some standard culture collections of Gram-negative, Gram-positive bacterial strains and Fungal strains, which are the most frequently isolated among the society and hospital-acquired infectious microorganisms as potential metallopharmaceutical agents. The Ag-NHC complexes showed effective antimicrobial activity against microorganisms with MIC values between 0.0024 and 1.25 mg/ml. Moreover, these Ag-NHC complexes exhibited significant antioxidant activities. In addition, of benzimidazoles salts 2,4 and Ag(I) complexes 3,5 were screened for their antitumor activity. The highest antitumor activity was observed for 3e and 3d Complexes.

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The literature of heterocyclic chemistry, Part XX, 2020

Беленький¹,

Газиева²,

Evdokimenkova³

et al. 2023

Advances in Heterocyclic Chemistry

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New dimensions in triazolo[4,3-a]pyrazine derivatives: The land of opportunity in organic and medicinal chemistry

Cited by 9 publications

References 79 publications

Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives

Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives

Novel N-Heterocyclic Carbene Silver (I) Complexes: Synthesis, Structural Characterization, Antimicrobial, Antioxidant and Cytotoxicity Potential Studies

The literature of heterocyclic chemistry, Part XX, 2020

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