Design and synthesis of novel 4-hydrazone functionalized/1,2,4-triazole fused pyrido[2,3-d]pyrimidine derivatives, their evaluation for antifungal activity and docking studies

Appna, Nooka Ratnam; Nagiri, Ravi Kumar; Korupolu, Raghu Babu; Kanugala, Sirisha; Chityal, Ganesh Kumar; Ganapathi, Thipparapu; Narsaiah, B.

doi:10.1007/s00044-019-02390-w

Cited by 19 publications

(15 citation statements)

References 46 publications

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“…Appna et al [ 126 ] described the fungicidal activity of novel 1,2,4-triazole fused pyrido [2,3-d] pyrimidine derivatives (53a-d and 54a-c) against different Candida strains. The antifungal activities of the synthesized compounds 53d, 54b, and 54c were shown.…”

Section: 124 Triazole Scaffold For the Development Of Antifungal Agentsmentioning

confidence: 99%

Novel 1, 2, 4-Triazoles as Antifungal Agents

Kazeminejad

Marzi

Shiroudi

et al. 2022

BioMed Research International

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The development of innovative antifungal agents is essential. Some fungicidal agents are no longer effective due to resistance development, various side effects, and high toxicity. Therefore, the synthesis and development of some new antifungal agents are necessary. 1,2,4-Triazole is one of the most essential pharmacophore systems between five-membered heterocycles. The structure-activity relationship (SAR) of this nitrogen-containing heterocyclic compound showed potential antifungal activity. The 1,2,4-triazole core is present as the nucleus in a variety of antifungal drug categories. The most potent and broad activity of triazoles have confirmed them as pharmacologically significant moieties. The goal of this review is to highlight recent developments in the synthesis and SAR study of 1,2,4-triazole as a potential fungicidal compound. In this study, we provide the results of a biological activity evaluation using various structures and figures. Literature investigation showed that 1, 2, 4-triazole derivatives reveal the extensive span of antifungal activity. This review will assist researchers in the development of new potential antifungal drug candidates with high effectiveness and selectivity.

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Section: 124 Triazole Scaffold For the Development Of Antifungal Agentsmentioning

confidence: 99%

Novel 1, 2, 4-Triazoles as Antifungal Agents

Kazeminejad

Marzi

Shiroudi

et al. 2022

BioMed Research International

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“…El-Borai et al [ 74 ] reported that compound 5-(4-chlorobenzoyl)-1-phenyl-3-(pyridin-3-yl)-1 H -pyrazolo[3,4-b]pyridin-6(7 H )-one 171 exhibited strong activity against E. coli , E. cloaca , and Serratia. Appna et al [ 75 ] synthesized pyrido[2,3-d]pyrimidines 173a – 173c in four steps from ethyl 2-amino-6-(trifluoromethyl) nicotinate 172 ( Scheme 38 ). All compounds exhibited significant antifungal activities against tested strains, C. albicans , C. parapsilosis , C. glabrata , C. krusei , and Issatchenkia hanoiensis.…”

Section: Synthesis Of Fused Pyridines With Other Heterocycles With An...mentioning

confidence: 99%

Pyridine Compounds with Antimicrobial and Antiviral Activities

Marinescu

Popa

2022

IJMS

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In the context of the new life-threatening COVID-19 pandemic caused by the SARS-CoV-2 virus, finding new antiviral and antimicrobial compounds is a priority in current research. Pyridine is a privileged nucleus among heterocycles; its compounds have been noted for their therapeutic properties, such as antimicrobial, antiviral, antitumor, analgesic, anticonvulsant, anti-inflammatory, antioxidant, anti-Alzheimer’s, anti-ulcer or antidiabetic. It is known that a pyridine compound, which also contains a heterocycle, has improved therapeutic properties. The singular presence of the pyridine nucleus, or its one together with one or more heterocycles, as well as a simple hydrocarbon linker, or grafted with organic groups, gives the key molecule a certain geometry, which determines an interaction with a specific protein, and defines the antimicrobial and antiviral selectivity for the target molecule. Moreover, an important role of pyridine in medicinal chemistry is to improve water solubility due to its poor basicity. In this article, we aim to review the methods of synthesis of pyridine compounds, their antimicrobial and antiviral activities, the correlation of pharmaceutical properties with various groups present in molecules as well as the binding mode from Molecular Docking Studies.

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“…The biological actions of 1,2 and 4 the triazoles and their fused heterocyclic derivatives are diverse. The 1,2 and 4 the triazole core has been used in the enormous range of medically relevant medicines, including antibacterial, antifungal, antiviral, and anticancer drugs (Karaca et al,2017;Appna et al,2019;Rode et al,2017;Peng et al, 2021;Li et al,2020). In vitro growth inhibitory activity of newly formed 1,2,4-triazole compounds was evaluated against conventional Gram ve+ and Gram ve-microbial strains.…”

Section: Introductionmentioning

confidence: 99%

In vitro evaluation of novel designed, and synthesized naproxen derivatives bearing 1,2,4 triazole moiety

Hafedh

Naser

Hussein

2022

ijhs

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The Objective of this study is created a novel derivative of the naproxen with the heterocyclic (1,2 and 4 the triazole) ring that reacted with benzoyl chloride derivatives, as well as preliminary antibacterial activity testing of the formed products. The derivatives are synthesized by esterifying naproxen hydrazine hydrate, then reacting with hydrated hydrazine and carbon disulfide, and finally reaction the benzoyl chloride derivatives (in the final step) with the triazole the derivatives of the naproxen including of amino group via a nucleophilic substitution reaction. In addition to naproxen, the antibacterial properties of the novel compounds (Va-Vd) were evaluated in agar at known doses (IN vivo). The antibacterial action of the compounds Va and Vd against staph was demonstrated in the topmost inhibited zone. In the case of E. coli, compound Vb has the smallest inhibitory zone. The findings of this study have implications to produce naproxen 1,2 and 4 the triazole-three-thiol derivatives, which reacted including the variety of benzoyl chloride derivatives. The potential of naproxen will be affected by the attraction of benzoyl chloride derivatives with para-groups on the benzen ring.

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Design and synthesis of novel 4-hydrazone functionalized/1,2,4-triazole fused pyrido[2,3-d]pyrimidine derivatives, their evaluation for antifungal activity and docking studies

Cited by 19 publications

References 46 publications

Novel 1, 2, 4-Triazoles as Antifungal Agents

Novel 1, 2, 4-Triazoles as Antifungal Agents

Pyridine Compounds with Antimicrobial and Antiviral Activities

In vitro evaluation of novel designed, and synthesized naproxen derivatives bearing 1,2,4 triazole moiety

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