Combinatorial approach: identification of potential antifungals from triazole minilibraries

Bhatia, Manish S.; Zarekar, Bandu Eknath; Choudhari, Prafulla; Ingale, Kundan B.; Bhatia, Neela M.

doi:10.1007/s00044-009-9283-8

Cited by 8 publications

(6 citation statements)

References 7 publications

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“…Bhatia et al (2010) carried out the combinatorial synthesis of 1,2,4-triazole derivatives with good yield percentages, which were evaluated against F. oxysporum (NCIM-1008). Compound 79 presented the lowest MIC values (32 µg/mL) [ 111 ]. The established synthesis method uses 2-phenylacetohydrazide as a precursor, which reacts with carbon disulfide in a basic medium and subsequently with hydroxylamine, achieving the formation of the 1,3,4-triazole heterocyclic system.…”

Section: Synthetic Methods For Highly Active Compounds Against Fox Speciesmentioning

confidence: 99%

A Compendium of the Most Promising Synthesized Organic Compounds against Several Fusarium oxysporum Species: Synthesis, Antifungal Activity, and Perspectives

2021

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Vascular wilt caused by F. oxysporum (FOX) is one of the main limitations of producing several agricultural products worldwide, causing economic losses between 40% and 100%. Various methods have been developed to control this phytopathogen, such as the cultural, biological, and chemical controls, the latter being the most widely used in the agricultural sector. The treatment of this fungus through systemic fungicides, although practical, brings problems because the agrochemical agents used have shown mutagenic effects on the fungus, increasing the pathogen’s resistance. The design and the synthesis of novel synthetic antifungal agents used against FOX have been broadly studied in recent years. This review article presents a compendium of the synthetic methodologies during the last ten years as promissory, which can be used to afford novel and potential agrochemical agents. The revision is addressed from the structural core of the most active synthetic compounds against FOX. The synthetic methodologies implemented strategies based on cyclo condensation reactions, radical cyclization, electrocyclic closures, and carbon–carbon couplings by metal–organic catalysis. This revision contributes significantly to the organic chemistry, supplying novel alternatives for the use of more effective agrochemical agents against F. oxysporum.

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Section: Synthetic Methods For Highly Active Compounds Against Fox Speciesmentioning

confidence: 99%

A Compendium of the Most Promising Synthesized Organic Compounds against Several Fusarium oxysporum Species: Synthesis, Antifungal Activity, and Perspectives

2021

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“…The basic characteristic used for designing library is illustrated in Fig.- [18][19][20][21][22][23][24][25] .…”

Section: Methodsmentioning

confidence: 99%

"In-Silico Design, Synthesis and Pharmacological Evaluation of Pyrrolidine-2-Carbonitrile Derived Anti-Diabetic Agents"

2018

RJC

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The design, synthesis and biological activity studies of series of the novel cyanopyrrolidines type II anti-diabetic agents reported in this paper. Three Dimensional Quantitative Structural Activity , pharmacophore, docking studies used for rational design of molecules, studies revealed that novel substituted cyanopyrrolidines were a promising candidate for further studies. Molecules were synthesized and evaluated for their anti-diabetic activity by using high-fat diet and multiple low doses STZ induced type II diabetes rat model. Amongst all the synthesized compounds 1-(2-(5-methylisoxazol-3-ylamino) acetyl) pyrrolidine-2-carbonitrile, 1-(2-(5-methyl-1, 2, 4-oxadiazol-3-ylamino) acetyl) pyrrolidine-2-carbonitrile and 1-(2-(1,2,4-thiadiazol-5-ylamino)acetyl)pyrrolidine-2-carbonitrile were found to be potent anti-diabetic agents.

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“…The molecules which are utilized in present study are synthesized using the procedure from our previous published work 8,9 .…”

Section: Methodsmentioning

confidence: 99%

Design, synthesis and evaluation of 1, 2, 4-triazole derivatives as antifungal.

Choudhari¹,

Dhavale²,

Jadhav³

et al. 2012

JCPR

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A series of 1, 2, 4-triazoles was designed, synthesized and screened for antifungal activity against strain of Aspergillus niger. The design of the triazole compounds was based on docking studies performed on Lanosterol 14α-demethylase an important enzyme required for the synthesis of ergosterol. The three-dimensional QSAR studies of 1, 2, 4-triazole for analysis of the structural requirements for antifungal activity using Vlife MDS 3.5 has been carried out. The negative logarithm of activity (MICs) of the compounds against resistant Aspergillus niger exhibited a strong correlation with the selected 3D molecular descriptors of the triazole analogues. The present findings suggest that the triazole framework is an attractive template for optimization of targeted antifungal activity to achieve better potency and a wider spectrum of activity.

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Combinatorial approach: identification of potential antifungals from triazole minilibraries

Cited by 8 publications

References 7 publications

A Compendium of the Most Promising Synthesized Organic Compounds against Several Fusarium oxysporum Species: Synthesis, Antifungal Activity, and Perspectives

A Compendium of the Most Promising Synthesized Organic Compounds against Several Fusarium oxysporum Species: Synthesis, Antifungal Activity, and Perspectives

"In-Silico Design, Synthesis and Pharmacological Evaluation of Pyrrolidine-2-Carbonitrile Derived Anti-Diabetic Agents"

Design, synthesis and evaluation of 1, 2, 4-triazole derivatives as antifungal.

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