Synthesis and Antimicrobal Activities of some Novel Triazolo[1,5-a]Pyrimidine Derivatives

Gami, Sagar P.; Vilapara, Kalpesh V.; Khunt, Hasmukh R.; Babariya, Jayesh S.; Naliapara, Yogesh T.

doi:10.18052/www.scipress.com/ilcpa.30.127

Cited by 9 publications

(4 citation statements)

References 11 publications

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“…Currently, there are many methods available to synthesize triazolo[1,5-a]pyrimidines, mainly they are cyclocondensations between 3-amino-1,2,4-triazoles and 1,3-bifunctional synthons such as 1,3-dicarbonyl compounds or their equivalents [52][53][54][55][56][57][58][59], vinylogous iminium salts [47,60,61], ketene dithioacetals [48,62,63], and 3-ketovinyl compounds [46]. We used -acetylenic Ketones of types A as 1,3-bifunctional synthons.…”

Section: Methodsmentioning

confidence: 99%

Similarity-based Virtual Screening to Find Antituberculosis Agents based on Novel Scaffolds

García-García¹,

Julián-Ortiz²,

Gálvez³

et al. 2022

Preprint

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A method is developed to identify molecular scaffolds potentially active against the Mycobacterium tuberculosis complex (MTBC). A structurally heterogeneous set of compounds active against MTBC was used to obtain a structural pattern model based on structural invariants. This model was statistically validated through a Leave-n-Out test. It successfully discriminated between active or inactive compounds over 86% in database sets and was also able to select new active chemical structures in external databases. The selection of new substituted pyrimidines, pyrimidones and triazolo[1,5-a]pyrimidines was particularly interesting because these structures could provide new scaffolds in this field. The seven selected candidates were synthesized and six of them showed activity in vitro.

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Section: Methodsmentioning

confidence: 99%

Similarity-based Virtual Screening to Find Antituberculosis Agents based on Novel Scaffolds

García-García¹,

Julián-Ortiz²,

Gálvez³

et al. 2022

Preprint

View full text Add to dashboard Cite

show abstract

“…Currently, there are many methods available to synthesize triazolo[1,5- a ]pyrimidines, mainly they are cyclocondensations between 3-amino-1,2,4-triazoles and 1,3-bifunctional synthons such as 1,3-dicarbonyl compounds or their equivalents [ 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 ], vinylogous iminium salts [ 47 , 60 , 61 ], ketene dithioacetals [ 48 , 62 , 63 ], and 3-ketovinyl compounds [ 46 ]. We used α-acetylenic Ketones of types A as 1,3-bifunctional synthons.…”

Section: Introductionmentioning

confidence: 99%

Similarity-Based Virtual Screening to Find Antituberculosis Agents Based on Novel Scaffolds: Design, Syntheses and Pharmacological Assays

García-García

Julián-Ortiz

Gálvez

et al. 2022

IJMS

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A method to identify molecular scaffolds potentially active against the Mycobacterium tuberculosis complex (MTBC) is developed. A set of structurally heterogeneous agents against MTBC was used to obtain a mathematical model based on topological descriptors. This model was statistically validated through a Leave-n-Out test. It successfully discriminated between active or inactive compounds over 86% in database sets. It was also useful to select new potential antituberculosis compounds in external databases. The selection of new substituted pyrimidines, pyrimidones and triazolo[1,5-a]pyrimidines was particularly interesting because these structures could provide new scaffolds in this field. The seven selected candidates were synthesized and six of them showed activity in vitro.

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“…Fused heteroaromatic systems are often of much greater interest in biological activity than the constituent monocyclic compounds. 1,2,4‐Triazolo[1,5‐a]pyrimidines have diverse pharmacological activities, such as antitumor potency, antimalarial, antimicrobial, anti‐inflammatory, inhibition of kinase insert domain receptor kinase (KDR), antifungal and macrophage activation .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Reactivity of Enaminones: Synthesis of Some 1,3,4‐Thiadiazole Linked to Pyrazole, Pyridine, Benzimidazolopyrimidine, Pyrazolopyrimidine, Pyrazolotriazine and Triazolotriazine Derivatives

Raslan

Omran

2015

Journal of Heterocyclic Chem

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1,3,4‐Thiadiazole‐enaminone (6) was synthesized via reaction of the benzamide (5) with DMF‐DMA. The simple thiadiazole‐enaminone (6) was used as a synthetic precursor for the synthesis of a wide variety of new heterocyclic compounds, including the 5‐substituted‐1,3,4‐thiadiazole derivatives (7), (8), (16), (17) and (18), which were obtained via reactions of (6) with nitrogen nucleophiles. Also, reactions of enaminone (6) with carbon nucleophiles afforded the respective 1,3,4‐thiadiazoles (10a,10b). Diazotization of the benzamide (20) with the heteroaromatic amine salts gave the hydrazone derivatives (21) and (22). Cyclization of the latter hydrazones yielded the corresponding pyrazolotriazine and 1,2,4‐triazolotriazine derivatives (23) and (24), respectively. All newly synthesized compounds were elucidated by considering the data of both elemental and spectral analysis.

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Synthesis and Antimicrobal Activities of some Novel Triazolo[1,5-a]Pyrimidine Derivatives

Cited by 9 publications

References 11 publications

Similarity-based Virtual Screening to Find Antituberculosis Agents based on Novel Scaffolds

Similarity-based Virtual Screening to Find Antituberculosis Agents based on Novel Scaffolds

Similarity-Based Virtual Screening to Find Antituberculosis Agents Based on Novel Scaffolds: Design, Syntheses and Pharmacological Assays

Synthesis and Reactivity of Enaminones: Synthesis of Some 1,3,4‐Thiadiazole Linked to Pyrazole, Pyridine, Benzimidazolopyrimidine, Pyrazolopyrimidine, Pyrazolotriazine and Triazolotriazine Derivatives

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