Cs2CO3-promoted one-pot synthesis of novel tetrahydrobenzofuran-4(2H)-ones: In vitro antimicrobial, antimalarial activity and in silico docking study

Bhalodiya, Savan S.; Parmar, Mehul P.; Upadhyay, Dipti B.; Patel, Chirag D.; Vala, Disha P.; Rajani, Dhanji; Patel, Hitendra M.

doi:10.1016/j.rechem.2023.101304

Results in Chemistry

2024

DOI: 10.1016/j.rechem.2023.101304

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Cs2CO3-promoted one-pot synthesis of novel tetrahydrobenzofuran-4(2H)-ones: In vitro antimicrobial, antimalarial activity and in silico docking study

Savan S. Bhalodiya,

Mehul P. Parmar,

Dipti B. Upadhyay

et al.

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2024

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Cited by 6 publications

References 49 publications

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Acetic Acid‐Driven One‐Pot Synthesis of 4,7‐dihydro‐[1,2,3]thiadiazolo[5,4‐b]pyridine‐6‐carboxamides and Pharmacological Evaluations

Bhalodiya,

Parmar,

Patel

et al. 2024

ChemMedChem

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A diverse set of 4,7‐dihydro‐[1,2,3]thiadiazolo[5,4‐b]pyridine‐6‐carboxamides 4(a‐o) were synthesized via a one‐pot reaction of 5‐amino[1,2,3]thiadiazole, various aromatic aldehydes, and different acetoacetanilides, using glacial acetic acid as the solvent and without the need for any catalysts. The resulting compounds were obtained in moderate to good yields. All the newly synthesized compounds were evaluated for their antimicrobial activity. Among them, compound 4e demonstrated superior efficacy against Salinivibrio proteolyticus strain of Gram‐(‐Ve)‐bacteria compared to ciprofloxacin. Compound 4d exhibited the highest potency against the fungal strain Candida albicans surpassing Amphotericin B. 4d and 4e's physicochemical characteristics were assessed. According to docking analysis, DHTDAPy 4e shows the higher binding affinity of ‐7.2 kcal moL‐1 in the binding cavity of the receptor. These findings illustrate the safety and tolerability as well as the potency of newly syntehsized DHTDAPy against the fungal and bacterial infections.

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Acetic Acid‐Driven One‐Pot Synthesis of 4,7‐dihydro‐[1,2,3]thiadiazolo[5,4‐b]pyridine‐6‐carboxamides and Pharmacological Evaluations

Bhalodiya,

Parmar,

Patel

et al. 2024

ChemMedChem

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Identification of O-arylated huperzinines as novel cholinergic anti-inflammatory pathway agonists against gout arthritis

Wu,

Zhang,

Dou

et al. 2024

Bioorganic Chemistry

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Synthesis of 4-(3-(1-substituted/unsubstituted-phenyl-1H-1,2,3-triazole-4-yl)propoxy)benzaldehydes: In vitro antimicrobial, antimalarial activities and In silico docking study

Al-Salehi,

Parmar,

Rajani

et al. 2024

Journal of Molecular Structure

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Cs2CO3-promoted one-pot synthesis of novel tetrahydrobenzofuran-4(2H)-ones: In vitro antimicrobial, antimalarial activity and in silico docking study

Cited by 6 publications

References 49 publications

Acetic Acid‐Driven One‐Pot Synthesis of 4,7‐dihydro‐[1,2,3]thiadiazolo[5,4‐b]pyridine‐6‐carboxamides and Pharmacological Evaluations

Acetic Acid‐Driven One‐Pot Synthesis of 4,7‐dihydro‐[1,2,3]thiadiazolo[5,4‐b]pyridine‐6‐carboxamides and Pharmacological Evaluations

Identification of O-arylated huperzinines as novel cholinergic anti-inflammatory pathway agonists against gout arthritis

Synthesis of 4-(3-(1-substituted/unsubstituted-phenyl-1H-1,2,3-triazole-4-yl)propoxy)benzaldehydes: In vitro antimicrobial, antimalarial activities and In silico docking study

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