Synthesis of New Triazole and Oxadiazole Derivatives of Quinazolin‐4(3<i>H</i>)‐one and Their Antimicrobial Activity

Vani, K. Veena; Ramesh, G.; Rao, C. Venkata

doi:10.1002/jhet.2353

Cited by 16 publications

(6 citation statements)

References 22 publications

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“…synthesised series of triazole and oxadiazole derivatives of quinazolin‐4‐(3H)‐one. The compounds were screened for their antifungal efficacy against the Candida albicans and compounds 57 was found to be most potent antifungal agent with ZOI value of 20 mm at 236.29 μmol/mL [87] . Similarly, Wahab‐Abdel et al .…”

Section: 23‐triazole Derivatives With Antifungal Activity Against As ...mentioning

confidence: 99%

“…The compounds were screened for their antifungal efficacy against the Candida albicans and compounds 57 was found to be most potent antifungal agent with ZOI value of 20 mm at 236.29 μmol/mL. [87] Similarly, Wahab-Abdel et al designed and synthesised a series of thiosemicarbazide-1,2,3-triazole based derivatives and tested for the antifungal activity against the Candida albicans. Among them, compound 58 was found to be most potent antifungal with MIC value of 315.26 μmol/mL.…”

Section: Miscellaneous 123-triazole Containing Derivativesmentioning

confidence: 99%

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1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

Singh

Sharma

et al. 2023

Chemistry & Biodiversity

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Candida infections are most prominent among fungal infections majorly target immunocompromised and hospitalized patients and cause significant morbidity and mortality. Candida albicans is the notorious and most prevalent among all pathogenic Candida strains. Its emerging resistance toward available antifungal agents making it hard to tackle and emerging as global healthcare emergency. Simultaneously, 1,2,3-triazole nucleus is a privileged scaffold that is gaining importance in antifungal drug development due to being a prominent bioactive linker and isostere of triazole based antifungal class core 1,2,4-triazole. Numerous reports have been updated in scientific literature in last few decades related to utilization of 1,2,3-triazole nucleus in antifungal drug development against Candida albicans. Present review will shed light on various preclinical studies focused on development of 1,2,3-triazole derivatives targeting Candida albicans along with brief highlight on clinical trials and newly approved drugs. Structure-activity relationship has been precisely discussed for each architect along with future perspective that will help medicinal chemists in design and development of potent antifungal agents for tackling infections derived from Candida albicans.

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Section: 23‐triazole Derivatives With Antifungal Activity Against As ...mentioning

confidence: 99%

Section: Miscellaneous 123-triazole Containing Derivativesmentioning

confidence: 99%

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

Singh

Sharma

et al. 2023

Chemistry & Biodiversity

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“…Vani et al [76] synthesized a series of quinazolin-4(3H)-one-triazole hybrids (63-65) quinazolin-4(3H)-one and oxadiazole hybrids (66)(67)(68). Compounds 64-67 showed significant antibacterial activity against all the bacterial strains, Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), while compounds (63,67,68) showed highest activity against fungal species, Candida albicans and Aspergillus niger compared with ciprofloxacin and fluconazole as reference drugs, respectively.…”

Section: Antimicrobial Activity Of Quniazolinonesmentioning

confidence: 99%

Biological Activity of Quinazolinones

Radwan¹,

Alanazi²

2020

Quinazolinone and Quinazoline Derivatives

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The chemical structure of quinazolinones includes benzene ring fused with 2-pyrimidinone (1), 4-pyrimidinone (2) or 2,4-pyrimidinedione (3) ring, and are named as quinazolin-2(1H)-one, quinazolin-4(3H)-one or quinazolin-2,4(1H, 3H)-one, respectively. The chemical structure of quinazolinones constitutes a crucial scaffold of natural and synthetic compounds with various therapeutic and biological activities. Quinazolinones are first synthesized by Stefan Niementowski (1866-1925) and named after Niementowski quinazolinone synthesis. Quinazolinones have strongly attracted the interest of medicinal chemist as they constitute a large class of compounds that exhibited broad spectrum of biological activities including antimicrobial, antimalarial, anticonvulsant, anticancer, antileishmanial, anti-inflammatory, etc. This chapter provides a brief overview on the recent advances on chemical and pharmacological aspects of quinazolinone derivatives published in the last decade.

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“…Quinazolinone derivatives have been attracting growing attention from medicinal and agricultural chemists, owing to their diverse biological activities, such as antibacterial [21][22][23][24][25][26][27], antifungal [28][29][30], antiviral [31,32], antitumor [33,34] and anticonvulsant [35] activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis And Antibacterial Activity of 6-Bromo-2-(O-Aminophenyl)-3-Amino-Quinazolin-4(3h)-One From 6-Bromo,2-(O-Aminophenyl)-3,1-Benzoxazin-4(3h)-One

Osarodion

2023

CCRT

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Introduction: Quinazolinone derivatives reveal various medicinal properties such as analgesic, anti-inflammatory and anticancer activities, as well as antimicrobial activity. These heterocycles are valuable intermediates in organic synthesis.Methods/Experimental: The compound, 6-bromo,2-(o-aminophenyl)-3,1-benzoxazin-4(3H)-one (1) was synthesized by dissolving 5-bromo anthranillic acid in 100 ml of pyridine. To this reaction mixture o-amino benzoyl chloride stirring at room temperature for 30 minutes this was refluxed with 75 mL of hydrazine hydrate for 3 hrs at 120-1300C. the reaction mixture was allowed to cool to room temperature to give 6-bromo-2-(o-aminophenyl)-3-amino-Quinazolin-4(3H)-one (2). These Compounds were evaluated for their bacterialrial activity (against some gram positive and gram negative microorganism) and antifungal activity (against Candida albicans). Study Design: This study was experimentally design and the antibacterial activity was evaluated against some microorganism, Staphylococcus aureus, Bacillus species, Aspergillus Species, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumonia, and candida albicans Result: The compounds exhibited significant antibacterial activity with a zone of inhibition in the range of 10 – 16mm in comparison to control. Conclusions: From our findings, the compounds synthesized have higher antibacterial activities as compared to Ciprofloxicin (CPX) and Ketonaxol (PEF) standard antibacterial drugs.

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Synthesis of New Triazole and Oxadiazole Derivatives of Quinazolin‐4(3H)‐one and Their Antimicrobial Activity

Cited by 16 publications

References 22 publications

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

Biological Activity of Quinazolinones

Synthesis And Antibacterial Activity of 6-Bromo-2-(O-Aminophenyl)-3-Amino-Quinazolin-4(3h)-One From 6-Bromo,2-(O-Aminophenyl)-3,1-Benzoxazin-4(3h)-One

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