Synthesis and Biological Evaluation of Novel 5,7‐Dichloro‐1,3‐benzoxazole Derivatives

Jayanna, N D; Vagdevi, H. M.; Dharshan, J. C.; Kekuda, T.R.Prashith; Hanumanthappa, B. C.; Gowdarshivannanavar, B. C.

doi:10.1155/2013/864385

Cited by 9 publications

(12 citation statements)

References 28 publications

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“…The enhanced activity of both these compounds is by virtue of absence of substitution or due to electron donating methoxy group. [31] Watanabe et al (2015) reported the fabrication of 2-arylbenzoxazole that was used in Gram negative bacteria in order to detect nitro-ductase activity. Compound 2-(2-nitrophenyl)benzoxazole ( 21) exhibited best results against Gram negative bacteria and strain of S. aureus for nitroductase activity.…”

Section: Antibacterial Activitymentioning

confidence: 99%

“…Among the tested compounds, 1-(5,7-dichlorobenzoxazol-2-yl)-1Hpyrazolo [3,4-b]quinolin-6-ol (79) exhibited good scavenging effect 59.21% to 78.70%. [31] Gudipati et al (2011) fabricated a novel series of 12 derivatives of N-(benzoxazol-2-yl)-2-(7-or 5-substituted-2-oxoindolin-3-ylidene) hydrazinecarboxamide. These compounds were evaluated for their antioxidant activity by employing method of DPPH comparable to standard ascorbic acid.…”

Section: Antioxidant Activitymentioning

confidence: 99%

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Synthetic transformations and biological screening of benzoxazole derivatives: A review

Sattar

Mukhtar

Atif

et al. 2020

Journal of Heterocyclic Chem

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The presence of benzoxazole moiety in most of the heterocyclic compounds is well reported. The present literature review mainly highlights the novel synthetic transformation and describes the biological potential of most of the heterocyclic compounds by virtue of presence of benzoxazole framework. Most of the researchers have revealed that benzoxazole derivatives exhibit significant antibacterial, anti-inflammatory, antifungal, anticancer, analgesic, antiviral, anti-tubercular, and anthelmintic activities. Benzoxazole moieties also act as tyrosinase inhibitor and cholesterol ester transfer protein inhibitor. This literature review may provide an opportunity to the chemists to design new derivatives of benzoxazole that proved to be the successful agent in view of safety, effectiveness, and efficacy.

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Section: Antibacterial Activitymentioning

confidence: 99%

Section: Antioxidant Activitymentioning

confidence: 99%

Synthetic transformations and biological screening of benzoxazole derivatives: A review

Sattar

Mukhtar

Atif

et al. 2020

Journal of Heterocyclic Chem

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“…Antimicrobial screening of the substituted pyrazolo [3,4-b]pyridines derivatives (PYR1-5) was performed by the Agar well diffusion method [38] and the dilution method (agar and liquid broth). The antimicrobial activity was evaluated using two different laboratory control strains of bacteria, i.e., Gram positive Bacillus subtilis CIP 5262, Gram negative, Escherichia coli CIP 53126.…”

Section: In Vitro Antibacterial and Antifungal Assaymentioning

confidence: 99%

Substituted Pyrazolo[3,4-B]Pyridin-3-Ones and Pyrazolo[3,4-B]Pyridine-5- Carbaldehyde, New One-Pot Synthesis Strategy Amelioration Using Vinamidinium Salts, Antibacterial and Antifungal Activities Promising Environmental Protection

Chtiba¹,

Amri²,

Tazarki³

et al. 2017

J Bacteriol Parasitol

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This review summarizes the current knowledge about the syntheses and biological behavior of some pyrazolo [5,4-b]pyridines. So, an expedient method for the synthesis of 2-phenyl-5-aryl-1,6-dihydropyrazolo [3,4-b]pyridin-3-ones and 2-phenyl-3-oxo-1,6-dihydropyrazolo[3,4-b]pyridine-5-carbaldehyde in a single-step via condensation of vinamidinium salts with 3-amino-1-phenyl-2-pyrazolin-5-one is described according to our recent study with synthesis strategy amelioration. Five derivatives (PYR 1-5 ) were prepared and characterized by spectral data (NMR and MS spectral studies). All the derivatives were studied for their antimicrobial activities. So, we screened for antibacterial effects at 1:2, and 1:4 dilutions by the paper disc diffusion method against respectively Bacteria (Escherichia coli CIP 53126 and Bacillus subtilis CIP 5262) and Fungi (Candida albicans ATCC 10231). Then, we screened for Fungi (Aspergillus niger ATCC 16404) by the dilution method (agar and liquid broth). The agar diffusion method (paper disc and well) and the dilution method (agar and liquid broth) are described.

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“…The benzoxazole derivatives have been investigated for their inhibitory activity on eukaryotic DNA topoisomerase, and are known to exhibit antibacterial, , antitubercular, anticancer, antiparasitic, and anti-HIV activity (Figure ). In view of such therapeutic significance of these compounds, several methods targeting their individual synthesis, as well synthesis in combined form have been reported. − These methods, however, suffer from drawbacks of being carried out in multiple steps; generate a large number of byproducts, long reaction time, use of harsh reagents and conditions, and low overall yield of the final product. With a view of harnessing the interesting biological properties of triazole and benzoxazole molecules, we attempted designing a simple synthetic route to construct these scaffolds.…”

Section: Introductionmentioning

confidence: 99%

One-Pot Sequential Alkynylation and Cycloaddition: Regioselective Construction and Biological Evaluation of Novel Benzoxazole–Triazole Derivatives

2014

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Individually, benzoxazole and triazole moieties are of significant biological interest owing to their importance in drugs and pharmaceuticals. To assess their combined biological impact when woven into one molecule, we designed a novel, regioselective, multicomponent, one-pot (MCOP) approach for the construction of benzoxazole-linked triazoles. The synthesis has been achieved in two sequential steps involving copper-catalyzed alkynylation of benzoxazole followed by a 1,3-dipolar cycloaddition reaction. By combination of these two bioactive units into one core, a series of new benzoxazole-triazole scaffolds has been synthesized and subjected to in vitro antibacterial and anticancer evaluation. Tests against clinical isolates of Staphylococcus aureus and Escherichia coli showed potent Gram-negative activity for compounds 4{1,1,1}, 4{1,1,4}, and 4{1,2,1}. The cytotoxicity of the synthesized library was determined against three cancer cell lines: HeLa, SKBr3, and Hep G2. Compound 4{2,2,2} showed significant cytotoxicity against all the cell lines. These preliminary bioassay evaluations strongly suggest the promise and scope of these novel molecules as therapeutic agents in medical science.

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Synthesis and Biological Evaluation of Novel 5,7‐Dichloro‐1,3‐benzoxazole Derivatives

Cited by 9 publications

References 28 publications

Synthetic transformations and biological screening of benzoxazole derivatives: A review

Synthetic transformations and biological screening of benzoxazole derivatives: A review

Substituted Pyrazolo[3,4-B]Pyridin-3-Ones and Pyrazolo[3,4-B]Pyridine-5- Carbaldehyde, New One-Pot Synthesis Strategy Amelioration Using Vinamidinium Salts, Antibacterial and Antifungal Activities Promising Environmental Protection

One-Pot Sequential Alkynylation and Cycloaddition: Regioselective Construction and Biological Evaluation of Novel Benzoxazole–Triazole Derivatives

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