Synthesis and antimicrobial activity of 2-substituted [4-(1,3,4-oxadiazol-2-yl methyl)] phthalazin-1(2H)-one derivatives

Sridhara, A. M.; Reddy, K. R. Venugopala; Keshavayya, J.; Goud, Palusa Sanath Kumar; Somashekar, Bankavadi C.; Bose, Prosenjit; Peethambar, S. K.; Gaddam, Satish Kumar

doi:10.1016/j.ejmech.2010.08.005

Cited by 37 publications

(16 citation statements)

References 33 publications

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“…Similarly, intermediate 1 furnished desired compounds 28 and 29 by reaction with cyanogen bromide in the presence of sodium bicarbonate at ambient temperature [ 29 ]. For preparation of 3-(2-substituted-1,3,4-oxadiazol-5-yl)-β-carbolines 30 – 36 , 1-phenyl-β-carboline-3-carbohydrazide was subjected to reaction with a series of acids, followed by treatment with phosphorus oxychloride under reflux [ 30 ]. The compound 30 could be synthesized using other methodology [ 31 ].…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Bioactivity Evaluation of Novel β-carboline 1,3,4-oxadiazole Derivatives

Zhang

Jiang

et al. 2017

Molecules

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A series of novel β-carboline 1,3,4-oxadiazole derivatives were designed and synthesized, and the in vitro cytotoxic activity against Sf9 cells and growth inhibitory activity against Spodoptera litura were evaluated. Bioassay results showed that most of these compounds exhibited excellent in vitro cytotoxic activity. Especially, compound 37 displayed the best efficacy in vitro (IC50 = 3.93 μM), and was five-fold more potent than camptothecin (CPT) (IC50 = 18.95 μM). Moreover, compounds 5 and 37 could induce cell apoptosis and cell cycle arrest and stimulate Sf-caspase-1 activation in Sf9 cells. In vivo bioassay also demonstrated that compounds 5 and 37 could significantly inhibit larvae growth of S. litura with decreasing the weight of larvae and pupae. Based on these bioassay results, compounds 5 and 37 emerged as lead compounds for the development of potential insect growth inhibitions.

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Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Bioactivity Evaluation of Novel β-carboline 1,3,4-oxadiazole Derivatives

Zhang

Jiang

et al. 2017

Molecules

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“…Compounds 112 and 113 were twice as potent as fluconazole against C. albicans [ 69 ] ( Figure 5 ). Other oxadiazole compounds with antibacterial activity are: 114 [ 70 ], 115 [ 71 ], 116 [ 72 ], 117 [ 13 ], 118 [ 73 ], 119 [ 24 ], 120 [ 74 ], 121 [ 75 ] and 122 [ 76 ] ( Figure 5 ).…”

Section: Pharmacological Activity Of 134-oxadiazolesmentioning

confidence: 99%

Synthetic Approaches and Pharmacological Activity of 1,3,4-Oxadiazoles: A Review of the Literature from 2000–2012

et al. 2012

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“…The results data revealed that the synthesized compounds showed variable degree of inhibition against the tested fungi and bacteria. Compound 77 was one of the synthesized compounds which exhibited promising activity against E. coli, S. aureus, Salmonella typhi, Chrysosporium keratinophilum and C. albicans [111].…”

Section: Antimicrobial Activitymentioning

confidence: 99%

Substituted oxadiazoles: a patent review (2010 – 2012)

Zarghi

Hajimahdi

2013

Expert Opinion on Therapeutic Patents

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Oxadiazoles have been used frequently in drug-like molecules as bioisosteres for ester and amide functionalities and displayed numerous prominent pharmacological effects. The broad pharmacological profile of oxadiazole derivatives has attracted the attention of many researchers to explore this scaffold to its multiple potential against several activities. Therefore, oxadiazole motif is likely to be present in other therapeutic molecules in the future.

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Synthesis and antimicrobial activity of 2-substituted [4-(1,3,4-oxadiazol-2-yl methyl)] phthalazin-1(2H)-one derivatives

Cited by 37 publications

References 33 publications

Design, Synthesis and Bioactivity Evaluation of Novel β-carboline 1,3,4-oxadiazole Derivatives

Design, Synthesis and Bioactivity Evaluation of Novel β-carboline 1,3,4-oxadiazole Derivatives

Synthetic Approaches and Pharmacological Activity of 1,3,4-Oxadiazoles: A Review of the Literature from 2000–2012

Substituted oxadiazoles: a patent review (2010 – 2012)

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