Synthesis of some novel 3,5-disubstituted 1,3,4-oxadiazole derivatives and anticancer activity on EAC animal model

Dash, Sasmita; Kumar, Binod; Singh, Jagadish; Maiti, B. R.; Maity, Tapan K.

doi:10.1007/s00044-010-9455-6

Cited by 30 publications

(17 citation statements)

References 19 publications

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“…Aromatic acid (1a-6a) was esterified with methanol using 12 sulfuric acid according to the literature methods in Scheme 1 and the resulting compounds (1b-6b) were refluxed with hydrazine hydrate in ethanol to give aroyl hydrazine (1c-6c …”

Section: Synthesismentioning

confidence: 99%

Development and Physicochemical, In Vitro and In Vivo Evaluation of Transdermal Patches of Zaleplon

Tirunagari¹,

Jangala²,

Nandagopal³

2014

IJPER

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A series of potential bioactive compounds, 4-Amino-5-mercapto-3-(4-chlorophenyl)-1, 2, 4-triazole (1d), 4-Amino-5-mercapto-3-(4-nitrophenyl)-1, 2, 4-triazole (2d) , 4-Amino-5-mercapto-3-(2, 4-dichlorophenyl)-1, 2, 4-triazole (3d), 4-Amino-5-mercapto-3-(2-chlorophenyl)-1, 2, 4-triazole (4d), 4-Amino-5-mercapto-3-(2-methylphenyl)-1, 2, 4-triazole (5d), 4-Amino-5-mercapto-, 2, 4-triazole (6d) were synthesized according to the 1 literature methods. The synthesized compounds were characterized by FT-IR, H NMR spectroscopy, C H N analysis and anticancer activity was evaluated.Male Swiss albino mice has been used as test animal. Tumor cells used for anticancer activity were EAC (Ehrlich Ascites Carcinoma). Compounds were given at a dose of 25 mg/kg body weight intraperitoneally. groups were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition and non-viable cell count and increase in life span (%ILS). All the compounds exhibited the significant (P< 0.01) anticancer activity compared to control and the compound 4d is found to be the most potent one. The standard drug was used as 5-Fluorouracil (20mg/kg, body weight).Keywords: 1, 2, 4-triazole, anticancer activity, tumor cell count, tumor weight inhibition. 3-(4-methoxyophenyl)-1 Compounds treated (III-VIII)ABSTRACT

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Section: Synthesismentioning

confidence: 99%

Development and Physicochemical, In Vitro and In Vivo Evaluation of Transdermal Patches of Zaleplon

Tirunagari¹,

Jangala²,

Nandagopal³

2014

IJPER

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“…Their synthesis and transformations have been of interest for a long time.This interesting group of compounds possesses diverse biological activity such as antimicrobial [5,6], anti-inflammatory [7], antitubercular [8], anticonvulsant [9], anti-cancer [10], anti-HIV [11], hypoglycemic [12] and genotoxic [13,14] activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Studies of 5-N-alkyl-1,3,4-oxadiazole-2-thiol Derivatives from Fatty Acids

Sudha¹,

Subbaiah²,

A³

et al. 2017

Asian J. Chem.

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The novel 5-N-alkyl-1,3,4-oxadiazole-2-thiol derivatives have been synthesized by esterification of fatty acid followed by reaction the ester with hydrazine hydrate. The acid hydrazide was converted to 1,3,4-oxadiazole by ring closure mechanism. The synthesized compounds have been characterized by physical (melting point and TLC) and spectral (IR, 1 H NMR and mass) data. All the compounds were screened for their antimicrobial activity. The compounds 3F1 & 3F4 showed good inhibition activity against all four types of bacteria; while compound 3F2 & 3F3 shown moderate activity.

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“…Pyrazole derivatives exhibited a broad spectrum of useful properties such as antitumor [11], antitubercular [12], antioxidant [13], anti-inflammatory [14,15], antibacterial [16], anti-obesity [17] and antidepressant [18] activities. Similarly, 1,3,4-oxadiazoles have been reported to exhibit various biological [19,20] and pharmacological activities [21][22][23][24][25]. These compounds, in particular, have been found to exhibit biological potential such as anticancer activity [26][27][28] specifically in the presence of some potent heterocyclic nuclei.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some Aroylhydrazones and 2,5-Disubstituted-1,3,4- Oxadiazoles as DNA Photocleaving Agents

Kumar¹,

Kumar²,

Beniwal³

et al. 2016

Med chem (Los Angeles)

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Some 2,5-disubstituted-1,3,4-oxadiazole derivatives have been synthesized conveniently via oxidative cyclization of various synthesized aroylhydrazones by (diacetoxyiodo)benzene in dichloromethane under mild reaction conditions. In addition, the effect of electron-withdrawing/releasing groups on the formation of oxadiazole nucleus has also been studied. Compounds were obtained in good yields and their structures have been established on the basis of their FT-IR, 1 H, 13 C NMR and mass spectral data. Herein, a total of 42 compounds (hydrazones as well as oxadiazoles) were synthesized and investigated for their DNA photocleavage potential using plasmid DNA. It has been observed that aroylhydrazones showed good DNA photocleavage activity in comparison to their corresponding oxadiazoles.

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Synthesis of some novel 3,5-disubstituted 1,3,4-oxadiazole derivatives and anticancer activity on EAC animal model

Cited by 30 publications

References 19 publications

Development and Physicochemical, In Vitro and In Vivo Evaluation of Transdermal Patches of Zaleplon

Development and Physicochemical, In Vitro and In Vivo Evaluation of Transdermal Patches of Zaleplon

Synthesis and Antimicrobial Studies of 5-N-alkyl-1,3,4-oxadiazole-2-thiol Derivatives from Fatty Acids

Synthesis of Some Aroylhydrazones and 2,5-Disubstituted-1,3,4- Oxadiazoles as DNA Photocleaving Agents

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