Synthesis and antihyperglycemic activity of suitably functionalized 3H-quinazolin-4-ones☆

Ram, Vishnu Ji; Farhanullah,; Tripathi, Brajendra K.; Srivastava, Arvind K.

doi:10.1016/s0968-0896(03)00142-1

Cited by 88 publications

(51 citation statements)

References 8 publications

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“…This reflects that the compound 4b may enhance the deteriorated insulin secretion in response to glucose in n-STZ diabetic rats. Our results are in concurrence with those of other publications [22,28] which revealed that the treatment with 3H-quinazolinone derivatives induced potential hypoglycemic and secretogouge effects in diabetic rats.…”

Section: Biological Studiessupporting

confidence: 93%

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Antidiabetic and Antioxidant Effects of Newly Synthesized Pyrimido[1,6-A] Pyrimidine Derivatives in Neonatal Streptozotocin-Induced Diabetic Rats

Ahmed¹,

Hussein²

2012

Med Chem

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Synthesis of some novel pyrimido[1,6-a]pyrimidine derivatives 4, 8 and 10 was described through the respective reactions of sodium salts of formyl ketones 1, 7 and 9 with 6-aminothiouracil. The characterization of the reaction products was confirmed by using the available elemental analysis and spectral data. One of these derivatives (4b), 1-thioxo-1,2,7,8,9,10-hexahydro-3H-pyrimido[1,6-a]quinazolin-3-one, was tested using sublethal dose level (10 mg/kg b. w./day for 3 weeks) and was found to have potent antihyperglycemic, antihyperlipidemic and antioxidant properties in neonatal streptozotocin-induced (n-STZ) diabetic male and female albino rats.

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Section: Biological Studiessupporting

confidence: 93%

“…3(H)-quinazolinone derivatives have been shown as a group of compounds of broad medical interest [17][18][19][20][21]. It was reported that some 3(H)-quinazolinone derivatives exhibited potent antihyperlipidemic and antihyperglycemic activity in alloxan diabetic-hypercholesterolemic and streptozotocin diabetic rats respectively [22,23].…”

Section: Introductionmentioning

confidence: 99%

Antidiabetic and Antioxidant Effects of Newly Synthesized Pyrimido[1,6-A] Pyrimidine Derivatives in Neonatal Streptozotocin-Induced Diabetic Rats

Ahmed¹,

Hussein²

2012

Med Chem

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“…It inflicts more than 60 million people worldwide according to epidemiological studies [1,2]. Different chemical classes such as hydantoins, barbiturates, benzodiazepines, gamma-amino butyric acid (GABA) analogs, dibenzazepines, and carbamates are known to be part of anti-epileptic scaffolds [3][4][5][6][7][8].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Anticonvulsant Activity (Chemo Shock) of N-1(substituted-N-4[(4-Oxo-3-Phenyl-3, 4-Dihydro-Quinazoline-2-Ylmethyl) Semicarbazones

Yadav

Tripathi²,

Goswami³

2017

Asian J Pharm Clin Res

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Objective: This work is designed at finding new structure leads with potential anticonvulsant activities of 4(3H)-quinazolinone pharmacophore scaffold. Methods:A new series of 4(3H)-quinazolinone pharmacophore was designed with substituted moieties possesses different electronic environment in the hope of developing potent and safe new effective compounds. In such fashion, in this paper, we report the synthesis and anticonvulsant activity (Chemo shock) of N-1(substituted-N-4[(4-oxo-3-phenyl-3, 4-dihydro-quinazoline-2-ylmethyl) semicarbazones 3A-d (1-7), 3B-d (1-7), 3C-d (1-7), their chemical structure were characterized using IR, 1 H-H NMR, and elemental analysis techniques. Their anticonvulsant activity was evaluated using chemicals strychnine, thiosemicarbazide and 4-aminopyridine induced seizure models at a dose of 30, 100, 300 mg/kg unto 2 hrs tests in mice. The rotarod assay was performed in mice to evaluate the neurotoxicity of the compounds.Results: Compounds 3C (d-4), 3B (d-4), and 3A (d-4) were observed to be most feasible to act against glutamate receptor for anticonvulsant activity. Conclusions:The results obtained revealed that numbers of novel quinazolinone semicarbazone derivatives are effective in chemical to induce (chemo shock) model and showing good anticonvulsant activity.

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“…To our knowledge, a 4(3H)-quinazolinone moiety is a class of important functional groups. Additionally, compounds containing the moiety have broadspectrum, high-efficiency bioactivities, such as bactericidal, 8,9) antipyretic, 10) analgesic, 11) fungicidal, 12) antitetanic, 13) antihypertensive, 14) anticancer 15) activities and so on. Motivated by the function of the 4(3H)-quinazolinone moiety, we have first described an efficient protocol for synthesizing of 3-aminoalkyl-2-arylaminoquinazolin-4(3H)-ones via an aza-Wittig reaction.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological activity of arylsulfonamide derivatives containing 2-arylamino-4(3<i>H</i>)-quinazolinone

Zeng

Gao

et al. 2016

J. Pestic. Sci.

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Twenty arylsulfonamide derivatives containing 2-arylamino-4(3H)-quinazolinone were synthesized and evaluated for their bioactivities. phenyl)amino)quinazolin-3(4H)-yl)-ethyl benzenesulfonamide, showed excellent activity both against Ralstonia solanacearum and Gibberella zeae with the inhibition rates of 100% (200 mg/L) and 95% (100 mg/L), and 69% (50 mg/L), respectively, exceeding that of the assigned commercial bactericide (thiodiazole-copper) and fungicide (hymexazol). The preliminary structure activity relationships (SAR) showed that both benzene rings of arylamino and arylsulfonamido moieties containing electron-withdrawing substitutes may be preferable for improving the bioactivity of target compounds.

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Synthesis and antihyperglycemic activity of suitably functionalized 3H-quinazolin-4-ones☆

Cited by 88 publications

References 8 publications

Antidiabetic and Antioxidant Effects of Newly Synthesized Pyrimido[1,6-A] Pyrimidine Derivatives in Neonatal Streptozotocin-Induced Diabetic Rats

Antidiabetic and Antioxidant Effects of Newly Synthesized Pyrimido[1,6-A] Pyrimidine Derivatives in Neonatal Streptozotocin-Induced Diabetic Rats

Synthesis and Anticonvulsant Activity (Chemo Shock) of N-1(substituted-N-4[(4-Oxo-3-Phenyl-3, 4-Dihydro-Quinazoline-2-Ylmethyl) Semicarbazones

Synthesis and biological activity of arylsulfonamide derivatives containing 2-arylamino-4(3<i>H</i>)-quinazolinone

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