Synthesis of some newer derivatives of substituted quinazolinonyl-2-oxo/thiobarbituric acid as potent anticonvulsant agents

Archana, .; Srivastava, Vinay Kumar; Kumar, Ashok

doi:10.1016/j.bmc.2003.08.035

Cited by 95 publications

(48 citation statements)

References 4 publications

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“…SHIMADZU Affinity-I spectrophotometer was for recording the IR spectrum. General synthesis scheme of the target compound [7][8][9][10][11] (SMMB [1][2][3] ) To a solution of barbituric acid (0.01 mol)/ thiobarbituric acid (0.01 mol) in methanol as solvent, formaldehyde (0.02 mol) and 3-amino-2-methylquinazolin-4(3H)-one (0.02 mol) were added drop wise. The reaction mixture was refluxed on a steam bath for 4 hr.…”

Section: Chemistrymentioning

confidence: 99%

See 1 more Smart Citation

In silico Design, Synthesis and Pharmacological screening of Quinazolinones as NMDA receptor antagonists for Anticonvulsant activity: Part II

Nerkar¹,

Sahu²,

Sawant³

2015

JYP

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Background: N-methyl-D-Aspartate (NMDA) receptor plays a main role in eliptogenisis and its inhibition has therapeutic significance in development of anticonvulsants. Prioritized quinazolinone molecules were synthesized, evaluated in vivo by AOT and then for anticonvulsant activity in NMDA induced convulsion model. Method: In silico Screening of prioritized molecule was done by biological activity predictions, partition coefficient predictions (Log P), molecular docking on NMDA receptors, in silico ADME predictions using PASS server and mol inspiration software, V Life MDS 4.3 software and Pre ADMET server respectively. This gave biological activity (BA) score for anticonvulsant activity and predicted Log P values (p Log P). The standard Log P required for anticonvulsant activities being more than 2.00, therefore molecules were also prioritized based on this p Log P criteria. Docking showed results of antagonism in silico as compared with Memnatine and molecules were prioritized for synthesis based on this criteria. Result: Quinazolinone molecules were prioritized based upon docking score, ADME and BA score, synthesized and pharmacologically screened for anticonvulsant activity. Conclusion: SMMB 1 , SMMB 2 , SMMB 3 showed the prominent anticonvulsant activity as compared with memantine used as standard for in vivo anticonvulsant activity. The compounds can serve as anticonvulsant Leads through NMDA antagonism.

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Section: Chemistrymentioning

confidence: 99%

“…Synthesis of 2(methyl) 6-Bromo-3-amino(-5-methyl (Thiobarbituryl) quinazoline-4(3H) one (SMMB 1 ): 7,8 To a solution of thiobarbituric acid (0.01 mol) in methanol as solvent, formaldehyde (0.02 mol) and 6-bromo-3-amino-2-methylquinazolin-4(3H)-one (0.02 mol) was added drop wise. The reaction mixture was refluxed on a steam bath for 4 hr.…”

Section: 7mentioning

confidence: 99%

In silico Design, Synthesis and Pharmacological screening of Quinazolinones as NMDA receptor antagonists for Anticonvulsant activity: Part II

Nerkar¹,

Sahu²,

Sawant³

2015

JYP

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“…Researchers has revealed that various 5-substituted barbituric acid derivatives possess potent anticonvulsant activity [9][10][11][12][13][14][15][16] . In view of these observations, it was thought worthwhile to synthesize a new series of 5-substituted barbituric acid derivatives bearing phenothiazinyl moiety.…”

Section: Oriental Journal Of Chemistrymentioning

confidence: 99%

Synthesis of 5- [(11substitutedphenothiazinoacetyl) semicarbazidothio- semicarbazido]-2- oxo/thiobarbiuric Acid as Anticonvulsant Agents

Tyagi¹,

Archana²

2014

Orient. J. Chem.

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ABSTRACT2-Substitutedphenathiazine was prepared according to the reported method. Ethylsubstitutedphenothiazinoacetates(1a-1b) were prepared by the reaction of ethylchloroacetate in the presence of anhydrous K 2 CO 3. 2-amino-5-N 10 substitutedphenothiazinoacetyl)-semicarbazdes/ thiosemicarbazides (2a-2d) were synthesized by refluxing compound (1a-1b) with thiosemicarbazide/semicarbazide. Compounds (2a-2d) were then underwent mannich reaction to yield compounds 3a-3d. All the newly synthesized compounds (i.e. 2a-2d and 3a-3d) were evaluated for their anticonvulsant activity. Almost all the compounds have shown promising anticonvulsant activity. Compound 3d was the most potent compound of this series. The most potent compound was evaluated for its anticonvulsant activity and acute toxicity.

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“…Such medical health problems have encouraged many medicinal chemists to search for novel antibacterial agents other than the analogs of existing antibiotics 7 . Quinazolines are frequently used in medicine because of their wide spectrum of biological activities [8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26] . Based on the good performances of quinazoline derivatives in anticancer application, development of novel quinazoline derivatives as anticancer drugs is a promising field 9 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, antitumor and antimicrobial activity of some new 6-methyl-3-phenyl-4(3H)-quinazolinone analogues: in silico studies

Alanazi

Abdel‐Aziz

Shawer

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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Some new derivatives of substituted-4(3H)-quinazolinones were synthesized and evaluated for their in vitro antitumor and antimicrobial activities. The results of this study demonstrated that compound 5 yielded selective activities toward NSC Lung Cancer EKVX cell line, Colon Cancer HCT-15 cell line and Breast Cancer MDA-MB-231/ATCC cell line, while NSC Lung Cancer EKVX cell line and CNS Cancer SF-295 cell line were sensitive to compound 8. Additionally, compounds 12 and 13 showed moderate effectiveness toward numerous cell lines belonging to different tumor subpanels. On the other hand, the results of antimicrobial screening revealed that compounds 1, 9 and 14 are the most active against Staphylococcus aureus ATCC 29213 with minimum inhibitory concentration (MIC) of 16, 32 and 32 mg/mL respectively, while compound 14 possessed antimicrobial activities against all tested strains with the lowest MIC compared with other tested compounds. In silico study, ADME-Tox prediction and molecular docking methodology were used to study the antitumor activity and to identify the structural features required for antitumor activity.

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Synthesis of some newer derivatives of substituted quinazolinonyl-2-oxo/thiobarbituric acid as potent anticonvulsant agents

Cited by 95 publications

References 4 publications

In silico Design, Synthesis and Pharmacological screening of Quinazolinones as NMDA receptor antagonists for Anticonvulsant activity: Part II

In silico Design, Synthesis and Pharmacological screening of Quinazolinones as NMDA receptor antagonists for Anticonvulsant activity: Part II

Synthesis of 5- [(11substitutedphenothiazinoacetyl) semicarbazidothio- semicarbazido]-2- oxo/thiobarbiuric Acid as Anticonvulsant Agents

Synthesis, antitumor and antimicrobial activity of some new 6-methyl-3-phenyl-4(3H)-quinazolinone analogues: in silico studies

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