Hit, Lead & Candidate Discovery A series of 2‐(2‐substituted benzylidenehydrazinyl‐2‐oxopropyl)‐3‐(4‐[4‐oxo‐2‐phenylthiazolo din‐3‐yl]phenyl)quinazolin‐4(3H)‐one 7a‐7l were synthesized and characterized by IR, 1H‐NM...
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https://www.riss.kr/link?id=O118980120
2018년
-
0272-4391
1098-2299
SCI;SCIE;SCOPUS
학술저널
260-274 [※수록면이 p5 이하이면, Review, Columns, Editor's Note, Abstract 등일 경우가 있습니다.]
0
상세조회0
다운로드다국어 초록 (Multilingual Abstract)
Hit, Lead & Candidate Discovery A series of 2‐(2‐substituted benzylidenehydrazinyl‐2‐oxopropyl)‐3‐(4‐[4‐oxo‐2‐phenylthiazolo din‐3‐yl]phenyl)quinazolin‐4(3H)‐one 7a‐7l were synthesized and characterized by IR, 1H‐NM...
Hit, Lead & Candidate Discovery
A series of 2‐(2‐substituted benzylidenehydrazinyl‐2‐oxopropyl)‐3‐(4‐[4‐oxo‐2‐phenylthiazolo din‐3‐yl]phenyl)quinazolin‐4(3H)‐one 7a‐7l were synthesized and characterized by IR, 1H‐NMR, 13C‐NMR, mass spectroscopy and elemental analyses. In this present study, the density functionality theory was performed to identify drug stability. Further we introduced graph theoretical analysis by utilised Kyoto Encyclopedia of Genes and Genomes (KEGG) database and Cytoscape software to identify drug target. Based on the observed drug target insilico modeling was executed to know effective drug. The antiepileptic effects of title compounds were evaluated by using MES and subcutaneous pentylenetetrazole (scPTZ) test. Acute neurological toxicity of title compounds was studied by using standardized rotorod test. After 0.5 hr of period many of the compounds showed anticonvulsant activity at MES or scPTZ test. Comparison of the biological activity of test compounds with its chemical structures indicates that, compounds possessing electron donating group exhibited superior activity than the analogs having electron withdrawing moieties. Among the electron donating group tested, amino derivative exhibited good activity than rest of derivatives. From the study it was concluded that, the compound 7j was established as very potent compared with rest of the compounds and standard drugs subjected to biological studies. Thus the compound 2‐(2‐[4‐aminobenzylidene]hydrazinyl‐2‐oxopropyl)‐3‐(4‐[4‐oxo‐2‐phenylthiazolidin‐3‐yl]phenyl) quinazolin‐4(3H)‐one (7j) came out as pilot derivative without any neurotoxicity with a wide spectrum of antiepileptic activity.
The performed work is having great significance in terms of
Graph theoretical analysis used to identify drug target
In silico modeling used to identify designed drug interaction with identify target
Density functionality studies used to identify synthesized compound energy band gap which is correlate with enhancement of its biological activity
Antiepileptic effects of entire synthesized quinazolinone scaffolds were evaluated by MES and scPTZ test
2‐(2‐[4‐aminobenzylidene]hydrazinyl‐2‐oxopropyl)‐3‐(4‐[4‐oxo‐2‐phenylthiazolidin‐3‐yl]phenyl) quinazolin‐4(3H)‐one (7j) was established as very potent compared to the rest of the compounds and standard drugs which were subjected to biological studies
Cover image, volume 79, issue 6