Synthesis of some new quinazolin-4(3H)-one derivatives and evaluation of their anticonvulsant activity

Nader M. Boshta; Farag A. El-Essawy; Ramy M. Ammar; Abd El Hamid Ismail; Nancy E. Wahba

doi:10.1007/s00706-016-1710-1

Synthesis of some new quinazolin-4(3H)-one derivatives and evaluation of their anticonvulsant activity

Nader M. Boshta
, Farag A. El-Essawy
, Ramy M. Ammar
, Abd El Hamid Ismail
, Nancy E. Wahba

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Research output: Contribution to journal › Article › peer-review

15 Scopus citations

Abstract

We reported the synthesis of a novel series of quinazolin-4(3H)-one derivatives bearing oxadiazole, thiadiazole, and other moieties in the 3-position of the quinazolinone nucleus using appropriate synthetic route. The compounds were evaluated for their anticonvulsant activity using picrotoxin model, GABA-A receptor antagonist. Five compounds showed significantly prolonged times for convulsions compared with the standard drug phenobarbital. Graphical abstract: [Figure not available: see fulltext.]

Original language	English
Pages (from-to)	2031-2042
Number of pages	12
Journal	Monatshefte fur Chemie
Volume	147
Issue number	11
DOIs	https://doi.org/10.1007/s00706-016-1710-1
State	Published - 1 Nov 2016

Keywords

Anticonvulsant
Drug research
Heterocycles
Quinazolinone
Structure–activity relationships

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10.1007/s00706-016-1710-1

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title = "Synthesis of some new quinazolin-4(3H)-one derivatives and evaluation of their anticonvulsant activity",

abstract = "We reported the synthesis of a novel series of quinazolin-4(3H)-one derivatives bearing oxadiazole, thiadiazole, and other moieties in the 3-position of the quinazolinone nucleus using appropriate synthetic route. The compounds were evaluated for their anticonvulsant activity using picrotoxin model, GABA-A receptor antagonist. Five compounds showed significantly prolonged times for convulsions compared with the standard drug phenobarbital. Graphical abstract: [Figure not available: see fulltext.]",

keywords = "Anticonvulsant, Drug research, Heterocycles, Quinazolinone, Structure–activity relationships",

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T1 - Synthesis of some new quinazolin-4(3H)-one derivatives and evaluation of their anticonvulsant activity

AU - Boshta, Nader M.

AU - El-Essawy, Farag A.

AU - Ammar, Ramy M.

AU - Ismail, Abd El Hamid

AU - Wahba, Nancy E.

PY - 2016/11/1

Y1 - 2016/11/1

N2 - We reported the synthesis of a novel series of quinazolin-4(3H)-one derivatives bearing oxadiazole, thiadiazole, and other moieties in the 3-position of the quinazolinone nucleus using appropriate synthetic route. The compounds were evaluated for their anticonvulsant activity using picrotoxin model, GABA-A receptor antagonist. Five compounds showed significantly prolonged times for convulsions compared with the standard drug phenobarbital. Graphical abstract: [Figure not available: see fulltext.]

AB - We reported the synthesis of a novel series of quinazolin-4(3H)-one derivatives bearing oxadiazole, thiadiazole, and other moieties in the 3-position of the quinazolinone nucleus using appropriate synthetic route. The compounds were evaluated for their anticonvulsant activity using picrotoxin model, GABA-A receptor antagonist. Five compounds showed significantly prolonged times for convulsions compared with the standard drug phenobarbital. Graphical abstract: [Figure not available: see fulltext.]

KW - Anticonvulsant

KW - Drug research

KW - Heterocycles

KW - Quinazolinone

KW - Structure–activity relationships

UR - https://www.scopus.com/pages/publications/84961134127

U2 - 10.1007/s00706-016-1710-1

DO - 10.1007/s00706-016-1710-1

M3 - Article

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SN - 0026-9247

VL - 147

SP - 2031

EP - 2042

JO - Monatshefte fur Chemie

JF - Monatshefte fur Chemie

IS - 11

ER -

Synthesis of some new quinazolin-4(3H)-one derivatives and evaluation of their anticonvulsant activity

Abstract

Keywords

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