Quinazolines: New horizons in anticonvulsant therapy

Ugale, Vinod G.; Bari, Sanjay B.

doi:10.1016/j.ejmech.2014.04.072

Cited by 159 publications

(84 citation statements)

References 54 publications

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“…As new horizons in anticonvulsant therapy, the quinazolines and quinazolinone structural class has been proved to be useful for the design and development of potent anticonvulsant agents [27,28].…”

Section: The Quinazoline or Quinazolinone Functional Groupsmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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Epilepsy affects about 1% of the world's population. Due to the fact all antiepileptic drugs (AEDs) have some undesirable side effects and about 30% of epileptic patients are not seizure-free with the existing AEDs, there is still an urgent need for the development of more effective and safer AEDs. Based on our research work on antiepileptic compounds and other references in recent years, this review covers the reported work on antiepileptic compounds which are classified according to their structures. This review summarized 244 significant anticonvulsant compounds which are classified by functional groups according to the animal model data, although there are some limitations in the data. This review highlights the properties of new compounds endowed with promising antiepileptic properties, which may be proven to be more effective and selective, and possibly free of unwanted side effects. The reviewed compounds represent an interesting possibility to overcome refractory seizures and to reduce the percentage of patients with a poor response to drug therapy.

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Section: The Quinazoline or Quinazolinone Functional Groupsmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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“…Виявлений ряд високоактивних сполук (1.6, 1.11, 1.12, 1.18, 1.19, 1.25), що за рівнем актопротекторної активності перевищують референс-препарат «Мілдро-нат» на 13,2-47,8 %. Показано, що вірогідної залежності між актопротекторною та антирадикальною активністю серед 3'-R-cпіро[циклоалкіл-1(2), (гетарил-3(4), 6')- [1,2,4]триазино [2,3-c]хіназолін]-2'(7'H)-2-онів немає. Аналіз взаємозв'язку «структура -активність» показав: критичними факторами у прояві високої актопротекторної дії є не тільки розмір і природа спіроциклу положення 6, а також замісник положення 3 триазино [2,3- Хиназолины и их производные -перспективный класс соединений с разнообразной биологической активностью, пред-ставители которого используются в медицинской практике в качестве снотворных, диуретических, противомикробных, противоопухолевых препаратов.…”

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“…Цель работы -первичный скрининг 3'-R-спиро[циклоалкил-1(2), (гетарил-3(4), 6')- [1,2,4]триазино[2,3-c]хиназо-лин]-2'(7'H)-2-онов на актопротекторную активность, изучение антирадикального действия как вероятного механизма проявления актопротекции и потенциальных высокоактивных соединений для дальнейшего углублённого изучения.…”

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“…Актопротекторная активность перспективных и неизвестных 3'-R-спиро[циклоалкил-1(2), (гетарил-3(4), 6')- [1,2,4]триазино [2,3-c]хиназолин]-2'(7'H)-2-онов была изучена с использованием теста плавательной пробы при температуре 24-26 °C (нормотермия) с дополнительной нагрузкой (10 % от массы тела экспериментальных животных). Исследования проведены на белых крысах линии Вистар, в качестве референс-препарата использован «Милдронат».…”

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“…Обнаружен ряд высокоэффективных соединений (1.6, 1.11, 1.12, 1.18, 1.19, 1.25), которые по уровню актопротекторной активности превышают референс-препарат «Милдронат» на 13,2-47,8 %. Показано, что достоверной зависимости между актопро-текторной и антирадикальной активностью среди 3'-R-cпиро[циклоалкил-1(2), (гетарил-3(4), 6')- [1,2,4] Quinazolines and its derivatives as perspective objects of structural modification and functionalization aimed to search for novel bioactive substances attract attention of scientists more and more [1][2][3][4]. Since their first synthesis in 1869, identifying the main quinazoline alkaloids and creation of drugs with diverse biological activity only 150 years have passed [5].…”

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3'-R-Spiro[cycloalkyl-1(2), (hetaryl-3(4), 6'-[1,2,4]triazino[2,3-c]quinazoline]-2'(7'H)-2-оnes as a perspective class of compounds with actoprotective activity

Kolomoets

Voskoboynik

Носуленко

et al. 2017

ZMJ

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C−N Cross‐Coupling Reactions Under Mild Conditions Using Singlet Di‐Radical Nickel(II)‐Complexes as Catalyst: N‐Arylation and Quinazoline Synthesis

et al. 2019

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Herein we report a cost-effective synthetic approach for CÀ N cross-coupling reactions of a broad array of nitrogen nucleophiles and aryl halides under mild conditions. These reactions are catalyzed by an inexpensive, air-stable, earth-abundant and easy-to-prepare singlet di-radical nickel(II)-catalyst containing two antiferromagnetically coupled single-electron oxidized diiminosemiquinonato type ligands. This protocol provides an alternative method for CÀ N cross-coupling reactions avoiding nickel(0)/nickel(II) or nickel(I)/ nickel(III) redox processes via cooperative participation of metal and ligand-centered redox events. Besides a wide range of N-arylation reactions, by judicious choice of aryl halides and nitrogen nucleophiles the synthesis of a variety of polysubstituted quinazolines has been achieved in moderate to good yields under relatively mild reaction conditions. Our catalyst has been found to be almost equally effective in quinazoline synthesis via CÀ N cross-coupling of (i) 2-bromobenzylamine with benzamide, and (ii) 2-bromobenzylbromide with amidine. Control experiments and DFT studies were performed to improve the understanding of the cooperative participation of ligand and metal (nickel)-centered redox events during oxidative addition/reductive elimination processes of the catalytic cycle and to shed light on the plausible mechanistic pathway of the CÀ N crosscoupling reactions.

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Quinazolines: New horizons in anticonvulsant therapy

Cited by 159 publications

References 54 publications

Current Research on Antiepileptic Compounds

Current Research on Antiepileptic Compounds

3'-R-Spiro[cycloalkyl-1(2), (hetaryl-3(4), 6'-[1,2,4]triazino[2,3-c]quinazoline]-2'(7'H)-2-оnes as a perspective class of compounds with actoprotective activity

C−N Cross‐Coupling Reactions Under Mild Conditions Using Singlet Di‐Radical Nickel(II)‐Complexes as Catalyst: N‐Arylation and Quinazoline Synthesis

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