Synthesis and biological activity of novel antibacterial quinazolines

Bedi, Preet Mohinder Singh; Kumar, Vipan; Mahajan, Mohinder P.

doi:10.1016/j.bmcl.2004.07.065

Cited by 113 publications

(48 citation statements)

References 13 publications

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“…It is a ketone derivative of tetralin having the molecular formula C 10 H 10 O. Tetrahydronaphthyl-heterocycle 1 has useful applications such as anticancer [2][3][4][5][6] , antimicrobial [7][8][9] , antiviral [10][11] , moluscidal 12 , schistosomicidal [13][14] and analgesic 15 . The present work deals with synthesis of some benzylidiene derivatives using 6-methoxy tetralone as a key starting material and these benzylidiene derivatives were further condensed with thiourea to give quinazoline thione derivatives which were evaluated for antifungal activity.…”

Section: 4-dihydro-1(2h)-naphthalenone Is Chemical Name Of Tetralomentioning

confidence: 99%

Synthesis, Characterization and Antifungal Activity of Quinazoline Thione Derivatives of 3, 4-Dihydro-1(2h)-Naphthalenone

Arora¹,

Nagori²

2014

Int. Res. J. Pharm.

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A series of 2-substituted benzylidene-tetralone was prepared from 6-methoxy-tetralone by using an Aldol condensation and then these synthesized benzylidene-tetralone derivatives were further condensed with thiourea to give various substituted quinazoline thione derivatives. All of these compounds have been characterized by IR, NMR and Mass spectral analysis for structure establishment and further evaluated for their antifungal activity against Aspergillus niger (MTCC-282) and Candida albicans (MTCC-227) by agar diffusion method using fluconazole as standard drug. Among 6-methoxy-benzylidiene derivatives; C1, C2, C7 were least active and C3, C4, C5, C6 were moderately active while among quinazoline thione derivatives; C8, C9 were least active and C10, C11, C12, C13 were moderately active. When electron-withdrawing substitutions were made on both ring antifungal activity increased in (NO2 > F> Cl) order. The maximum zone of inhibition (60.7 % and 69.7 %) was shown by compound C5 among 6-methoxy-benzylidiene derivative and C11 had (72 % and 73 %) activity among quinazoline thione derivative against Aspergillus niger and Candida albicans respectively.

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Section: 4-dihydro-1(2h)-naphthalenone Is Chemical Name Of Tetralomentioning

confidence: 99%

Synthesis, Characterization and Antifungal Activity of Quinazoline Thione Derivatives of 3, 4-Dihydro-1(2h)-Naphthalenone

Arora¹,

Nagori²

2014

Int. Res. J. Pharm.

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“…Kinazolin türevlerinin pek çok ve çeşitli biyolojik özellikleri, bu bileşiklerin sentezi ve kullanım alanlarının araştırılmasını yıllardır ilgi odağı haline getirmiştir. Bu grubu içeren bileşikler diüretik, antihipertansif, antibiyotik, antiinflamatuar, antikonvülsan, antibakteriyel ve antitümör gibi pek çok farmakolojik aktivite gösterirler [4][5][6][7][8][9][10][11][12].…”

Section: Introductionunclassified

Bis{3-(2-amino-benzilimino)-pentan-2-on oksimato}kobalt(III) sakkarinat monohidrat kompleksinin sentezi, karakterizasyonu ve teermal özellikleri

Gençkal

2017

Balıkesir Üniversitesi Fen Bilimleri Enstitüsü Dergisi

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“…Quinazoline derivatives, endowed with a broad spectrum of biological activities and therapeutic properties, have shown promise as anti-bacterial, anti-fungal, antitumor, anti-inflammatory, anti-virus and anti-rheumatic drugs (Agarwal et al 2009;Bedi et al 2004;Foote et al 2008;Mohamed et al 2010). Such promising potential allows quinazoline derivatives to become good candidates for further pharmaceutical applications.…”

mentioning

confidence: 99%

Multiparameter-Based Bioassay of 2-(4-Chlorophenyl)-4-(4-methoxyphenyl) Quinazoline, a Newly-Synthesized Quinazoline Derivative, Toward Microcystis aeruginosa HAB5100 (Cyanobacteria)

Zhao

Liu

et al. 2015

Bull Environ Contam Toxicol

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Quinazoline derivatives have wide biological activities and therapeutic properties, implying their potential for development and application on a large scale. In the present study, 2-(4-chlorophenyl)-4-(4-methoxyphenyl) quinazoline (CMQ), was selected to examine its effect on unicellular cyanobacteria, Microcystis aeruginosa by evaluating growth, physiological and molecular responses. Growth was inhibited by CMQ, with a 96 h EC 50 of 1.93 ± 0.19 mg L -1 . The up-regulated expression of prx was shown, reflecting that oxidative stress might be a toxic factor of CMQ. At higher concentrations of CMQ, the quantum yields of Y(II) and Y(NPQ) in photosystem II decreased seriously and Y(NO) increased sharply, and psbA gene encoding for D1 protein was over-expressed. These results demonstrated that high concentrations of CMQ had different inhibitory targets associated with photosystem electron transport and with sites beyond the electron transport chain, leading to severe toxicity.

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Synthesis and biological activity of novel antibacterial quinazolines

Cited by 113 publications

References 13 publications

Synthesis, Characterization and Antifungal Activity of Quinazoline Thione Derivatives of 3, 4-Dihydro-1(2h)-Naphthalenone

Synthesis, Characterization and Antifungal Activity of Quinazoline Thione Derivatives of 3, 4-Dihydro-1(2h)-Naphthalenone

Bis{3-(2-amino-benzilimino)-pentan-2-on oksimato}kobalt(III) sakkarinat monohidrat kompleksinin sentezi, karakterizasyonu ve teermal özellikleri

Multiparameter-Based Bioassay of 2-(4-Chlorophenyl)-4-(4-methoxyphenyl) Quinazoline, a Newly-Synthesized Quinazoline Derivative, Toward Microcystis aeruginosa HAB5100 (Cyanobacteria)

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