Synthesis and pharmacological investigation of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a] quinazolin-5-ones as a new class of H1-antihistaminic agents

Alagarsamy, V.; Kavitha, K.; M, Rupesh Kumar; Solomon, V. Raja; Kumar, Jaya; Kumar, Dinakaran Sathesh; Sharma, Hemant

doi:10.2478/v10007-009-0003-1

Cited by 8 publications

(25 citation statements)

References 7 publications

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“…Derivatives of [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one showed the H1-antihistaminic [1][2][3][4][5][6][7][8][9], anticonvulsant [10], antiHIV [11], anticancer [12], anti-asthmatic [8,13], antiallergic [13], anti-inflammatory [13, 14] bioactivities. 1-Alkyl-3-aryl [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones demonstrated moderate antibacterial [11,12] including antitubercular [12] and antifungal [11] properties.…”

Section: Analysis Of Recent Studies and Publications In Which A Solutmentioning

confidence: 99%

Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

Danylchenko¹,

Drushlyak²,

Коваленко³

et al. 2016

ScienceRise

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Otsenka adgezivnykh svoystv spor vaktsinnykh shtammov Bacillus Anthracis na eritrotsitakh mlekopitayushchikh s pomoshch'yu fotokolorimetrii [Evaluation of adhesive properties of spore vaccine strains of Bacillus Anthracis on erythrocytes of mammals using photocolorimetry]. Problemy osobo opasnykh infektsiy, 110, 41-43. 11. Makhrova, T. V., Zaslavskaja, M. Y., Majanskyj, A. N. (2004). Vliyanie metabolitov stafilokokkov na adgezivnye reaktsii v sisteme «Candida albicansbukkal'nye epiteliotsity» [Influence of staphylococcal metabolites on reaction adhesive system "Candida albicansbuccal epithelial cells]. ZhMEI, 5, 4-7. 12. Khyzhnyak, O. S. (2015). Vyvchennya adhezyvnykh vlastyvostey bifidobakteriy ta laktobatsyl pry sumisnomu kul'tyvuvanni [Study of adhesive properties of bifidobacteria and lactobacilli in the joint cultivation]. Farmakom, 1, 71-74. 13. Anisimov, T. I., Bukovskaja, S. N. et. al (1989). Rukovodjashhij dokument po standartizacii. rD 42-28-8-89 / Doklinicheskie ispytanija novyh medicinskih immunobiologicheskih preparatov [Guidance document on standardization. 42-28-8-89 pA / Pre-clinical testing of new medical immunobiological preparations]. Moscow, 31. 14. Khyzhnyak, O. S. (2015). Rozrobka skladu kapsul'noyi masy profilaktychnoho zasobu na osnovi probiotychnykh bakteriy [Development of the capsule mass of drug based on probiotic bacteria]. Farmakom, 3-4, 43-48.

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Section: Analysis Of Recent Studies and Publications In Which A Solutmentioning

confidence: 99%

Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

Danylchenko¹,

Drushlyak²,

Коваленко³

et al. 2016

ScienceRise

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“…Derivatives of [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-one are representatives of important class of condensed heterocycles possessing wide biological activity range. Among their potential pharmacologically significant properties, the antibacterial [2,10,13], antitubercular [2,13], antifungal [2,10], anti-HIV [2], antihistaminic [3,4,5,6,14,15], anticonvulsant [1], anticancer [13], antiasthmatic [12,14], antiallergic [12], anti-inflammatory [11,12] bioactivities should be mentioned. Hence, it was of interest to check some [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-one derivatives against tropical disease protozoa.…”

Section: Introductionmentioning

confidence: 99%

“…Among their potential pharmacologically significant properties, the antibacterial [2,10,13], antitubercular [2,13], antifungal [2,10], anti-HIV [2], antihistaminic [3,4,5,6,14,15], anticonvulsant [1], anticancer [13], antiasthmatic [12,14], antiallergic [12], anti-inflammatory [11,12] bioactivities should be mentioned. Hence, it was of interest to check some [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-one derivatives against tropical disease protozoa. The aim of this study was to evaluate [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-one derivatives containing an amide group that was connected to 1 position of triazoloquinazoline moiety via sulfur-carbon or carbon chain against tropical parasitic protozoa Leishmania, Plasmodium and Trypanosoma.…”

Section: Introductionmentioning

confidence: 99%

“…Hence, it was of interest to check some [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-one derivatives against tropical disease protozoa. The aim of this study was to evaluate [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-one derivatives containing an amide group that was connected to 1 position of triazoloquinazoline moiety via sulfur-carbon or carbon chain against tropical parasitic protozoa Leishmania, Plasmodium and Trypanosoma.…”

Section: Introductionmentioning

confidence: 99%

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[1,2,4]triazolo[4,3-a]quinazolin-5-one deriva tives as antimalarial agents

et al. 2016

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Five novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives containing an amide group connected to 1 position of triazoloquinazoline moiety via sulfur-carbon or carbon chain were synthesized. The structure was confirmed by elemental analysis and 1 H NMR spectroscopy. Their in vitro antiprotozoal activity was evaluated against Leishmania infantum, Plasmodium falciparum, Trypanosoma brucei and Trypanosoma cruzi. 4-Benzyl-1-{4-[4-(4-methoxyphenyl)piperazin-1-yl]-4-oxobutyl}[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one 7e with an amide group connected via carbon chain showed noticeable antimalarial activity (IC 50 0.2 µM). The lead structure 7e may be promising for further investigations as novel antimalarial agents.

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“…Compound ( [66][67][68]. It was found that by varying substitution over the first position of the triazolo quinazoline (52) ring there was variation in the biological activity.…”

Section: Compound 50mentioning

confidence: 99%

A Review on a Highly Important Hetrocycle Quinazolinone Compounds and their Diverse Biological Activities

2016

European Reviews of Chemical Research

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Quinazolinone and their derivatives have been studied extensively for various biological activities such as anti-inflammatory, antimicrobial, anticancer, anticonvulsant and anti-HIV activity etc. The purpose of this review was to collate literature work reported by researchers on quinazoline for their various pharmacological activities. Quinazolinone derivatives are one of the most active classes of compounds possessing a wide spectrum of biological activity. Recently several scientists have been reported that introduction of various heterocyclic moieties at quinazolinone nucleus modulate the activity. Various derivatives of quinazolinone have been synthesized and evaluated for their biological activities. This review might be helpful in the development of these novel lead molecules to potential drug candidates for future prospect.Keywords: Quinazoline, antimicrobial, Anti HIV, Anti cancer, biologically active. IntroductionHeterocyclic chemistry comprises at least half of all organic chemistry research worldwide. In particular, heterocyclic structures form the basis of many pharmaceutical, agrochemical and veterinary products. Quinazoline (1) are classes of fused heterocycles that are of considerable interest because of the diverse range of their biological activities such as, antimicrobial, anticancer, anticonvulsant, anti-tubercular, etc [1][2][3][4][5]. Quinazolin is a heterocyclic compound consists of two fused six membered simple aromatic rings, a benzene ring and a pyrimidine ring. The quinazolin nucleus has attracted the attention of medicinal chemists due to its well known anticancer activity, and many substituted quinazolin derivatives have recently earned great interest in chemotherapy as antitumor drugs [6]. Pharmacologically quinazolin particularly quinazolin-4-one (2) or quinazolinone are the most important classes of heterocyclic compounds. Quinazolin-4-one is synthesized when the keto group is introduced in the pyrimidine ring of quinazolin. Quinazolinone compounds possess versatile biological activities; such as anticancer [7][8]

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Synthesis and pharmacological investigation of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a] quinazolin-5-ones as a new class of H1-antihistaminic agents

Cited by 8 publications

References 7 publications

Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

[1,2,4]triazolo[4,3-a]quinazolin-5-one deriva tives as antimalarial agents

A Review on a Highly Important Hetrocycle Quinazolinone Compounds and their Diverse Biological Activities

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