Synthesis and pharmacological study of ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates

Maggio, Benedetta; Daidone, Giuseppe; Raffa, Demetrio; Plescia, Salvatore; Mantione, Lucilla Maria Grazia; Cutuli, V. M. C.; Mangano, Nunzio Guido; Caruso, A.

doi:10.1016/s0223-5234(01)01259-4

Cited by 96 publications

(28 citation statements)

References 9 publications

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“…Many show remarkable biological activity [7][8][9][10][11][12][13]. Pyrazole-functionalized silica is applied for quantitative extraction and elimination of Pb II from natural water [14], while trinitropyrazole derivatives were considered as potential candidates for high-energy density materials [15].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, structure and thermokinetic studies on perchlorate salts of metal complexes containing a formamidine-type ligand

Holló

Jašo

Leovac

et al. 2013

Journal of Coordination Chemistry

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2013) Synthesis, structure and thermokinetic studies on perchlorate salts of metal complexes containing a formamidine-type ligand, Journal of Coordination Chemistry, 66:3, 453-463, Two formamidine-type transition metal complexes of N,N′-bis(4-acetyl-5-methylpyrazol-3-yl) formamidine (ampf) have been synthesized by a template reaction in methanolic solution of the corresponding metal perchlorates and 4-acetyl-3-amino-5-methylpyrazole (aamp) precursor in the presence of triethyl orthoformate. Compounds of composition [M(ampf)(H 2 O) 3 ](ClO 4 ) 2 ·H 2 O (M = Co II , Ni II ) have been formed. The crystal and molecular structures of the compounds have been determined by X-ray crystallography. The complexes were characterized by IR spectroscopy. The thermal stability and the decomposition kinetics of the two potential explosives were determined by thermal methods.

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Section: Introductionmentioning

confidence: 99%

Synthesis, structure and thermokinetic studies on perchlorate salts of metal complexes containing a formamidine-type ligand

Holló

Jašo

Leovac

et al. 2013

Journal of Coordination Chemistry

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“…The medical importance of pyrazole derivatives is indicated by the large number of reports documenting their various biological activities, such as reported antitumor [16 -18], anti-inflammatory [19,20], ulcerogenic [21], antiviral [22], immunosupressant [23], and antimicrobial activities [17, 24 -27]. Some members of this class of compounds have also been investigated for their local anaesthesic and antiarrhythmic [28], herbicidal [29], and molluscicidal [30] properties.…”

Section: Introductionmentioning

confidence: 99%

Antileishmanial and Antibacterial Activity of a New Pyrazole Derivative Designated 4‐[2‐(1‐(Ethylamino)‐2‐methyl‐ propyl)phenyl]‐3‐(4‐methyphenyl)‐1‐phenylpyrazole

Dardari

Lemrani

Sebban

et al. 2006

Archiv der Pharmazie

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Here, we report for the first time the synthesis and the antileishmanial activity of a new pyrazole derivative, namely 4-[2-(1-(ethylamino)-2-methylpropyl)phenyl]-3-(4-methyphenyl)-1-phenylpyrazole). Micromolar concentrations of this compound were found to inhibit the in vitro multiplication of Leishmania tropica, Leishmania major, and Leishmania infantum, three species causing different forms of leishmaniasis. Furthermore, the 50% inhibitory concentration (IC50) values for the compound are only slightly higher than those of amphotericin B, one of the most active antileishmanial agents used as a satisfactory substitute in cases not responding to pentostam. The IC50 values after 48 h for L. tropica, L. major, and L. infantum promastigote growth were 0.48 microg/mL, 0.63 microg/mL and 0.40 microg/mL, respectively for the compound, while they were 0.23 microg/mL, 0.29 microg/mL and 0.24 microg/mL, respectively for amphotericin B. We also tested this compound for its antibacterial activity against several bacteria. The strongest antibacterial activity was observed against Entrococcus feacalis and Staphylococcus aureus with a minimal inhibitory concentration (MIC) of 60 microg/mL.

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“…Various quinazolines exhibited antimicrobial (Jantová et al 2005), antiinflammatory, diuretic, anticonvulsant, antiallergic, antihypertensive, antiparkinsonian, and anticancer effects (Chao et al 1999;Maggio et al 2001). Some medicinal applications of the quinazoline derivatives were reported for Doxazosin (Natale 2004), Gefitinib, Tomudex, BIBN 4096 BS, and R115777 (Schwartz et al 2004) being antihypertension, anticancer R. Ovádeková et al 2626 and antimigraine drugs.…”

Section: Introductionmentioning

confidence: 99%

Detection of the Effective DNA Protection by Quinazolines Using a DNA‐Based Electrochemical Biosensor

2005

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A DNA biosensor can serve as a powerfull tool during simple in vitro tests of chemical toxicity. In this paper, damage to dsDNA attached to the surface of a screen-printed carbon electrode by acridine orange (AO) in 5 Â 10 23 M phosphate buffer solution and an effective DNA protection by selected quinazolines are described. Damage to DNA was detected using voltammetric signals of the dsDNA guanine moieties. Using the Co(III) complex with 1,10-phenanthroline, [Co(phen) 3 ] 3þ , as an electrochemical DNA marker, the portion of original dsDNA that survives an incubation of the biosensor in the medium of AO and quinazolines was evaluated. The quinazoline derivatives under study were found to be very effective DNA protectors, particularly at low concentration level. The results were confirmed by microbiological tests with green seaweed, Euglena gracilis, as well as by conventional electrophoretic experiments.

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Synthesis and pharmacological study of ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates

Cited by 96 publications

References 9 publications

Synthesis, structure and thermokinetic studies on perchlorate salts of metal complexes containing a formamidine-type ligand

Synthesis, structure and thermokinetic studies on perchlorate salts of metal complexes containing a formamidine-type ligand

Antileishmanial and Antibacterial Activity of a New Pyrazole Derivative Designated 4‐[2‐(1‐(Ethylamino)‐2‐methyl‐ propyl)phenyl]‐3‐(4‐methyphenyl)‐1‐phenylpyrazole

Detection of the Effective DNA Protection by Quinazolines Using a DNA‐Based Electrochemical Biosensor

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