Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs

Bhandari, Shashikant V.; Dangre, Sudarshan C.; Bothara, Kailash G.; Patil, Ajit; Sarkate, Aniket P.; Lokwani, Deepak K.; Gore, Suraj T; Deshmane, Bhavana J.; Raparti, Vyankatesh T.; Khachane, Chetan V.

doi:10.1016/j.ejmech.2009.06.035

Cited by 38 publications

(25 citation statements)

References 24 publications

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“…Anti-tumor activities are also reported for 2,3-dihydro-2-aryl-4-quinazolines [13,14]. Several quinazoline derivatives have been reported for their antibacterial, antifungal, anti-Human Immunodeficiency Virus (HIV) [15,16], anthelmintic [17], central nervous system depressant [18], antitubercular [19], hypotensive [20], anticonvulsant [21], anti-fibrillatory [22], diuretic [23] and antiviral activities [24][25][26]. Some reports have suggested that 2-styrylquinazolin-4-ones [27,28] could be effective inhibitors of tubulin polymerization.…”

Section: Introductionmentioning

confidence: 96%

Vibrational spectra and computational study of 3-amino-2-phenyl quinazolin-4(3H)-one

Panicker¹,

Varghese

Ambujakshan³

et al. 2010

Journal of Molecular Structure

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Section: Introductionmentioning

confidence: 96%

Vibrational spectra and computational study of 3-amino-2-phenyl quinazolin-4(3H)-one

Panicker¹,

Varghese

Ambujakshan³

et al. 2010

Journal of Molecular Structure

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“…They are used in medicine because of their wide spectrum of biological activities such as antitumor, antibacterial and antifungal, antimicrobial activities (Pendergast et al, 1993). Several quinazoline derivatives have been reported for their antibacterial, antifungal, anti-Human Immunodeficiency Virus (HIV) (Alagarsamy et al, 2006), anti-inflammatory (Alagarsamy et al, 2006), anticonvulsant (Gupta et al, 1988), antidepressant (Jatav et al, 2008), hypolipidemic (Joshi and Chaurasia, 1987), antiulcer (Prouse, 1993), analgesic (Bhandari et al, 2008) or immunotropic activities (Azza et al, 2004). Some of the aminoquinazoline derivatives were found to be inhibitors of the tyrosine kinase (Fry et al, 1994) or dihydrofolate reductase enzymes (Traxler et al, 1996) and so they work as potent anticancer agents.…”

Section: Introductionmentioning

confidence: 98%

Synthesis, characterization and density functional theory investigations of the N,N-diacylaniline derivatives

Al‐Sehemi

Alamri

2017

Arabian Journal of Chemistry

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Different N,N-diacylaniline derivatives such as N-acetyl-N-(2have been synthesized and characterized by FTIR and NMR techniques. The ground state geometries have been optimized by using density functional theory (DFT) at B3LYP/6-31G* level. The frequencies have been computed at the same level of theory. To shed light on the rotational barrier, the electron correlation has been taken into account. The steric effect of o-substituents twists the aromatic ring out of planarity with the imide moieties, creating an axis of chirality. The introduction of different substituents on the benzene ring causes some changes in the ring C-C bond distances. The observed vibrational assignments and analysis of DAA (2f) have been discussed in terms of fundamental bands.ª 2013 Production and hosting by Elsevier B.V. on behalf of King Saud University.

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“…In the past decade, numerous advances have taken place in the understanding of pathogenesis and as a result, significant progress has been made and is still being made in the development of novel anti-inflammatory drugs (Bhandari et al, 2009). Inflammation is a fundamental physiological process that is essential for survival but at the same time is one of the major causes of human morbidity and mortality (O'Neill, 2006;Cheeseright et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Microwave assisted synthesis of novel pyrazolone derivatives attached to a pyrimidine moiety and evaluation of their anti-inflammatory, analgesic and antipyretic activities

Antre¹,

Cendilkumar²,

Goli³

et al. 2011

Saudi Pharmaceutical Journal

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In the present research work, the motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antipyretic agents. Various 4-(2-amino-6-(substituted)pyrimidin-4-yl)-3-methyl-1-(substituted)-1H-pyrazol-5(4H)-one derivatives (5a-5j) and their Schiff bases (6a-6j) were synthesized. The newly synthesized compounds were characterized by TLC and spectral data. The compounds containing pyrazolone and amino pyrimidine as basic moieties (5a-5j), were screened for their anti-inflammatory, analgesic and antipyretic activities, compounds 5a, 5c-5f, 5h exhibited activities nearly similar to the standard. The pharmacological studies reveal that the presence of 4-hydroxy, 4-methoxy, 4-(N,N-dimethylamino) or 2-hydroxy groups on phenyl ring at C6 of amino pyrimidine exhibits anti-inflammatory, analgesic and antipyretic activities nearly similar to the standard and substitutions like 4-chloro, 2-nitro, 3-nitro or 4-nitro on same phenyl ring lead to a decrease in activities.

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Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs

Cited by 38 publications

References 24 publications

Vibrational spectra and computational study of 3-amino-2-phenyl quinazolin-4(3H)-one

Vibrational spectra and computational study of 3-amino-2-phenyl quinazolin-4(3H)-one

Synthesis, characterization and density functional theory investigations of the N,N-diacylaniline derivatives

Microwave assisted synthesis of novel pyrazolone derivatives attached to a pyrimidine moiety and evaluation of their anti-inflammatory, analgesic and antipyretic activities

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