Literature DB >> 23960745

Synthesis, characterization, and antimicrobial evaluation of carbostyril derivatives of 1H-pyrazole.

Nilesh J Thumar1, Manish P Patel.   

Abstract

A new series of 12 derivatives of 4-pyrazolyl-N-arylquinoline-2,5-dione (4a-l) were synthesized by one pot base catalyzed cyclocondensation reaction of 1-aryl-5-chloro-3-methyl-1H-pyrazole-4-carbaldehyde (1a-c), Meldrum's acid (2) and 3-arylamino-5,5-disubstitutedcyclohex-2-enone (3a-d). All the compounds were characterized by elemental analysis, FT-IR, (1)H NMR and (13)C NMR spectral data and were screened, against six bacterial pathogens, namely Bacillus subtilis, Clostridium tetani, Streptococcus pneumoniae, Salmonella typhi, Vibrio cholerae, Escherichia coli and antifungal activity, against two fungal pathogens Aspergillus fumigatus and Candida albicans, using broth microdilution MIC (minimum inhibitory concentration) method. Some of the compounds were found to be equipotent or more potent than commercial drugs, against most of the employed strains, as evident from the screening data.

Entities:  

Keywords:  1H-Pyrazole-4-carbaldehyde; Antimicrobial activity; Carbostyril; Minimum inhibitory concentration; Multicomponent reaction

Year:  2011        PMID: 23960745      PMCID: PMC3745187          DOI: 10.1016/j.jsps.2011.01.005

Source DB:  PubMed          Journal:  Saudi Pharm J        ISSN: 1319-0164            Impact factor:   4.330


  24 in total

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2.  A quinolone alkaloid with antioxidant activity from the aleurone layer of anthocyanin-pigmented rice.

Authors:  H S Chung; W S Woo
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3.  Synthesis and antifungal activity of a ferrocene-fluconazole analogue.

Authors:  C Biot; N François; L Maciejewski; J Brocard; D Poulain
Journal:  Bioorg Med Chem Lett       Date:  2000-04-17       Impact factor: 2.823

4.  4-hydroxymethyl-1,6,8-trimethylfuro[2,3-h]quinolin-2(1H)-one induces mitochondrial dysfunction and apoptosis upon its intracellular oxidation.

Authors:  Adriana Chilin; Giuliano Dodoni; Christian Frezza; Adriano Guiotto; Vera Barbieri; Fabio Di Lisa; Marcella Canton
Journal:  J Med Chem       Date:  2005-01-13       Impact factor: 7.446

5.  Quinolone alkaloids with nitric oxide production inhibitory activity from Orixa japonica.

Authors:  Chihiro Ito; Masataka Itoigawa; Akiko Furukawa; Takashi Hirano; Tomiyasu Murata; Norio Kaneda; Youichi Hisada; Kazuyo Okuda; Hiroshi Furukawa
Journal:  J Nat Prod       Date:  2004-11       Impact factor: 4.050

6.  Conversion of some 2(3H)-furanones bearing a pyrazolyl group into other heterocyclic systems with a study of their antiviral activity.

Authors:  Ahmed I Hashem; Ahmed S A Youssef; Kamal A Kandeel; Wael S I Abou-Elmagd
Journal:  Eur J Med Chem       Date:  2007-01-14       Impact factor: 6.514

7.  Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.

Authors:  Christian Peifer; Robert Urich; Verena Schattel; Mohammed Abadleh; Marc Röttig; Oliver Kohlbacher; Stefan Laufer
Journal:  Bioorg Med Chem Lett       Date:  2008-01-05       Impact factor: 2.823

8.  Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.

Authors:  Pi Cheng; Quan Zhang; Yun-Bao Ma; Zhi-Yong Jiang; Xue-Mei Zhang; Feng-Xue Zhang; Ji-Jun Chen
Journal:  Bioorg Med Chem Lett       Date:  2008-05-20       Impact factor: 2.823

9.  Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.

Authors:  Adnan A Bekhit; Hayam M A Ashour; Yasser S Abdel Ghany; Alaa El-Din A Bekhit; Azza Baraka
Journal:  Eur J Med Chem       Date:  2007-04-14       Impact factor: 6.514

10.  Synthesis, antiproliferative, and antiplatelet activities of oxime- and amide-containing quinolin-2(1H)-one derivatives.

Authors:  I-Li Chen; Ken-Ming Chang; Chang-Ling Miaw; Chang-Hui Liao; Jih-Jung Chen; Tai-Chi Wang
Journal:  Bioorg Med Chem       Date:  2007-07-26       Impact factor: 3.641

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  3 in total

1.  5,6-Dimethyl-4-(thio-phen-2-yl)-1H-pyrazolo-[3,4-b]pyridin-3-amine.

Authors:  Hatem A Abdel-Aziz; Khalid A Al-Rashood; Hazem A Ghabbour; Suchada Chantrapromma; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-02-04

2.  3-Acetyl-1,5-diphenyl-1H-pyrazole-4-carbonitrile.

Authors:  Hatem A Abdel-Aziz; Hazem A Ghabbour; Suchada Chantrapromma; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-17

3.  Synthesis and anti-breast cancer evaluation of novel N-(guanidinyl)benzenesulfonamides.

Authors:  Mostafa M Ghorab; Marwa G El-Gazzar; Mansour S Alsaid
Journal:  Int J Mol Sci       Date:  2014-04-01       Impact factor: 5.923

  3 in total

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