Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles.

Literature DB >> 16087337

Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles.

Akihiko Tanitame¹, Yoshihiro Oyamada, Keiko Ofuji, Hideo Terauchi, Motoji Kawasaki, Masaaki Wachi, Jun-ichi Yamagishi.

Abstract

The 2-arylvinyl moiety in 1-(3-chlorophenyl)-3-(4-piperidyl)-5-[(E)-2-(5-chloro-1H-indol-3-yl)vinyl]pyrazole 2, which has previously shown improved DNA gyrase inhibition and target-related antibacterial activity, was transformed to other groups and the in vitro antibacterial activity of the synthesized compounds was evaluated. Many of the 5-[(E)-2-arylvinyl]pyrazoles synthesized in this study exhibited potent antibacterial activity against quinolone-resistant clinical isolates of gram-positive bacteria with minimal inhibitory concentration values equivalent to those against susceptible strains.

Entities: Chemical Gene

Mesh：

Substances：

Year: 2005 PMID： 16087337 DOI： 10.1016/j.bmcl.2005.06.103

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

Keyword Cloud
Cited

10 in total

1. Pyrazolylthiazole as DeltaF508-cystic fibrosis transmembrane conductance regulator correctors with improved hydrophilicity compared to bithiazoles.

Authors: Long Ye; John M Knapp; Panjamaporn Sangwung; James C Fettinger; A S Verkman; Mark J Kurth
Journal: J Med Chem Date: 2010-05-13 Impact factor: 7.446

Review 2. Challenges of antibacterial discovery.

Authors: Lynn L Silver
Journal: Clin Microbiol Rev Date: 2011-01 Impact factor: 26.132

3. The challenge of developing robust drugs to overcome resistance.

Authors: Amy C Anderson; Michael P Pollastri; Celia A Schiffer; Norton P Peet
Journal: Drug Discov Today Date: 2011-07-19 Impact factor: 7.851

4. Microwave Assisted Synthesis of 1-[5-(Substituted Aryl)-1H-Pyrazol-3-yl]-3,5-Diphenyl-1H-1,2,4-Triazole as Antinociceptive and Antimicrobial Agents.

Authors: Shantaram Gajanan Khanage; Popat Baban Mohite; Ramdas Bhanudas Pandhare; S Appala Raju
Journal: Adv Pharm Bull Date: 2013-12-24

5. Crystal structure of 6-amino-4-(3-bromo-4-meth-oxy-phen-yl)-3-methyl-2,4-di-hydro-pyrano[2,3-c]pyrazole-5-carbo-nitrile dimethyl sulfoxide monosolvate.

Authors: Sammer Yousuf; Huma Bano; Munira Taj Muhammad; Khalid Mohammed Khan
Journal: Acta Crystallogr E Crystallogr Commun Date: 2015-06-06

Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles.

1. Pyrazolylthiazole as DeltaF508-cystic fibrosis transmembrane conductance regulator correctors with improved hydrophilicity compared to bithiazoles.

Review 2. Challenges of antibacterial discovery.

3. The challenge of developing robust drugs to overcome resistance.

4. Microwave Assisted Synthesis of 1-[5-(Substituted Aryl)-1H-Pyrazol-3-yl]-3,5-Diphenyl-1H-1,2,4-Triazole as Antinociceptive and Antimicrobial Agents.

5. Crystal structure of 6-amino-4-(3-bromo-4-meth-oxy-phen-yl)-3-methyl-2,4-di-hydro-pyrano[2,3-c]pyrazole-5-carbo-nitrile dimethyl sulfoxide monosolvate.

6. Crystal structure of 1-(2,4-di-nitro-phen-yl)-3,5-diphenyl-1H-pyrazole.

7. Microwave-assisted one pot three-component synthesis of some novel pyrazole scaffolds as potent anticancer agents.

8. Biological Validation of Novel Polysubstituted Pyrazole Candidates with in Vitro Anticancer Activities.

9. Pyrazoles and Pyrazolines as Anti-Inflammatory Agents.

10. PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer.