Novel antibacterial active quinolone-fluoroquinolone conjugates and 2D-QSAR studies

Siva S Panda; Sumaira Liaqat; Adel S Girgis; Ahmed Samir; C Dennis Hall; Alan R Katritzky

doi:10.1016/j.bmcl.2015.07.077

Novel antibacterial active quinolone-fluoroquinolone conjugates and 2D-QSAR studies

Bioorg Med Chem Lett. 2015 Sep 15;25(18):3816-21. doi: 10.1016/j.bmcl.2015.07.077. Epub 2015 Jul 26.

Authors

Siva S Panda¹, Sumaira Liaqat², Adel S Girgis³, Ahmed Samir⁴, C Dennis Hall⁵, Alan R Katritzky⁵

Affiliations

¹ Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA; Department of Chemistry & Physics, Georgia Reagents University, Augusta, GA 30912, USA. Electronic address: sspanda12@gmail.com.
² Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA; Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
³ Pesticide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt.
⁴ Microbiology Department, Faculty of Veterinary Medicine, Cairo University, Cairo, Egypt.
⁵ Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA.

PMID: 26253630
DOI: 10.1016/j.bmcl.2015.07.077

Abstract

Novel, quinolone-fluoroquinolone conjugates 10a-f, 11a-f, 13a-f and 14a-f with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antibacterial bioassay showed the synthesized bis-conjugates exhibit anti-bacterial properties comparable with the parent drugs.

Keywords: Amino acids; Anti-bacterial; Conjugates; Fluoroquinolone; QSAR; Quinolone.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Dose-Response Relationship, Drug
Gram-Negative Bacteria / drug effects*
Gram-Positive Bacteria / drug effects*
Microbial Sensitivity Tests
Molecular Structure
Quantitative Structure-Activity Relationship*
Quinolones / chemical synthesis
Quinolones / chemistry
Quinolones / pharmacology*

Substances

Anti-Bacterial Agents
Quinolones