A new modification of anti-tubercular active molecules

Bioorg Med Chem. 2007 Apr 1;15(7):2551-9. doi: 10.1016/j.bmc.2007.01.051. Epub 2007 Feb 2.

Abstract

The connection of two active molecules across an easily released bridge as a new type of potentially active molecule has been studied. The synthesis is based on derivatives that originate from isonicotinoyl hydrazide, pyrazinamide, p-aminosalicylic acid (PAS), ethambutol, and ciprofloxacin. The lipophilicity, hydrolysis (stability of the compounds), and antituberculotic activity as well as the structure-lipophilicity and structure-activity relationships are discussed.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry*
  • Antitubercular Agents / pharmacology*
  • Chemical Phenomena
  • Chemistry, Physical
  • Chromatography, High Pressure Liquid
  • Half-Life
  • Isoniazid / chemical synthesis
  • Isoniazid / pharmacology
  • Kinetics
  • Lipids / chemistry
  • Microbial Sensitivity Tests
  • Mycobacterium avium / drug effects
  • Mycobacterium kansasii / drug effects
  • Pyrazinamide / chemical synthesis
  • Pyrazinamide / pharmacology
  • Quantitative Structure-Activity Relationship

Substances

  • Antitubercular Agents
  • Lipids
  • Pyrazinamide
  • Isoniazid