Quinolines derivatives as novel sunscreening agents

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4506-10. doi: 10.1016/j.bmcl.2013.06.046. Epub 2013 Jun 26.

Abstract

Currently, the research and development of sunscreens play an important role on the synthesis of actives that are stable in various kinds of formulations-in addition to their efficiency and broad spectrum of protection against ultraviolet radiation. Our objective here was to synthesize new sunscreening chemical agents using quinoline as a base molecule. Twelve quinoline derivatives were synthesized, four of them novel molecules, and their photoprotective activity was determined in vitro using diffuse transmittance spectrophotometry. We determined their SPF, UVAPF, UVA/UVB ratio, critical wavelength and Boots Star Rating. The quinolines derivatives presented a varied profile of photoprotection, their SPF ranging from 2 to 11 and their UVAPF from 2 to 7. In terms of the critical wavelength, all molecules were considered of broad-spectrum by different classifications. Regarding the Boots Star Rating, one compound received no rating, seven of them received a three stars rating, three received a four stars rating and three were given a five stars rating. The molecules showed in the present work have a wide range of possibilities for creating new sunscreen products, once they have good SPF or UVAPF for single molecules, and they also possess other different qualities that can act synergistically.

Keywords: Chemical synthesis; Photoprotective activity; Quinolines; Structure–activity relationship; Sunscreening agents/UV filters; Ultraviolet radiation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical
  • Molecular Structure
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Spectrophotometry
  • Sunscreening Agents / chemical synthesis*
  • Sunscreening Agents / chemistry

Substances

  • Quinolines
  • Sunscreening Agents