Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.

@article{Bartrol1995SynthesisAA,
  title={Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.},
  author={Javier Bartrol{\'i} and E Turmo and Miguel Alguer{\'o} and E Boncompte and M. L. Vericat and Juli{\'a}n Garc{\'i}a-Rafanell and Javier Forn},
  journal={Journal of medicinal chemistry},
  year={1995},
  volume={38 20},
  pages={3918-32}
}
A series of azole derivatives carrying an N-acylmorpholine ring are described. The compounds were chemically designed to simulate the lanosterol D ring, taking advantage of the conformational preferences of 2-alkyl-1-acylmorpholines. Three structural variables, the nature of the N-benzoyl group, the phenyl substituents, and the degree of oxidation at carbon 2 of the morpholine, were optimized for maximum activity. Only the (5R,6R) isomers showed antifungal activity. Cyclic hemiacetal (-)-39a… CONTINUE READING
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