synthesis, molecular modeling, and biological evaluation of novel tetrahydro-β-carboline hydantoin and tetrahydro-β-carboline thiohydantoin derivatives as phosphodiesterase 5 inhibitors

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ID: 205488
2011
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Abstract
Two series of fused tetrahydro-β-carboline hydantoin and tetrahydro-β-carboline thiohydantoin derivatives with a pendant 2,4-dimethoxyphenyl at position 5 were synthesized, and chiral carbons at positions 5 and 11a swing from R,R to R,S, S,R, and S,S. The prepared analogues were evaluated for their capacity to inhibit phosphodiesterase 5 (PDE5) isozyme. The R absolute configuration of C-5 in the β-carboline hydantoin derivatives was found to be essential for the PDE5 inhibition. Chiral carbon derived from amino acid even if of the S configuration (L-tryptophan) may lead to equiactive or more active isomers than those derived from amino acid with the R configuration (D-tryptophan). This expands the horizon from which efficient PDE5 inhibitors can be derived and may offer an economic advantage. The thiohydantoin derivatives were less active than their hydantoin congeners.
Reference Key
abadi2011internationalsynthesis, Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Ashraf H. Abadi;Jochen Lehmann;Gary A. Piazza;Mohammad Abdel-Halim;Mohamed S. M. Ali
Journal Journal of human genetics
Year 2011
DOI
10.1155/2011/562421
URL
http://dx.doi.org/10.1155/2011/562421
Keywords
therapeutics pharmacology

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