Ontology highlight
ABSTRACT:
SUBMITTER: Mohamed HA
PROVIDER: S-EPMC4994518 | biostudies-literature | 2011 Jan
REPOSITORIES: biostudies-literature
Mohamed Heba A HA Girgis Nancy M R NM Wilcken Rainer R Bauer Matthias R MR Tinsley Heather N HN Gary Bernard D BD Piazza Gary A GA Boeckler Frank M FM Abadi Ashraf H AH
Journal of medicinal chemistry 20101228 2
New derivatives based upon the tetrahydro-β-carboline-hydantoin and tetrahydro-β-carboline-piperazinedione scaffolds were synthesized. All compounds were evaluated for their ability to inhibit PDE5 in vitro, and numerous compounds with IC(50) values in the low nanomolar range were identified including compounds derived from l-tryptophan. Compounds with high potency versus PDE5 were then evaluated for inhibitory activity against other PDEs to assess isozyme selectivity. Compound 5R,11aS-5-(3,4-di ...[more]