The design and synthesis of a novel, orally active, selective ETA antagonist

Article abstract of DOI:10.1007/s00044-004-0021-y

The potency and pharmacokinetic properties of an indole-based series of endothelin antagonists have been optimised using in vitro, in silico and in vivo methods. Compound 8 is oxidised in vivo to the active metabolite 7 and has been highlighted as an oral