Piperidine renin inhibitors: from leads to drug candidates
Non-peptidomimetic renin inhibitors of the piperidine type represent a novel structural class of compounds potentially free of the drawbacks seen with peptidomimetic compounds so far. Synthetic optimization in two structural series focusing on improvement
Maerki, H. P.,Binggeli, A.,Bittner, B.,Bohner-Lang, V.,Breu, V.,Bur, D.,Coassolo, Ph.,Clozel, J. P.,D'Arcy, A.,Doebeli, H.,Fischli, W.,et al.
p. 21 - 28
(2007/10/03)
Piperidine-renin inhibitors compounds with improved physicochemical properties
Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D((pH 7.4)) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets.
Gueller, Rolf,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Hirth, Georges,Jenny, Christian,Kansy, Manfred,Montavon, Francois,Mueller, Marcel,Oefner, Christian,Stadler, Heinz,Vieira, Eric,Wilhelm, Maurice,Wostl, Wolfgang,Maerki, Hans Peter
p. 1403 - 1408
(2007/10/03)
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