Piperidine-renin inhibitors compounds with improved physicochemical properties

Bioorg Med Chem Lett. 1999 May 17;9(10):1403-8. doi: 10.1016/s0960-894x(99)00196-1.

Abstract

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.

MeSH terms

  • Animals
  • Antihypertensive Agents / chemistry*
  • Antihypertensive Agents / pharmacology
  • Callithrix
  • Dose-Response Relationship, Drug
  • Humans
  • Piperidines / chemistry*
  • Piperidines / pharmacology
  • Recombinant Proteins / antagonists & inhibitors
  • Renin / antagonists & inhibitors*

Substances

  • Antihypertensive Agents
  • Piperidines
  • Recombinant Proteins
  • Renin