Optimization of orally bioavailable alkyl amine renin inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC{sub 50} of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg resulted in >20 h reduction of blood pressure in a double transgenic rat model of hypertension.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1002629
- Journal Information:
- Bioorg. Med. Chem. Lett., Vol. 20, Issue (2) ; 01, 2010; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
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