| 18763754 |
Lucas S, Heim R, Negri M, Antes I, Ries C, Schewe KE, Bisi A, Gobbi S, Hartmann RW: Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach. J Med Chem. 2008 Oct 9;51(19):6138-49. Epub 2008 Sep 3.
Pharmacophore modeling of a series of aldosterone synthase (CYP11B2) inhibitors triggered the design of compounds 11 and 12 by extending a previously established naphthalene molecular scaffold (e.g., present in molecules 1 and 2) via introduction of a phenyl or benzyl residue in 3-position. |
34(0,1,1,4) |
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| 18672861 |
Heim R, Lucas S, Grombein CM, Ries C, Schewe KE, Negri M, Muller-Vieira U, Birk B, Hartmann RW: Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity. J Med Chem. 2008 Aug 28;51(16):5064-74. Epub 2008 Aug 1.
In the present study, we examined the influence of substituents in the heterocycle of lead structures with a naphthalene molecular scaffold to overcome this unwanted side effect. |
5(0,0,0,5) |
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