Imidazoline ligands selectivity

LNP 509), an 1] imidazoline receptor selective ligand with hypotensive activity. Journal of Medicinal Chemistry, 44, 1588-1593. 

Discovery of Highly Selective Imidazoline Receptor Ligands... 

Molecular superimposition is the most critical step in any CoMFA study and it was therefore thoroughly studied by testing several different alignments. Benazoline was chosen as the template, since it is the most active ligand and has a relatively limited conformational mobility. Its lowest minimum energy conformer, in which the inter-ring torsion angle between naphtyl and imidazoline moieties is -32.3, was selected for the different molecular overlays. 

Brasili L, Pigini M, Bousquet P, Carotti A, Dontenwill M, Giannella M, Moriconi R, Piergentili A, Quaglia W, Tayebati SK Discovery of highly selective imidazoline receptor ligands... 

Figure 1 Selected examples of (a) five-membered imidazole and imidazoline-based NHC ligands and (b) Pd-NHC pre-catalysts used in cross-coupling...

Discovery of highly selective imidazoline receptor ligands. Perspective in Receptor Research 24, 361-376. 

In medicinal applications, l,2,3,4-tetrahydropyrazino[l,2-alindoles were of interest as high-affinity selective imidazoline receptor ligands <04BMCL1003>, 3,4-dihydro-l//-pyrido[2,3-l ]-pyrazin-2-ones as corticotropin-releasing factor-1 (CRF 1) receptor antagonists <04JMC5783>,... 

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