| Title : Synthesis and pharmacological evaluation of imidazoline sites I1 and I2 selective ligands - Anastassiadou_2001_Bioorg.Med.Chem_9_585 |
| Author(s) : Anastassiadou M , Danoun S , Crane L , Baziard-Mouysset G , Payard M , Caignard DH , Rettori MC , Renard PY |
| Ref : Bioorganic & Medicinal Chemistry , 9 :585 , 2001 |
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Abstract :
Several series of 2-aryl or heterocyclic-imidazoline compounds have been prepared and evaluated in vitro as imidazoline sites (I1 and I2) and alpha-adrenergic (alpha1 and alpha2) receptor ligands. Their pKi values indicate that linkage of the imidazoline moiety at the 2-position with an aromatic substituent dramatically decreases alpha-adrenergic affinity. I1 sites are more accessible by phenyl imidazolines substituted by a methyl or a methoxy group at the ortho or meta position. Indeed, 2-(2'-methoxyphenyl)-imidazoline (17) is one of the best I1 ligands ever reported (pKi = 8.53 and I1/I2 > 3388). On the other hand, I2 selectivity increases in the presence of a methyl group in the para position. The original compound, 2-(3'-fluoro-4'-tolyl)-imidazoline (31) is a new potent ligand for the I2 sites with high selectivity (pKi = 8.53 and I2/I1 > 3388). |
| PubMedSearch : Anastassiadou_2001_Bioorg.Med.Chem_9_585 |
| PubMedID: 11310592 |
Anastassiadou M, Danoun S, Crane L, Baziard-Mouysset G, Payard M, Caignard DH, Rettori MC, Renard PY (2001)
Synthesis and pharmacological evaluation of imidazoline sites I1 and I2 selective ligands
Bioorganic & Medicinal Chemistry
9 :585
Anastassiadou M, Danoun S, Crane L, Baziard-Mouysset G, Payard M, Caignard DH, Rettori MC, Renard PY (2001)
Bioorganic & Medicinal Chemistry
9 :585