Saczewski, Franciszek; Kornicka, Anita; Hudson, Alan L.; Laird, Shayna; Scheinin, Mika; Laurila, Jonne M.; Rybczynska, Apolonia; Boblewski, Konrad; Lehmann, Artur; Gdaniec, Maria published the artcile< 3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α2-adrenoceptor compared to the imidazoline I1 receptor>, Computed Properties of 94087-40-8, the main research area is imidazolidinyl indazole preparation adrenoceptor ligand SAR.
A series of 3-[(4,5-dihydroimidazolidin-2-yl)imino]indazoles has been synthesized as positional analogs of marsanidine, a highly selective α2-adrenoceptor ligand. Parent compound 4a (I) and its 4-chloro (4c) and 4-Me (4d) derivatives display α2-adrenoceptor affinity at nanomolar concentrations (Ki = 39.4, 15.9 and 22.6 nM, resp.) and relatively high α2/I1 selectivity ratios of 82, 115 and 690, resp. Evidence was obtained that these compounds act as partial agonists at α2A-adrenoceptors. Compound 4d with intrinsic activity comparable with that of marsanidine, but lower than that of clonidine, elicited pronounced cardiovascular effects in anesthetized rats at doses as low as 0.01 mg/kg iv.
Bioorganic & Medicinal Chemistry published new progress about Antihypertensives. 94087-40-8 belongs to class nitriles-buliding-blocks, and the molecular formula is C7H3ClFN, Computed Properties of 94087-40-8.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts