The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Chloro-8-methylquinoline( cas:18436-73-2 ) is researched.SDS of cas: 18436-73-2.Chen, Junli; Campbell, Adrian P.; Urmi, Kaniz F.; Wakelin, Laurence P. G.; Denny, William A.; Griffith, Renate; Finch, Angela M. published the article 《Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines》 about this compound( cas:18436-73-2 ) in Bioorganic & Medicinal Chemistry. Keywords: human adrenoceptor selectivity homobivalent aminoquinoline; 4-Aminoquinolines; 5-HT(1A)-receptor; Affinity; Selectivity; α(1)-adrenoceptor. Let’s learn more about this compound (cas:18436-73-2).
A series of ring-substituted ethyl- and heptyl-linked 4-aminoquinoline dimers were synthesized and evaluated for their affinities at the 3 human α1-adrenoceptor (α1-AR) subtypes and the human serotonin 5-HT1A-receptor (5-HT1A-R). We find that the structure-specificity profiles are different for the two series at the α1-AR subtypes, which suggests that homobivalent 4-aminoquinolines can be developed with α1-AR subtype selectivity. The 8-Me ethyl-linked analog has the highest affinity for the α1A-AR, 7 nM, and the greatest capacity for discriminating between α1A-AR and α1B-AR (6-fold), α1D-AR (68-fold), and the 5-HT1A-R (168-fold). α1B-AR selectivity was observed with the 6-Me derivative of the ethyl- and heptyl-linked 4-aminoquinoline dimers and the 7-methoxy (7-OMe) derivative of the heptyl-linked analog. These substitutions result in 4- to 80-fold selectivity for α1B-AR over α1A-AR, α1D-AR, and 5-HT1A-R. In contrast, 4-aminoquinoline dimers with selectivity for α1D-AR are more elusive, since none studied to date has greater affinity for the α1D-AR over the other two α1-ARs. The selectivity of the 8-Me ethyl-linked 4-aminoquinoline dimer for the α1A-AR, and 6-Me ethyl-linked, and the 6-Me and 7-OMe heptyl-linked 4-aminoquinoline dimers for the α1B-AR, makes them promising leads for drug development of α1A-AR or α1B-AR subtype selective ligands with reduced 5-HT1A-R affinity.
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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia