
pmid: 16919453
Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated.
Molecular Structure, Drug Evaluation, Preclinical, Stereoisomerism, In Vitro Techniques, Binding, Competitive, Cell Line, Structure-Activity Relationship, Aminoquinolines, Humans, Receptors, Somatostatin
Molecular Structure, Drug Evaluation, Preclinical, Stereoisomerism, In Vitro Techniques, Binding, Competitive, Cell Line, Structure-Activity Relationship, Aminoquinolines, Humans, Receptors, Somatostatin
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