Kopinathan, Anitha; Draper-Joyce, Christopher; Szabo, Monika; Christopoulos, Arthur; Scammells, Peter J.; Lane, J. Robert; Capuano, Ben published the artcile< Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-((trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity at the Dopamine D2 Receptor>, Recommanded Product: 5-Fluoroindole-2-carboxylic acid, the main research area is SB269652 derivative preparation indolecarboxamide motif modification drug design antipsychotics.
SB269652 (I) is a neg. allosteric modulator of the dopamine D2 receptor. Herein, we present the design, synthesis, and pharmacol. evaluation of “”second generation”” analogs of I whereby subtle modifications to the indole-2-carboxamide motif confer dramatic changes in functional affinity (5000-fold increase), cooperativity (100-fold increase), and a novel action to modulate dopamine efficacy. Thus, structural changes to this region of I allows the generation of a novel set of analogs with distinct pharmacol. properties.
Journal of Medicinal Chemistry published new progress about Amidation. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Recommanded Product: 5-Fluoroindole-2-carboxylic acid.
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles