The C-C chemokine receptor type 5 (CCR5) is a transmembrane receptor that plays a pivotal role as a HIV anchor to human cell membranes, mediating viral entry. CCR5 antagonists, acting by blocking the receptor and preventing its interaction with the HIV proteins, are key agents towards effective anti-viral therapy. This work describes the computational study, synthesis and viral inhibition assay of a number of camphor derivatives as a first step towards new drug leads to block this specific entry pathway. Viral inhibition assays have identified three molecules, camphor carboxylic acid, its tri(hydroxymethyl)aminomethane amide derivative, and an hydroxyl-imide camphor derivative as promising agents to develop new drugs, with IC 50 values (0.16, 0.22 and 1.02 mM, respectively) one order below that of maraviroc (0.02 mM), a clinically used CCR5 antagonist.
In situreduction of CuCl2enables formation of Cu(i) complexes prone to activate molecular oxygen from air towards catalytic oxidation of 1,3-dicarbonyls.
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