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A novel series of IKKbeta inhibitors part I: Initial SAR studies of a HTS hit
A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKbeta. In this Letter we document our early efforts at optimization of the quinoline core, the imidazole and the semithiocarbazone moiety. Most potency gains came from substitution around the 6- and 7-positions of the quinoline ring. Replacement of the semithiocarbazone with a semicarbazone decreased potency but led to some measurable exposure.
We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 1055361-35-7, and how the biochemistry of the body works.Synthetic Route of 1055361-35-7
Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H884N | ChemSpider