Group of substituted benzoheterocycle amine derivatives and preparation method and related application thereof as IMPDH (inosine monophosphate dehydrogenase) inhibitor
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A kind of benzo, unsubstituted technology, be used in the field of substituted benzoheterocyclic amine derivatives and preparation thereof
Active Publication Date: 2014-08-20
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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Embodiment 1
[0088] , N-(thiophene-2-methyl)-1H-indol-6-amine
[0089] Put 0.132g (0.001mol) of 6-aminoindole and 0.112 (0.001mol) of thiophene-2-carbaldehyde into a 25ml eggplant-shaped bottle, add 5ml of absolute ethanol, stir overnight at room temperature, then add 50mg of sodium borohydride, and continue the reaction for 3 Hour. After the reaction is complete, add 2ml of water, adjust the pH of the reaction solution to neutral with dilute hydrochloric acid, stir for 20 minutes, extract with dichloromethane, wash with water, wash several layers with saturated sodium chloride solution, and dry over anhydrous magnesium sulfate. After filtration and concentration, the obtained product was separated by silica gel column chromatography to obtain 0.109 g (yield: 45%) of off-white solid compound.
[0092] Using 6-aminoindole and 5-methyl-2-thiophenecarbaldehyde as raw materials, a pale white solid compound 2 (yield: 46%) was synthesized according to the similar method of Example 1.
[0095] Using 6-aminoindole and 5-chloro-2-thiophenecarbaldehyde as raw materials, a pale white solid compound 3 (yield: 47%) was synthesized according to the similar method of Example 1.
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Abstract
The invention discloses a group of substituted benzoheterocycle amine derivatives and a preparation method and related application thereof as an IMPDH (inosine monophosphate dehydrogenase) inhibitor. The IMPDH inhibitor has good application prospects in virus resistance, immunosuppression, tumor resistance, bacterium resistance, parasite resistance and the like. In the invention, a new-structure IMPDH inhibitor shown by the formula (I) is obtained through the design, synthesis and activity screening study on an active compound targeting IMPDH, and a foundation is laid for the development and application of the compounds as the medicines and medicinal compositions thereof with related effects such as virus resistance, tumor resistance, immunosuppression and the like.
Description
technical field [0001] The invention relates to a group of substituted benzoheterocyclic amine derivatives and a preparation method thereof, and also relates to the related application of the substituted benzoheterocyclic amine derivatives as inosine nucleotide dehydrogenase (IMPDH) inhibitors, belonging to biological field of medicine. Background technique [0002] Inosine MONOPHOSPHATE DEHYDROGE NASE (IMPDH) is a key enzyme in the biosynthesis of purine nucleotides, which relies on nicotinamide adenine dinucleotide (NAD) and catalyzes the de novo synthesis of guanine nucleotides The rate-limiting step in the oxidation of inosine nucleotides (IMP) to xanthine nucleotides (XMP). XMP is then converted to GMP by the action of GMP synthetase. This is key to cell growth and proliferation. IMPDH / GMP is present in every organism except a few protozoan parasites. Inhibition of IMPDH results in inhibition of proliferation and many important intracellular responses. Human IMPDH ...
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