The invention relates to a glycogen phosphorylase inhibitor cholic acid derivative containing bio-cleavable dipeptide, a preparation method thereof and a pharmaceutical composition containing the same. The glycogen phosphorylase inhibitor cholic acid derivative is a liver-targeted pro-drug for glycogen phosphorylase; compared with a glycogen phosphorylase inhibitor, the concentration of the glycogen phosphorylase inhibitor in a liver can be increased after the glycogen phosphorylase inhibitor cholic acid derivative is taken orally, so that the glycogen phosphorylase inhibitor cholic acid derivative can serve as a preferred drug for lowering blood sugar, particularly for treating impaired fasting glucose. The compound can be used for preventing and treating diabetes and complications thereof, hyperlipidemia, obesity, high-glucagon disease, insulin resistance, impaired fasting glucose, hypertension and complications thereof, atherosclerosis, metabolic syndrome or tumor.

Glycogen phosphorylase inhibitor cholic acid derivative containing bio-cleavable dipeptide and preparation method and medical application thereof

The invention belongs to the technical field of drug synthesis and discloses a glycogen phosphorylase inhibitor and a preparation method and application thereof. The gGlycogen phosphorylase inhibitor has a structural general formula shown as a formula (1) or pharmaceutically-acceptable salt or ester, wherein each of X1, X2, X3 and X4 is a carbon atom connecting group, or one of X1, X2, X3 and X4 is a nitrogen atom connecting group while each of the others is a carbon atom connecting group; R is H, halogen, hydroxyl, cyan, alkyl of C1-6, alkoxy of C1-6, trifluromethyl, vinyl or acetylenyl. The glycogen phosphorylase inhibitor of a novel structure has inhibiting effect on glycogen phosphorylase, is equivalent to PSN-357 in glycogenolysis inhibiting effect on a cell level and can be used for preparing drugs for treating diabetes and complications thereof, hyperlipemia, hypertension and complications thereof, atherosis, obesity and metabolic syndrome.

Glycogen phosphorylase inhibitor and preparation method and application thereof

The present disclosure provides a triazole antibacterial derivative and a pharmaceutical composition thereof and a use thereof and in particular relates to a compound represented by the following formula (I), and a racemate, a stereoisomer, a tautomer, an oxynitride or a pharmaceutically acceptable salt thereof:The compound of the present disclosure has a desirable water solubility and can be formulated into an injection for use without adding a cosolvent having a potential safety risk (such as hydroxypropyl-β-cyclodextrin, sulfobutylether-β-cyclodextrin, and the like), facilitating drug administration for patients, and greatly improving clinical safety. The drug can be used even by patients with moderate or severe renal impairment, thereby expanding the application scope of the drug.

Triazole antimicrobial derivative, pharmaceutical composition and use thereof

The invention discloses a compound having a structure formula I as shown in the specification, a preparation method and application thereof as well as pharmaceutically acceptable salts or esters of the compound. The compound is a novel cholic acid conjugated pyrrole amide based glycogen phosphorylase inhibitor, can take effect on glycogen phosphorylase of the liver effectively and can function as an optimal medicine for patients with type II diabetes to control blood sugar. The compound can be used for preparing medicines for resisting diabetes and complication thereof, medicines for resisting cardiovascular diseases, medicine for reducing weight and medicines for treating metabolic syndromes.

Compound as well as preparation method and application thereof

The invention discloses a mangiferin cholic acid derivative as well as a preparation method and application thereof, and discloses a chemical structure and a chemical synthesis method of the mangiferin cholic acid derivative. The mangiferin derivative prepared by the method has liver-targeting properties, and can be accumulated in livers and gall bladders in a targeted manner through the enterohepatic circulation mechanism of cholic acid, so that the concentration of a drug is improved, and the effect of the mangiferin cholic acid derivative on inhibiting hepatobiliary inflammation is improved.

Mangiferin cholic acid derivative as well as preparation method and application thereof

The invention relates to a glycogen phosphorylase inhibitor cholic acid derivative, a preparation method thereof and a pharmaceutical composition containing the same. The glycogen phosphorylase inhibitor cholic acid derivative is a liver-targeted pro-drug for glycogen phosphorylase; compared with a glycogen phosphorylase inhibitor, the concentration of the glycogen phosphorylase inhibitor in a liver can be increased after the glycogen phosphorylase inhibitor cholic acid derivative is taken orally, so that the glycogen phosphorylase inhibitor cholic acid derivative can serve as a preferred drug for lowering blood sugar, particularly for treating impaired fasting glucose. The compound can be used for preventing and treating diabetes and complications thereof, hyperlipidemia, obesity, high-glucagon disease, insulin resistance, impaired fasting glucose, hypertension and complications thereof, atherosclerosis, metabolic syndrome or tumor.

Liver-targeted glycogen phosphorylase inhibitor cholic acid derivative and preparation method and medical application thereof

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Liver-targeted glycogen phosphorylase inhibitor cholic acid derivative and preparation method and medical application thereof