Shaanxi University of Science and Technology

Yanzi Wang

Chengyuan Liang

Wen Wang

Kairui Kang

Xiuding Yang

Yuting Liu

Ying Zhou

Yunfei Zhang

Bingxing Zhang

Chenguan Liang

Mengzhou Wang

Changhua Ke

Jiaxuan Li

The present invention discloses a pleuromutilin derivative containing thiazole-pyridine benzyl quaternary ammonium salt side chain and a preparation method and use thereof and belongs to the field of medicinal chemistry. A pleuromutilin derivative with thiazole-pyridine benzyl quaternary ammonium salt side chain is successfully prepared by structural reconstruction of pleuromutilin and then structural modification with a quaternary ammonium salt compound. This compound synthesis method has the advantages of easily available raw materials, simple operation and high product yield, and is suitable for industrial production. The results of in vitro pharmacological experiments show that the pleuromutilin derivative of the present invention have good antibacterial and anti-mycoplasma activities, as well as good solubility, and these results show that the pleuromutilin derivative is of great value in the development of an anti-pathogenic microorganism drug.

Pleuromutilin derivative containing thiazole-pyridine benzyl quaternary ammonium salt side chain and preparation method and use thereof

A compound of formula I, a pharmaceutically acceptable salt thereof, or a solvent compound, an enantiomer, a diastereomer or a tautomer of the compound or a pharmaceutically acceptable salt thereof is disclosed, wherein R is a phenyl substituted with an electron withdrawing group or a phenyl substituted with an electron donating group. The pleuromutilin derivative containing a thiazolo[5,4-C]pyridine side chain in the present invention exhibits good in vitro antibacterial activity and improves the problem of poor solubility of pleuromutilin derivatives.

Pleuromutilin derivative containing a thiazolo[5,4-c]pyridine side chain, and a preparation method and application thereof

A compound of formula I, a pharmaceutically acceptable salt thereof, or a solvent compound, an enantiomer, a diastereomer or a tautomer of the compound or a pharmaceutically acceptable salt thereof is disclosed. The 3H-imidazo[4,5-C]pyridine pleuromutilin onium salt derivatives exhibit good water solubility and excellent activity against resistant, in vivo and in vitro antibacterial activity, and are of great value in the development of anti-resistant bacteria drugs and have good medical application prospects.

Pleuromutilin onium salt derivative containing a 3H-imidazo[4,5-c]pyridine side chain, and a preparation method and application thereof

Growing community of inventors

Xi'an, China

Yanzi Wang