Panorama Research Inc.

Xiaojian Jiang

Yuqiang Wang

Pei Yu

Zaijun Zhang

Jie Jiang

Zhaoqi Yang

Ying Yeung Yeung

The present invention provides novel chiral bisamino-ether compounds, and method of preparation and use thereof. The chiral bisamino-ether compounds have the structure of formula (I). The method of preparation includes: using chiral aminomethanol compounds as starting materials to react with halogenated aryl compounds in the presence of a base to give a variety of chiral bisamino-ether compounds. The novel chiral bisamino-ether compounds can be used for asymmetric fluorocyclization of unsaturated heterocyclic compounds with excellent enantioselectivity and great potentials for industrial applications.

Chiral bisamino-ether compounds, and method of preparation and use thereof

The present invention relates to an andrographolide derivative of the formula (I), wherein R, Rand Rare same or different substituents selected from hydrogen, substituted or unsubstituted organic acid radicals, inorganic acid radicals, alkyl, aryl or heteroaryl, and at least one of R, Rand Ris R-lipoic acid, S-lipoic acid or a mixture thereof, or corresponding dihydrolipoic acids thereof, or N-acetylcysteine radical. The derivative has good antitumor effect, can induce apoptosis of tumor cells, can directly kill Gram-positive bacteria () and drug resistance bacteria (MRSA5676 and MRSA5677), can inhibit the QS-system of Gram-negative bacteria (), can inhibit and destroy the formation of biofilm of; and exhibits significant hypoglycemic effect, so that it can be used in manufacture of medicaments for treatment of cancers, inflammation, diabetes, and bacterial and viral infections. 

Andrographolide derivatives and use thereof in manufacture of medicaments

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Guangzhou, China

Xiaojian Jiang