Salicylamide ether compounds of pleuromutilin and preparation method thereof

A technology of pleuromutilin and salicylamide ether, which is applied in the field of chemical synthesis of drugs, can solve the problems of adverse reactions and low bioavailability, and achieve the effect of improving drug efficacy and reducing costs
CN102180809AInactive Publication Date: 2011-09-14WUHAN INSTITUTE OF TECHNOLOGY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
WUHAN INSTITUTE OF TECHNOLOGY
Publication Date
2011-09-14
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to pleuromutilin derivatives, particularly salicylamide ether compounds of pleuromutilin and a preparation method thereof. The structural formula of the salicylamide ether compounds of pleuromutilin is disclosed as a general formula I, wherein R is NHCmH2mCH3, and m is a whole number which is greater than or equal to 0. In the invention, the pleuromutilin, which is used as the raw material, is esterified, subjected to amine-ester exchange and etherified to obtain the pleuromutilin derivatives. The related pharmaceutic adjuvant groups are changed to enhance the pharmaceutic activity, thereby achieving the corresponding pharmacodynamic goal. In normal cases, most receptors are proteins or derivatives thereof; the amido group contained in the pharmaceutic molecule can promote the pharmaceutic molecule to be combined with the corresponding receptor in an easier way, thereby enhancing the pharmaceutic effect. All the pharmaceutic materials in the synthetic process are common, cheap and accessible, thereby lowering the production cost.
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Description

technical field

[0001] The invention relates to the field of chemically synthesized medicines, in particular to a pleuromutilin derivative salicylamide ether compound of pleuromutilin and a preparation method thereof. Background technique

[0002] Pleuromutilin was first isolated and initially identified by Kavanagh et al. in 1951. It is a class of broad-spectrum diterpene antibiotics produced by the higher fungi Pleuromyces and Pleuromyces, which can effectively inhibit Gram Positive bacteria, especially staphylococcus and streptococcus are the most obvious, and also have therapeutic effect on mycoplasma infection. Many of its derivatives have stronger antibacterial activity and scope than pleuromutilin, and have a wider antibacterial spectrum. In recent years, with the increasing drug resistance of G+ bacteria, including methicillin-resistant Staphylococcus aureus, penicillin-resistant pneumococcus, and vancomycin-resistant enterococcus, the commonly used antibacterial dru...

Claims

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