首页> 外国专利> S-OXIDE AND S,S,-DIOXIDE TETRAHYDROTHIOPYRAN PHENYLOXAZOLIDINONES, THEIR USE FOR PREPARATION OF PHARMACEUTICAL COMPOSITIONS AND PROCESS FOR DETERMINING THE INHIBITORY ACTIVITY OF COMPOUNDS TO HUMAN MONOAMINO OXIDASE

S-OXIDE AND S,S,-DIOXIDE TETRAHYDROTHIOPYRAN PHENYLOXAZOLIDINONES, THEIR USE FOR PREPARATION OF PHARMACEUTICAL COMPOSITIONS AND PROCESS FOR DETERMINING THE INHIBITORY ACTIVITY OF COMPOUNDS TO HUMAN MONOAMINO OXIDASE

机译:S-氧化物和S,S,-二氧化物四氢噻吩并苯并恶唑烷酮,其在制备药物成分中的用途以及测定化合物对人单胺氧化酶的抑制活性的过程

摘要

The present invention relates to compounds of general formula (I) and (II) having antimicrobial activity, wherein R1 is methyl, ethyl, cyclopropyl or dichloromethyl, R2 and R3 are independently hydrogen or fluorine and R4 is ethyl or dichloromethyl. . The present invention relates to the use of the above compounds for the preparation of a pharmaceutical composition which can be administered as an antibacterial agent. The compounds of formula (I) and (II) have the advantage of moderately inhibiting the activity of monoamine oxidase (MAO) with known oxazolidinone derivatives, resulting in the absence of various side effects. The present invention also provides a novel assay for determining the inhibitory effect of oxazolidinone derivatives and other compounds on human monoamine oxidase. SHE
机译:本发明涉及具有抗微生物活性的通式(I)和(II)的化合物,其中R 1是甲基,乙基,环丙基或二氯甲基,R 2和R 3独立地是氢或氟并且R 4是乙基或二氯甲基。 。本发明涉及上述化合物在制备可以作为抗菌剂给药的药物组合物中的用途。式(I)和(II)的化合物具有用已知的恶唑烷酮衍生物适度抑制单胺氧化酶(MAO)活性的优点,导致没有各种副作用。本发明还提供了一种新颖的测定法,用于测定恶唑烷酮衍生物和其他化合物对人单胺氧化酶的抑制作用。她

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