- Fluoroquinolone derivative and application of fluoroquinolone derivative as antibacterial drug
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The invention discloses a fluoroquinolone derivative which is characterized in that the fluoroquinolone derivative has a structure as shown in a general formula (I) or an isomer thereof or a pharmaceutically acceptable salt thereof or a mixture of the structures. Wherein R1 is selected from C1-C4 alkyl groups; or R1 is selected from a spiro or bridged alkane chain which shares one or two carbon atoms with pyrrolidinyl connected with R1, and R1 contains 1-6 carbon atoms; O atom on the benzene ring is alternatively connected with R2 or R3: when the O atom on the benzene ring is connected with R2, R2 is selected from substituted or unsubstituted C2-C4 alkylene, and R3 does not exist; when O atom is connected with R3, R2 is selected from C3-C6 cycloalkyl, and R3 is selected from C1-C3 alkyl. The fluoroquinolone derivative provided by the invention has a good inhibition effect on escherichia coli, staphylococcus aureus and tetracoccus, and provides a certain reference for further design of quinolone compound structures.
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Paragraph 0031-0033
(2021/09/21)
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- Substituted alkynyl pyridine compounds and methods of use thereof, and use thereof
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The invention provides a substituted alkynylpyridine compound with a structure represented by a formula (I) as described in the specification and a pharmaceutically acceptable salt and a medicinal preparation thereof. The compound is used for adjusting activity of protein kinase and adjusting intercellular or intracellular signal response. The invention also relates to a pharmaceutical composition including the compound provided by the invention and a method of applying the pharmaceutical composition in treating mammals, especially in treating highly proliferative diseases of the mankind.
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- SUBSTITUTED ALKYNYL PYRIDINE COMPOUNDS AND METHODS OF USE
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The present invention provides novel substituted alkynyl pyridine compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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- Synthesis and In-Vitro Activity of Novel 1β-Methylcarbapenems Having Spiro[2,4]heptane Moieties
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The synthesis of a new series of 1β-methylcarbapenems having spiro[2,4]heptane moieties is described. Their in-vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. Most compounds were shown to be more active than the compared meropenem and imipenem against Escherichia coli. One particular compound, IIIb, having hydroxy a moiety showed the most potent antibacterial activity.
- Park, Hyeong Beom,Jo, Nam Hyun,Hong, Joon Hee,Chei, Jung Hoon,Cho, Jung-Hyuck,Yoo, Kyung Ho,Oh, Chang-Hyun
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p. 530 - 537
(2008/12/21)
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- Optically active pyridonecarboxylic acid derivatives
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N1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: STR1 These compounds have pate
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- Spiro compound
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The present invention relates to spiro compounds of general formula I: STR1 wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.
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