309762-63-8Relevant academic research and scientific papers
Syntheses and biological evaluation of new fluoroquinolone antibacterials containing chiral oxiimino pyrrolidine
Choi, Dong Rack,Shin, Jung Han,Yang, Jin,Yoon, Sue Hye,Jung, Yong Ho
, p. 1273 - 1277 (2004)
The design and syntheses of new fluoroquinolone antibacterial agents having pyrrolidine ring at C-7 position are described. The pyrrolidine ring is optically active and possesses methyloxime functional group. Two of them have excellent in vitro antibacterial activities and pharmacokinetic profiles.
Tri-, tetra-substituted-3-aminopyrrolidine derivative
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Page/Page column 48, (2008/06/13)
A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):
TRI- OR TETRA-SUBSTITUTED-3-AMINOPYRROLIDINE DERIVATIVES
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Page/Page column 110-111, (2008/06/13)
It is intended to provide quinolone type synthetic antibacterial agents having a potent antibacterial activity against a broad scope of gram-positive and gram-negative bacteria and a high safety and remedies for infections. A compound represented by the following general formula (I), its salt or hydrate thereof: I wherein R1 and R2 represent each hydrogen, etc.; R3 represents C1-6 alkyl, etc.; R4 and R5 independently represent each hydrogen, C1-6 alkyl, etc., provided that R4 and R5 are not hydrogen atoms at the same time, and the above substituents R4 and R5 may be united and form a spiro ring structure structure together with the pyrrolidine ring; R6 and R7 independently represent each hydrogen or C1-6 alkyl; R8 represents a C1-6 haloalkyl group, etc.; X1 represents hydrogen or halogen; and A represents a nitrogen atom or a partial structure represented by the following general formula (II).
Optically active quinoline carboxylic acid derivatives with 7-pyrrolidine substituents causing optical activity and a process for the preparation thereof
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Page/Page column 13, (2010/01/31)
The present invention relates to optically active quinoline carboxylic acid derivatives, their pharmaceutically acceptable salts, their solvates, and a process for the preparation thereof. More specifically, the present invention relates to optically active quinoline carboxylic acid derivatives containing 4-aminomethyl-4-methyl-3-(Z)-alkoxyirninopyrrolidine substituents causing optical activity at the 7-position of the quinolone nuclei. As the compounds of the present invention have superior antibacterial activity and pharmacokinetic profiles to their enantiomers, their racemates and conventional antibacterial agents, with nearly no phototoxicity, the compounds of this invention are useful for antibacterial agents.
