Literature DB >> 1846917

Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride.

D T Chu1, C W Nordeen, D J Hardy, R N Swanson, W J Giardina, A G Pernet, J J Plattner.   

Abstract

Temafloxacin hydrochloride [(+/-)-7-(3-methylpiperazin-1-yl)-6-fluoro-1-(2,4-difluorophenyl)- 1,4-dihydro- 4-oxoquinoline-3-carboxylic acid hydrochloride] is a potent member of the 4-pyridone-3-carboxylic acid class of antibacterial agents and is currently under clinical development as a broad-spectrum antimicrobial agent. It is a racemate having a chiral center at the C3 of the 7-piperazin-1-yl group. The two enantiomers were synthesized and tested for their antibacterial activities. Although no difference in in vitro antibacterial activities was observed, a minor difference in in vivo antibacterial activities was observed. However, they both exhibited similar pharmacological profiles.

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Year:  1991        PMID: 1846917     DOI: 10.1021/jm00105a025

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  5 in total

1.  Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.

Authors:  Chengxin Zhi; Zheng-Yu Long; Andrzej Manikowski; Jeanne Comstock; Wei-Chu Xu; Neal C Brown; Paul M Tarantino; Karsten A Holm; Edward J Dix; George E Wright; Marjorie H Barnes; Michelle M Butler; Kimberly A Foster; William A LaMarr; Benoit Bachand; Richard Bethell; Caroline Cadilhac; Sylvie Charron; Serge Lamothe; Irina Motorina; Richard Storer
Journal:  J Med Chem       Date:  2006-02-23       Impact factor: 7.446

Review 2.  Classification and structure-activity relationships of fluoroquinolones.

Authors:  A Bryskier; J F Chantot
Journal:  Drugs       Date:  1995       Impact factor: 9.546

3.  Conformational Preference of 2'-Fluoro-Substituted Acetophenone Derivatives Revealed by Through-Space 1H-19F and 13C-19F Spin-Spin Couplings.

Authors:  Chinatsu Otake; Takuya Namba; Hidetsugu Tabata; Kosho Makino; Kiriko Hirano; Tetsuta Oshitari; Hideaki Natsugari; Takenori Kusumi; Hideyo Takahashi
Journal:  J Org Chem       Date:  2021-03-01       Impact factor: 4.354

4.  Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones.

Authors:  Aneta Pokorna; Pavel Bobal; Michal Oravec; Lucie Rarova; Janette Bobalova; Josef Jampilek
Journal:  Molecules       Date:  2019-02-04       Impact factor: 4.411

5.  Species Differences in Stereoselective Pharmacokinetics of HSG4112, A New Anti-Obesity Agent.

Authors:  In Yong Bae; Min Sun Choi; Young Seok Ji; Sang-Ku Yoo; Kyungil Kim; Hye Hyun Yoo
Journal:  Pharmaceutics       Date:  2020-02-03       Impact factor: 6.321

  5 in total

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