Unique spirocyclopiperazinium salt I: synthesis and structure–Activity relationship of spirocyclopiperazinium salts as analgesics
作者:Feng-Li Gao、Xin Wang、Hong-Mei Zhang、Tie-Ming Cheng、Run-Tao Li
DOI:10.1016/s0960-894x(03)00177-x
日期:2003.5
spirocyclopiperazinium derivatives 7a-n and 10a-h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure-activityrelationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds
This disclosure describes novel pyrazolylpiperazines useful as hypotensive agents in mammals and as intermediates for the preparation of certain pyrazolo[1,5-a]pryrimidines.
本公开描述了作为哺乳动物降压剂和某些吡唑并[1,5-a]嘧啶的制备中间体有用的新型吡唑基哌嗪。
[EN] 2-PIPERAZIN-1-YL-4H-1,3-BENZOTHIAZIN-4-ONE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MAMMALIAN INFECTIONS<br/>[FR] DÉRIVÉS DE 2-PIPÉRAZIN-1-YL-4H-1,3-BENZOTHIAZIN-4-ONE ET LEUR UTILISATION DANS LE TRAITEMENT DES INFECTIONS CHEZ LES MAMMIFÈRES
申请人:ECOLE POLYTECH
公开号:WO2012066518A1
公开(公告)日:2012-05-24
The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin- 4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I).
2-PIPERAZIN-1-YL-4H-1,3-BENZOTHIAZIN-4-ONE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MAMMALIAN INFECTIONS
申请人:Makarov Vadim
公开号:US20130245007A1
公开(公告)日:2013-09-19
The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I).
Antibacterial Activity of 6, 8-Disubstituted-Quinolone-3-Carboxylic Acids
作者:Raghavan Krishnan、S.A. Lang
DOI:10.1002/jps.2600751214
日期:1986.12
Twelve 6,8-disubstituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid derivatives were prepared and evaluated for their antibacterialactivity. Among these, only the 6,8-difluoroquinolinone-3-carboxylic acid showed moderate activity.