Synthesis and anti-HIV activity of arylpiperazinyl fluoroquinolones: A new class of anti-HIV agents

被引:48
作者
Hagihara, M
Kashiwase, H
Katsube, T
Kimura, T
Komai, T
Momota, K
Ohmine, T
Nishigaki, T
Kimura, S
Shimada, K
机构
[1] Ube Ind Ltd, Pharmaceut Res Dept, Ube Lab, Ube, Yamaguchi 7550067, Japan
[2] Sankyo Co Ltd, Biol Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
[3] Sankyo Co Ltd, Med Chem Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
[4] Univ Tokyo, Dept Med, Bunkyo Ku, Tokyo 1138655, Japan
[5] Tokyo Senbai Hosp, Minato Ku, Tokyo 1088329, Japan
关键词
D O I
10.1016/S0960-894X(99)00537-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Synthesis and anti-HIV activity of a series of novel arylpiperazinyl fluoroquinolones are reported. In the SAR study, the aryl substituents on the piperazine nitrogen were found to play an important role for the anti-HIV-1 activity. A few of the compounds exhibited potent anti-HIV activity: IC50 = 0.06 mu M in chronically infected cells. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3063 / 3068
页数:6
相关论文
共 18 条
[1]  
Albrecht R, 1977, Prog Drug Res, V21, P9
[2]   Positive effects of combined antiretroviral therapy on CD4(+) T cell homeostasis and function in advanced HIV disease [J].
Autran, B ;
Carcelain, G ;
Li, TS ;
Blanc, C ;
Mathez, D ;
Tubiana, R ;
Katlama, C ;
Debre, P ;
Leibowitch, J .
SCIENCE, 1997, 277 (5322) :112-116
[3]   Potent and selective inhibition of human immunodeficiency virus type 1 transcription by piperazinyloxoquinoline derivatives [J].
Baba, M ;
Okamoto, M ;
Makino, M ;
Kimura, Y ;
Ikeuchi, T ;
Sakaguchi, T ;
Okamoto, T .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (06) :1250-1255
[4]   INVITRO ACTIVITY OF CIPROFLOXACIN, NORFLOXACIN AND NALIDIXIC-ACID [J].
BAUERNFEIND, A ;
PETERMULLER, C .
EUROPEAN JOURNAL OF CLINICAL MICROBIOLOGY & INFECTIOUS DISEASES, 1983, 2 (02) :111-115
[5]   Changing incidence of AIDS-defining illnesses in the era of antiretroviral combination therapy [J].
Brodt, HR ;
Kamps, BS ;
Gute, P ;
Knupp, B ;
Staszewski, S ;
Helm, EB .
AIDS, 1997, 11 (14) :1731-1738
[6]   Impact of new antiretroviral combination therapies in HIV infected patients in Switzerland: prospective multicentre study [J].
Egger, M ;
Hirschel, B ;
Francioli, P ;
Sudre, P ;
Wirz, M ;
Flepp, M ;
Rickenbach, M ;
Malinverni, R ;
Vernazza, P ;
Battegay, M ;
Bernasconi, E ;
Burgisser, P ;
Erb, P ;
Fierz, W ;
Grob, P ;
Gruninger, U ;
Jeannerod, L ;
Ledergerber, B ;
Luthy, R ;
Matter, L ;
Opravil, M ;
Paccaud, F ;
Perrin, L ;
Pichler, W ;
Piffaretti, GC ;
Rutschmann, O ;
Zanetti, G .
BMJ-BRITISH MEDICAL JOURNAL, 1997, 315 (7117) :1194-1199
[7]   Identification of a reservoir for HIV-1 in patients on highly active antiretroviral therapy [J].
Finzi, D ;
Hermankova, M ;
Pierson, T ;
Carruth, LM ;
Buck, C ;
Chaisson, RE ;
Quinn, TC ;
Chadwick, K ;
Margolick, J ;
Brookmeyer, R ;
Gallant, J ;
Markowitz, M ;
Ho, DD ;
Richman, DD ;
Siliciano, RF .
SCIENCE, 1997, 278 (5341) :1295-1300
[8]   Decline in deaths from AIDS due to new antiretrovirals [J].
Hogg, RS ;
OShaughnessy, MV ;
Gataric, N ;
Yip, B ;
Craib, K ;
Schechter, MT ;
Montaner, JSG .
LANCET, 1997, 349 (9061) :1294-1294
[9]   A new fluoroquinolone derivative exhibits inhibitory activity against human immunodeficiency virus type 1 replication [J].
Kashiwase, H ;
Momota, K ;
Ohmine, T ;
Komai, T ;
Kimura, T ;
Katsube, T ;
Nishigaki, T ;
Kimura, S ;
Shimada, K ;
Furukawa, H .
CHEMOTHERAPY, 1999, 45 (01) :48-55
[10]  
KIMURA T, Patent No. 0572259