Dihydropyrimidinones -: A new class of anti-staphylococcal antibiotics

被引:55
作者
Brands, M [1 ]
Endermann, R [1 ]
Gahlmann, R [1 ]
Krüger, J [1 ]
Raddatz, S [1 ]
机构
[1] BAYER AG, Business Res Pharma Res, D-42096 Wuppertal, Germany
关键词
D O I
10.1016/S0960-894X(02)00880-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report the synthesis and pharmacological evaluation of new derivatives of natural dipeptide antibiotic TAN-1057 A, B. In the course of this program, we identified novel analogues of the natural product that display similar antibacterial activity and showed improved tolerability. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:241 / 245
页数:5
相关论文
共 20 条
[1]   Novel antibiotics for the treatment of gram-positive bacterial infections [J].
Brands, M ;
Endermann, R ;
Gahlmann, R ;
Krüger, J ;
Raddatz, S ;
Stoltefuss, J ;
Belov, VN ;
Nizamov, S ;
Sokolov, VV ;
de Meijere, A .
JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (19) :4246-4253
[2]  
BRANDS M, Patent No. 0012484
[3]  
Ehlert K, 1999, CURR PHARM DESIGN, V5, P45
[4]   REGIOSELECTIVE NUCLEOPHILIC-ATTACK ON N-BOC-PYROGLUTAMATE ETHYL-ESTER [J].
EZQUERRA, J ;
DEMENDOZA, J ;
PEDREGAL, C ;
RAMIREZ, C .
TETRAHEDRON LETTERS, 1992, 33 (38) :5589-5590
[5]   A NEW ANTI-MRSA DIPEPTIDE, TAN-1057-A [J].
FUNABASHI, Y ;
TSUBOTANI, S ;
KOYAMA, K ;
KATAYAMA, N ;
HARADA, S .
TETRAHEDRON, 1993, 49 (01) :13-28
[6]   STEREOSPECIFIC SYNTHESIS OF (2R,3S)-3-AMINO-2-PIPERIDINEACETIC ACID-DERIVATIVES FOR USE AS CONFORMATIONAL CONSTRAINT IN PEPTIDES [J].
GOMEZMONTERREY, I ;
GONZALEZMUNIZ, R ;
HERRANZ, R ;
GARCIALOPEZ, MT .
TETRAHEDRON LETTERS, 1993, 34 (22) :3593-3594
[7]   A convenient and versatile method for the synthesis of protected guanidines [J].
Guo, ZX ;
Cammidge, AN ;
Horwell, DC .
SYNTHETIC COMMUNICATIONS, 2000, 30 (16) :2933-2943
[8]   TAN-1057A, TAN-1057B, TAN-1057C, TAN-1057D, NEW ANTIBIOTICS WITH POTENT ANTIBACTERIAL ACTIVITY AGAINST METHICILLIN-RESISTANT STAPHYLOCOCCUS-AUREUS - TAXONOMY, FERMENTATION AND BIOLOGICAL-ACTIVITY [J].
KATAYAMA, N ;
FUKUSUMI, S ;
FUNABASHI, Y ;
IWAHI, T ;
ONO, H .
JOURNAL OF ANTIBIOTICS, 1993, 46 (04) :606-613
[9]   Solid-phase synthesis of 2-aminothiazoles [J].
Kearney, PC ;
Fernandez, M ;
Flygare, JA .
JOURNAL OF ORGANIC CHEMISTRY, 1998, 63 (01) :196-200
[10]   The HgCl2-promoted guanylation reaction: The scope and limitations [J].
Levallet, C ;
Lerpiniere, J ;
Ko, SY .
TETRAHEDRON, 1997, 53 (14) :5291-5304