Dimeric L-Dopa derivatives as potential prodrugs

被引:31
作者
Di Stefano, A [1 ]
Mosciatti, B
Cingolani, GM
Giorgioni, G
Ricciutelli, M
Cacciatore, I
Sozio, P
Claudi, F
机构
[1] Univ G DAnnunzio, Dipartimento Sci Farmaco, I-66100 Chieti, Italy
[2] Univ Camerino, Dipartimento Sci Chim, I-62032 Camerino, Italy
关键词
D O I
10.1016/S0960-894X(01)00140-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of dimeric derivatives ( +)-1, and ( +)-2. and (+)-3a-d of L-Dopa diacetyl esters was synthesized and evaluated as potential L-Dopa prodrugs with improved physicochemical properties. All the new compounds showed chemical stability in aqueous buffer solutions (pH 1.3 and 7.4). A relatively slow release of r-Dopa in human plasma was observed. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1085 / 1088
页数:4
相关论文
共 12 条
[1]   Protective and symptomatic strategies for therapy of Parkinson's disease [J].
Blandini, F ;
Greenamyre, JT .
DRUGS OF TODAY, 1999, 35 (06) :473-483
[2]  
BODOR N, Patent No. 3988799
[3]   Cardiovascular hybrid drugs: Combination of more than one pharmacological property in one single molecule [J].
Christiaans, JAM ;
Timmerman, H .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 1996, 4 (01) :1-22
[4]   Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa [J].
Cingolani, GM ;
Di Stefano, A ;
Mosciatti, B ;
Napolitani, F ;
Giorgioni, G ;
Ricciutelli, M ;
Claudi, F .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (12) :1385-1388
[5]   L-DOPA ESTERS AS POTENTIAL PRODRUGS .3. BEHAVIORAL ACTIVITY IN EXPERIMENTAL-MODELS OF PARKINSONS-DISEASE [J].
COOPER, DR ;
MARREL, C ;
VANDEWATERBEEMD, H ;
TESTA, B ;
JENNER, P ;
MARSDEN, CD .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1987, 39 (08) :627-635
[6]  
FARGHALY AO, 1998, EUR J MED CHEM, V33, P123
[7]  
GIANNOLA LI, 1992, PHARMAZIE, V47, P423
[8]   SYNTHESIS OF SYMMETRICAL PSEUDOPEPTIDES AS POTENTIAL INHIBITORS OF THE HUMAN IMMUNODEFICIENCY VIRUS-1 PROTEASE [J].
LANGLOIS, M ;
QUINTARD, D ;
ABALAIN, C .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1994, 29 (09) :639-647
[9]   Metronidazole twin ester prodrugs: synthesis, physicochemical properties, hydrolysis kinetics and antigiardial activity [J].
Mahfouz, NM ;
Aboul-Fadl, T ;
Diab, AK .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1998, 33 (09) :675-683
[10]  
WANG HP, 1995, BIOORG MED CHEM LETT, V5, P2195