Synthesis and anticonvulsant activity of a series of benzamides

被引:6
作者
Musso, DL
Boswell, GE
Mehta, NB
Soroko, FE
Burchall, CJ
机构
[1] BURROUGHS WELLCOME CO, DIV ORGAN CHEM, RES TRIANGLE PK, NC 27709 USA
[2] BURROUGHS WELLCOME CO, DIV PHARMACOL, RES TRIANGLE PK, NC 27709 USA
关键词
N-(2-(dimethylamino)-1,1-dimethylethyl)benzamide; anticonvulsant activity;
D O I
10.1016/0223-5234(96)80370-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of benzamides containing N,N,2-trimethyl-1,2-propane diamine as the amide moiety was synthesized. The compounds were evaluated in the maximal electroshock (MES) and pentylenetetrazol (metrazole, MET) screens for anticonvulsant activity. The 3,5-trifluoromethyl, 3,5-dichloro, and 3-bromo analogues proved to be either equipotent with or more potent than phenytoin.
引用
收藏
页码:331 / 334
页数:4
相关论文
共 11 条
[1]   ANTICONVULSANT ACTIVITY OF SOME 4-AMINOBENZAMIDES [J].
CLARK, CR ;
WELLS, MJM ;
SANSOM, RT ;
NORRIS, GN ;
DOCKENS, RC ;
RAVIS, WR .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (06) :779-782
[2]   ANTICONVULSANT PROPERTIES OF SOME SUBSTITUTED BENZAMIDES [J].
HORROM, BW ;
LYNES, TE .
JOURNAL OF MEDICINAL CHEMISTRY, 1963, 6 (05) :528-&
[3]   NEW N-ARYL ISOXAZOLECARBOXAMIDES AND N-ISOXAZOLYBENZAMIDES AS ANTICONVULSANT AGENTS [J].
LEPAGE, F ;
TOMBRET, F ;
CUVIER, G ;
MARIVAIN, A ;
GILLARDIN, JM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1992, 27 (06) :581-593
[4]  
LYNES T. E., 1961, FED PROC, V20, P323
[5]   POTENTIAL ANTICONVULSANTS .1. 5-BENZYLHYDANTOINS [J].
MEHTA, NB ;
DIUGUID, CAR ;
SOROKO, FE .
JOURNAL OF MEDICINAL CHEMISTRY, 1981, 24 (04) :465-468
[6]   DISCOVERY AND ANTICONVULSANT ACTIVITY OF THE POTENT METABOLIC INHIBITOR 4-AMINO-N-(2,6-DIMETHYLPHENYL)-3,5-DIMETHYLBENZAMIDE [J].
ROBERTSON, DW ;
LEANDER, JD ;
LAWSON, R ;
BEEDLE, EE ;
CLARK, CR ;
POTTS, BD ;
PARLI, CJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (10) :1742-1746
[7]  
Stanley M., 1982, BENZAMIDES PHARM NEU
[8]   LABORATORY EVALUATION OF ANTIEPILEPTIC DRUGS - REVIEW OF LABORATORY METHODS [J].
SWINYARD, EA .
EPILEPSIA, 1969, 10 (02) :107-&
[9]   CHANCE CORRELATIONS IN STRUCTURE-ACTIVITY STUDIES USING MULTIPLE REGRESSION-ANALYSIS [J].
TOPLISS, JG ;
COSTELLO, RJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1972, 15 (10) :1066-&
[10]  
WOODBURY LA, 1952, ARCH INT PHARMACOD T, V92, P97