SYNTHESIS AND ANTICONVULSANT PROPERTIES OF 3-(1,3,4-THIADIAZOL-2-YL)THIAZOLIDIN-4-ONES

被引：0
|
作者：
CHIMIRRI, A
GRASSO, S
MONFORTE, AM
ZAPPALA, M
DESARRO, A
DESARRO, GB
机构：
[1] UNIV MESSINA,FAC MED & CHIRURG,IST FARMACOL,I-98122 MESSINA,ITALY
[2] UNIV REGGIO CALABRIA,FAC MED & CHIRURG,IST FARMACOL,I-8100 CATANZARO,ITALY
来源：
FARMACO | 1991年 / 46卷 / 7-8期
关键词：
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A series of 2-substituted 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-ones were synthesized and evaluated for anticonvulsant activity in a genetic model of reflex epilepsy (sound-induced seizures in DBA/2 mice). The combination of preferred substituents in the 2-position coupled with the introduction of a mercapto group on the thiadiazole moiety led to a number of active compounds. The anticonvulsant activity of most derivatives is better than that of the clinically useful anticonvulsant sodium valproate and some of them appear to possess potencies in the same range as phenytoin and clobazam.
引用
收藏
页码：935 / 943
页数：9
相关论文
共 50 条
  • [1] 3-[5-(4-Fluorophenyl)-1,3,4-thiadiazol-2-yl]-2-phenyl-thiazolidin-4-one
    Wan, R
    Wu, F
    Yin, J
    Wang, JT
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2006, 62 : O746 - O747
  • [2] 2-phenyl-3-{5-[3-(trifluoromethyl)phenyl]1,3,4-thiadiazol-2-yl}thiazolidin-4-one
    Wan, Rong
    Wu, Feng
    Han, Feng
    Cao, Lin
    Wang, Jin-Tang
    ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2006, 62 : O4072 - O4074
  • [3] 3-(α-phosphorylalkyl)thiazolidin-4-ones
    Onysko, PP
    Kim, TV
    Kiseleva, EI
    Sinitsa, AD
    ZHURNAL OBSHCHEI KHIMII, 1997, 67 (10): : 1642 - 1645
  • [4] 2-(4-fluorophenyl)-3-[5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl]thiazolidin-4-one
    Wan, Rong
    Wu, Feng
    Guan, Jian-Ling
    Han, Feng
    Wang, Jin-Tang
    ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2006, 62 : O3984 - O3985
  • [5] 2-(4-chlorophenyl)-3-[5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl] thiazolidin-4-one
    Wan, Rong
    Guan, Jianning
    Han, Feng
    Wu, Feng
    Wang, Jin-Tang
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2006, 62 : O5274 - O5275
  • [6] 3-[5-(3,5-dimethylphenyl)-1,3,4-thiadiazol-2-yl]-2-(4-methoxyphenyl)thiazolidin-4-one
    Wan, R
    Wu, F
    Cao, L
    Wang, JT
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2006, 62 : O2115 - O2116
  • [7] Bis(1,3,4-thiadiazol-2-yl) disulfide
    Hu, Pu-Zhou
    Zhang, Yong-Hua
    Wang, Jian-Ge
    Qin, Jian-Hua
    Zhao, Bang-Tun
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2009, 65 : O2483 - +
  • [8] Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl) thiazolidin-4-one derivatives
    Buemi, Maria Rosa
    Gitto, Rosaria
    Ielo, Laura
    Pannecouque, Christophe
    De Luca, Laura
    BIOORGANIC & MEDICINAL CHEMISTRY, 2020, 28 (08)
  • [9] 3-[5-(4-fluorophenyl)-1,3,4-thiadiazol-2-yl]-2-(4-methoxyphenyl)-1,3-thiazolidin-4-one
    Yin, Li-He
    Wan, Rong
    Han, Feng
    Wang, Bin
    Wang, Jin-Tang
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2008, 64 : O1359 - U2756
  • [10] 2-(4-Fluorophenyl)-3-[5-(4-nitrophenyl)-1,3,4-thiadiazol-2-yl]-1,3-thiazolidin-4-one
    Yu, Peng
    An, Kang
    He, Qiu
    Zhang, Jian-Qaing
    Wan, Rong
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O1737 - U869
12345