Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity
Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity
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DOI：
10.1016/j.bmcl.2006.03.048
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发表时间：
2006-06-15
影响因子：
2.7
通讯作者：
Woster, Patrick M.
中科院分区：
文献类型：
--
作者：
Bi, Xiangdong;Lopez, Christina;Woster, Patrick M.
合成了一系列多氨基胍和多氨基双胍类抗锥虫药物。这些类似物抑制锥虫硫酮还原酶（TR），IC 50值低至0.95 μ M，但不抑制密切相关的人酶谷胱甘肽还原酶（GR）。最有效的类似物，7a，7b和8d，在体外抑制寄生虫的生长，IC 50值分别为0.18，0.09和0.18 μ M。这些药物代表了一类有前途的新的潜在抗锥虫药物。(c)2006爱思唯尔有限公司保留所有权利。
A series of polyaminoguanidines and polyaminobiguan ides were synthesized and evaluated as potential antitrypanosomal agents. These analogues inhibit trypanothione reductase (TR) with IC50 values as low as 0.95 mu M, but do not inhibit the closely related human enzyme glutathione reductase (GR). The most effective analogues, 7a, 7b and 8d, inhibited parasitic growth in vitro with IC50 values of 0.18, 0.09 and 0.18 mu M, respectively. These agents represent a promising new class of potential antitrypanosomal agents. (c) 2006 Elsevier Ltd. All rights reserved.