Dihydrofolate reductase inhibitors as antibacterial agents
Dihydrofolate reductase inhibitors as antibacterial agents
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DOI：
10.1016/j.bcp.2005.10.052
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发表时间：
2006-03-30
影响因子：
5.8
通讯作者：
Islam, K
中科院分区：
文献类型：
--
作者：
Hawser, S;Lociuro, S;Islam, K
虽然只有少数DHFR抑制剂作为抗生素进入市场，但人们对新一代DHFR抑制剂作为抗菌剂的发现和开发重新产生了兴趣。本文介绍了以甲氧苄啶（TMP）为例成功开发DHFR作为可药物靶点和几种新的二氨基嘧啶的开发。Iclaprim是目前处于III期临床试验的新型二氨基嘧啶的最新例子，也与临床前开发的抗dhfr抗菌化合物的几个例子一起进行了描述。(c) 2005爱思唯尔公司版权所有。
Although only a few DHFR inhibitors have progressed as antibiotics to the market there is much renewed interest in the discovery and development of new generation DHFR inhibitors as antibacterial agents. This article describes the success in exploiting DHFR as a drugable target as exemplified by trimethoprim (TMP) and the development of several new diaminopyrimidines. Iclaprim, a recent example of a novel diaminopyrimidine currently in Phase III clinical trials, is also described together with several examples of anti-DHFR antibacterial compounds in pre-clinical development. (c) 2005 Elsevier Inc. All rights reserved.