New arylsulfonohydrazide inhibitors of enzymes MurC and MurD
申请人:UNIVERZA V LJUBLJANI, FAKULTETA ZA FARMACIJO
公开号:EP1845083A2
公开(公告)日:2007-10-17
This invention belongs to the field of pharmaceutical chemistry and relates to new arylsulfonohydrazides as inhibitors of UDP-N-acetylmuramyl:L-alanine ligaze (MurC) and UDP-N-acetylmuramyl-L-alanine:D-glutamate ligaze (MurD), to procedures for their preparation and pharmaceutical preparations containing the same. The enzymes MurC and MurD are the key enzymes involved in the synthesis of bacterial peptidoglycan, so arylsulfonohydrazide inhibitors possess antibacterial activity. Compounds of general formula I
and the pharmaceutically acceptable salts are described. The appropriate substituents are clearly presented in the body of the text and in claims.
本发明属于药物化学领域,涉及作为 UDP-N-乙酰基氨酰基:L-丙氨酸连接酶(MurC)和 UDP-N-乙酰基氨酰基-L-丙氨酸:D-谷氨酸连接酶(MurD)抑制剂的新型芳基磺酰肼、其制备方法以及含有这些抑制剂的药物制剂。MurC 和 MurD 是参与合成细菌肽聚糖的关键酶,因此芳基磺酰肼抑制剂具有抗菌活性。通式 I 的化合物
及其药学上可接受的盐类。适当的取代基在正文和权利要求中均有清楚的表述。
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