This invention relates to certain bicyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections.
In accordance with the present invention there are provided compounds of general formula I or a pharmaceutically acceptable salt or in vivo hydrolyzable ester R
5
thereof:
wherein: One of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X═O or S.
本发明涉及某些双环6-烷基亚烯基
青霉素类化合物,其作为D类酶的
抑制剂。β-内酰胺酶
水解β-内酰胺类抗生素,因此是细菌耐药的主要原因。本发明的化合物与β-内酰胺类抗生素结合后,将提供有效的治疗致命细菌感染的方法。根据本发明,提供了一般式I的化合物或其药学上可接受的盐或体内可
水解的酯R5:其中:A和B中的一个表示氢,另一个表示可选的取代的融合双环杂环基;X═O或S。