新型碳青霉烯类抗生素

New carbapenem antibiotics

自硫霉素被发现以来 ,碳青霉烯类抗生素亚胺培南 西司他丁、帕尼培南 倍他米隆和美罗培南已用于临床多种耐药菌引起的严重感染的治疗。目前 ,碳青霉烯类抗生素的主要研究领域是开发对肾脱氢肽酶I(DHP I)稳定、抗铜绿假单胞菌和抗耐甲氧西林的金葡球菌 (MRSA)活性强的长效口服药物。正在开发的碳青霉烯主要有抗MRSA活性较强的L 6 95 2 5 6 ,L 786 392 ,BO 3482 ,SM 174 6 6 ,FR 2 1818和J 1112 2 5 ,抗铜绿假单胞菌活性较强的为DX 8739,S 4 6 6 1,BO 2 5 0 2A ,ER 35 786和BMS 181139,长效活性的有L 74 9345 ,BO 2 72 7,口服给药的有GV 118819,CS 834,DZ 2 6 4 0 ,CL 19112 1和L 0 84等。

Since the discovery of thienamycin,carbapenem antibiotics imipenem cilastatin,panipenem betamipron and meropenem have been used in clinical treatment of severe bacterial infections caused by multidrug resistant strains. Parenteral and oral carbapenem antibiotics, without coadministration of cilastatin or betamipron have been extensively studied. Present research is focused on the discovery of anti MRSA and antipseudomonal carbapenems, novel long acting carbapenems and new oral carbapenems exhibiting no cross resistance with cephalosporins and new quinolones.Anti MRSA carbapenems L 695256, L 786392,BO 3482,SM 17466,FR 21818 and J 111225,antipseudomonal carbapenems DX 8739,S 4661,BO 2502A,ER 35786 and BMS 181139,long acting carbapenems L 749345 and BO 2727, oral carbapenems GV 118819,CS 834,DZ 2640,CL 191121 and L 084 are in developing practice.