Study On The Synthesis And Preliminary In-vitro Antibacterial Activity And Acute Toxicity Of The Derivativeof Cefmenoxime

Infectious diseases have represented one of the great scourges since the dawn of humanity,the cephalosporins played an important role in the treatment with these diseases.Among the50or so cephalosporins on the market,there were nearly10of them whose C3-position containing1-methyl-lH-tetrazole-5-thiol(N-methylthiotetrazole,NMTT)group.These drugs were used extensively in clinical practices,but due to the NMTT group,there are two distinct side effects,which are hypoprothrombinemia and disulfiram effects.In this article,cefmenoxime was picked up as the mother compound,according to minimal modification principle,the C3-side chain of ceforanide which was2-(5-mercapto-lH-tetrazol-1-yl)acetic acid(MTAA) and C7-side chain of cefozopran which is Z-1-(5-amino-1,2,4-thiodiazol-3-yl)-1-methoxyiminoacetyl were introduced to the C3-and C7-position of the mother compound respectively,finally new derivatives L-1and L-2were obtained.The aim of L-1was to lower the mother compound’s side effects. The aim of L-2was investigated for the side effects whether or not related to the C7-side chain of the mother compound.Through information retrieving,L-1and L-2were proved to be new compounds,the structure of L-1was confirmed by spectral analyses,and the structure of L-2was partly confirmed.Preliminary in-vitro antibacterial activity and acute toxicity studies were carried on L-1and L-2.