| 摘要 |
<p>Indolizino-isoquinoline derivs. of formula (I) and their acid addn. salts are new (where R is opt. branched alkyl of which the terminal C-atom is substd. by a dialkylaminomethyl residue or by a satd. 5- or 6-membered N-heterocyclylmethyl residue opt. contg. N (opt. N-methylated), O or S as a further hetero atom. The various alkyl residues are 1-4C). (I) are antimicrobial and antifungal agents with low toxicity (mouse toxicity 750 mg/kg or more p.o.). (I) are active in vitro against Gram-pos. organisms (active at concns. of 0.1-2 mu g/ml against Staphylococcus aureus 209P) and most cpds. (I) are active against Gram-neg. organisms e.g. active against E. coli Monod at concns. of 0.1-20 mu g/ml). Antifungal activity is shown against Saccharomyces pastorianus at concns. of 1-125 mu g/ml. Specific. cpds. (I) include 4-(2-diethylaminoethoxy)-10-nitro-7-oxo-7H-indolizino 7,6,5-de is- oquinoline. In an example, this is prepd. by nitration of 4-(2-diethylaminoethoxy)-7-oxo-7H-indolizino 7,6,5-d,e isoquinoli- ne with a mixt. of HNO3 d = 1.33 and HNO3 d = 1.52.</p> |
