W. Malinka, Synthesis of some pyrrolo[3,4-d]pyridazinones and their preliminary anticancer, antimycobacterial and CNS screening, PHARMAZIE, 56(5), 2001, pp. 384-389
Starting from 1-substituted-2,5-dimethyl-3,4-pyrroledicarboxylic acid anhyd
rides 1 and N-methylhydrazine, 1,2,3,4-tetrahydro-6-substituted-2,5,7-trime
thyl-6H-pyrrolo[3,4-d]pyridazin-1,4-ones 2 were prepared. Reaction of compo
unds 2 with alkylating agents give 3-N- or 4-O-alkylated products 3, 4 or m
ixtures of these isomers in ratios depending on the alkylating agents. Unde
r preliminary pharmacological screening two of four new pyrrolo[3,4-d]pyrid
azinones were active as cystostatic agents, all the eight compounds display
ed moderate activity against Mycobacterium tuberculosis and two compounds w
ere active as CNS-depressive agents.