Synthesis of some pyrrolo[3,4-d]pyridazinones and their preliminary anticancer, antimycobacterial and CNS screening

Authors
Citation
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
Citations number
17
Categorie Soggetti
Pharmacology & Toxicology
Journal title
PHARMAZIE
ISSN journal
00317144 → ACNP
Volume
56
Issue
5
Year of publication
2001
Pages
384 - 389
Database
ISI
SICI code
0031-7144(200105)56:5<384:SOSPAT>2.0.ZU;2-E
Abstract
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.