Application In Synthesis of Pyridazin-4-amine, The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states.
From a high-throughput screen of 42 444 known human kinases inhibitors, a pyrazolo[1,5-b]pyridazine scaffold was identified to begin optimization for the treatment of human African trypanosomiasis. Previously reported data for analogous compounds against human kinases GSK-3beta, CDK-2, and CDK-4 were leveraged to try to improve the selectivity of the series, resulting in 23a which showed selectivity for T. b. brucei over these three human enzymes. In parallel, properties known to influence the absorption, distribution, metabolism, and excretion (ADME) profile of the series were optimized resulting in 20g being progressed into an efficacy study in mice. Though 20g showed toxicity in mice, it also demonstrated CNS penetration in a PK study and significant reduction of parasitemia in four out of the six mice.
The result showed that such a combination of chemo- and biocatalysis improved the catalytic yield more than two times compared with that of sole metal catalysis.I hope my blog about 20744-39-2 is helpful to your research.Application In Synthesis of Pyridazin-4-amine
Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N147 – PubChem