Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation was written by Woodring, Jennifer L.;Bachovchin, Kelly A.;Brady, Kimberly G.;Gallerstein, Mitchell F.;Erath, Jessey;Tanghe, Scott;Leed, Susan E.;Rodriguez, Ana;Mensa-Wilmot, Kojo;Sciotti, Richard J.;Pollastri, Michael P.. And the article was included in European Journal of Medicinal Chemistry in 2017.Related Products of 5469-70-5 This article mentions the following:
Human African trypanosomiasis (HAT) is a deadly disease in need of new chemotherapeutics that can cross into the central nervous system. The authors previously reported the discovery of (NEU-617), a small mol. with activity against T. brucei bloodstream proliferation. Further optimization of NEU-617 to improve the physicochem. properties (LogP, LLE, [1], and MPO score) [2] have led us to twelve sub-micromolar compounds, most importantly the headgroup variants I and II, and the linker variant III. Although these 3 compounds had reduced potency compared to NEU-617, they all had improved LogP, LLE and MPO scores. Cross-screening these analogs against other protozoan parasites uncovered IV with potent activity towards T. brucei, T. cruzi and L. major, while four others compounds showed activity towards P. falciparum D6. This reinforces the effectiveness of lead repurposing for the discovery of new protozoan disease therapeutics. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Related Products of 5469-70-5).
3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazines are rare in nature, possibly reflecting the scarcity of naturally occurring hydrazines, common building blocks for the synthesis of these heterocycles. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Related Products of 5469-70-5
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem