Synthesis and Ca2+-desensitizing Activity of 2-methyl-7-aryl(α-furyl)-[1,3]thiazolo[4,5-d]pyridazin-4(5H)-ones

Aims: Search of new chemical compounds for pressure decrease in accordance with new mode of action.

Study Design: Novel 2-methyl-7-aryl(α-furyl)-[1,3]thiazolo[4,5-d]pyridazin-4(5H)-ones were synthesized in 67-84% yields via reaction of 2-methyl-5-benzoyl(furoyl)-thiazol-4-carboxylates with hydrazines.

Place and Duration of Study: Synthesis of new compounds has been performed at National T. Shevchenko University “Chernihiv Collegium” and Institute of Pharmacology and Toxicology, National Academy of Medical Sciences. Physiological studies have been conducted at Institute of Pharmacology and Toxicology, National Academy of Medical Sciences of Ukraine.

Methodology: Design of chemical structures which relax vascular smooth muscle cells without significant decreasing in intracellular calcium concentration, [Ca2+]i.

Results: These new compounds have been successfully tested for the aim to search so-called calcium desensitizers, i.e. compounds which possess the ability to decrease Ca2+-sensitivity of myofilaments and therefore, vascular smooth muscle cells (VSMc) contractility and, hence, vascular tone.

Conclusion: 2-Methyl-7-aryl(α-furyl)-[1,3]thiazolo[4,5-d]pyridazin-4(5H)-ones may be used in future as safety and good therapeutic approach under arterial hypertension and local vasospasm development.