137384-49-7Relevant academic research and scientific papers
Synthetic studies on condensed-azole derivatives. IV. Synthesis and anti-asthmatic activities of ω-sulfamoylalkyloxyimidazo[1,2-b]pyridazines
Kuwahara, Masaaki,Kawano, Yasuhiko,Shimazu, Hiroshi,Ashida, Yasuko,Miyake, Akio
, p. 122 - 131 (2007/10/03)
A series of novel (imidazo[1,2-b]pyridazin-6-yl)oxyalkylsulfonamides was synthesized and evaluated for the ability to inhibit platelet activating factor (PAF)-induced bronchoconstriction in guinea pigs. The compounds bearing a gem-dialkyl or a cycloalkylidene group at the 2 position of the sulfamoylpropyloxy group in the side chain were found to have potent activity. Among them, 3-(imidazo[1,2-b]pyridazin-6-yl)oxy-2,2-dimethylpropanesulfonamide (6) showed excellent anti-asthmatic activity and the longest duration of action. The compounds bearing a methyl group at the 7 or 8 position of the imidazo[1,2-b]pyridazine ring were found to have enhanced activity. Among them, 3-(7-methylimidazo[1,2-b]pyridazin-6-yl)oxy-2,2-dimethylpropanesulfonamide (25) showed the most potent inhibitory effect, and its anti-asthmatic effect in an experimental model of allergic asthma was superior to that of theophylline. The structure-activity relationships in this series of compounds are discussed.
Imidazopyridazines, their production and use
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, (2008/06/13)
An imidazo [1,2-b]pyridazine compound of the formula (I): STR1 wherein R1 is a halogen atom or a lower alkyl group optionally having substituent(s), R2 and R3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R2 and R3 together with the adjacent nitrogen atom to which they bond may form a heterolcyclic ring optionally having substituent(s), X is an oxygen atom or S(O)k (k is zero to two), a group -- A-- is a bivalent three to seven membered homocyclic or heterocyclic group optionally having substituent(s), m1 and m2 each is an integer of 0 to 4 and n is an integer of 0 or 1; or its salt, which is useful as antiasthmatics.
