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Lipoxygenase Inhibitors, Part 6[1]. Synthesis of New Tetrahydropyrazine and Other Heterocyclic Compounds by Reaction of Hydrazonoyl Chlorides

✍ Scribed by Petra Frohberg; Michael Wiese; Peter Nuhn

Book ID
102750456
Publisher
John Wiley and Sons
Year
1997
Tongue
English
Weight
646 KB
Volume
330
Category
Article
ISSN
0365-6233

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✦ Synopsis

Cyclization reactions of a-ketoarylhydrazonoyl chlorides with various dinucleophiles lead to new 1,4-benzothiazine, quinoxaline, tetrahydropyrazine, thiazole, and thiadiazoline derivatives of methyl butanoate or methyl 5-oxopentanoate. The inhibition of 5-lipoxygenase (LO) was determined by monitoring the leukotriene B j (LTB4) formation of human polymorphonuclear leukocytes (PMNL). The IC50 values for the most active compounds with an arylhydrazone structure were found to lie between 0.7 and 7.5 pM.

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