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2004
Enzyme inhibiting activity
X 0220
Novel δ2-Isoxazolines as Group II Phospholipase A2 Inhibitors. — Novel imidazolyl δ2-isoxazoline libraries are constructed via key intermediate (I) through 1,3-dipo47- 217 lar
cycloaddition reaction with dipolarophiles like mono substituted alkenes. The crystal structure of imidazolylcarbaldehyde oxime (I) is determined by X-ray diffraction.
The novel δ2-isoxazolines are evaluated for their phopholipase A2 enzyme inhibitory
activity against snake venom source and the structure—activity relationship of this type
of molecules is discussed. The new compounds exert significant PLA2 enzyme inhibitory activity against group II PLA2. Compounds (II) show antiinflammatory in vivo activity, comparable to that of ursolic acid. — (BASAPPA; KUMAR, M. S.; SWAMY, S.
N.; MAHENDRA, M.; PRASAD, J. S.; VISWANATH, B. S.; RANGAPPA*, K. S.;
Bioorg. Med. Chem. Lett. 14 (2004) 14, 3679-3681; Dep. Stud. Chem., Univ. Mysore,
Manasagangotri, Mysore 570 006, India; Eng.) — H. Hoennerscheid
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