Indolizine 1-sulfonates as potent inhibitors of 15-lipoxygenase from soybeans
2005; Elsevier BV; Volume: 13; Issue: 9 Linguagem: Inglês
10.1016/j.bmc.2005.02.056
ISSN1464-3391
AutoresSolomon Teklu, Lise‐Lotte Gundersen, Tove Larsen, Karl Egil Malterud, Frode Rise,
Tópico(s)Synthesis and Biological Evaluation
ResumoA number of indolizine 1-sulfonates have been prepared by cyclization of cyclopropenones with pyridines followed by trapping of the intermediate 1-indolizinol with a sulfonyl halide, and examined as inhibitors of 15-lipoxygenase (15-LO). The compounds display IC(50) values between 15 and 42 microM; all are more active than the well-known 15-LO inhibitor quercetin (IC(50) 51 microM). A wide variety of substituents are well tolerated. The enzyme inhibition was not affected by preincubation or the presence of a detergent and no significant particle formation was observed. Hence, inhibition from aggregates of indolizines, promiscuous inhibition, is highly unlikely.
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