Sivelestat (INN, research name ONO 5046, marketed as Elaspol) is an inhibitor of human neutrophil elastase.[1]

It is used in the treatment of acute respiratory failure[2] and preliminary studies show it may also improve neuropathic pain.[3]

Synthesis

Sivelestat is synthesised as follows:[4]

References

  1. ^ Kawabata K, Suzuki M, Sugitani M, Imaki K, Toda M, Miyamoto T (June 1991). "ONO-5046, a novel inhibitor of human neutrophil elastase". Biochemical and Biophysical Research Communications. 177 (2): 814–820. doi:10.1016/0006-291X(91)91862-7. PMID 2049103.
  2. ^ Imokawa S, Mori K, Harada M, Sagisaka S, Sano T, Uchiyama H, et al. (June 2008). "[Acute respiratory failure due to pneumocystis pneumonia successfully treated with combined use of sivelestat sodium hydrate]". Nihon Kokyuki Gakkai Zasshi = the Journal of the Japanese Respiratory Society (in Japanese). 46 (6): 461–465. PMID 18592991.
  3. ^ Weyer AD, Stucky CL (May 2015). "Repurposing a leukocyte elastase inhibitor for neuropathic pain". Nature Medicine. 21 (5): 429–430. doi:10.1038/nm.3861. PMID 25951529. S2CID 10240018.
  4. ^ US 5017610, Imaki K, Arai Y, Okegawa T, "Derivatives of p-substituted phenyl ester of pivalic acid", issued 21 May 1991, assigned to Ono Pharmaceutical Co Ltd 
Allikas: http://en.wikipedia.org/wiki/Sivelestat
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