2. Academic Validation
  3. Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'

Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'

  • Bioorg Med Chem Lett. 2001 Feb 26;11(4):587-90. doi: 10.1016/s0960-894x(01)00003-8.
K Seno 1,  T Okuno,  K Nishi,  Y Murakami,  K Yamada,  S Nakamoto,  T Ono
Affiliations

Affiliation

  • 1 Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan. [email protected]
PMID: 11229777 DOI: 10.1016/s0960-894x(01)00003-8
Abstract

We synthesized a potent and crystallized human cytosolic Phospholipase A2alpha inhibitor, pyrrophenone (6) which inhibits the isolated Enzyme with an IC50 value of 4.2 nM. Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglandin E2, thromboxane B2, and leukotriene B4 formation in human whole blood. The magnitudes of prostaglandin E2 and thromboxane B2 inhibition are the same as those of indomethacin.

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