Design and synthesis of new secretory phospholipase A2 inhibitor of a phospholipid analog

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 24, 1998, Pages 3495-3498

  Iwama, Seiji ^a   Segawa, Masaki ^a   Fujii, Shinobu ^b   Ikeda, Kiyoshi ^b   Katsumura, Shigeo ^a  

^a KWANSEI GAKUIN UNIVERSITY   (Japan)

^b OSAKA MEDICAL COLLEGE   (Japan)

Author keywords

Oxazolidinone phospholipid analog; Phospholipase A2; Stereoselective synthesis; Stronger inhibitory activity

Indexed keywords

OXAZOLIDINONE DERIVATIVE; PHOSPHOLIPASE A2 INHIBITOR; PHOSPHOLIPID DERIVATIVE;

ARTICLE; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

DRUG DESIGN; ENZYME INHIBITORS; PHOSPHOLIPASES A; PHOSPHOLIPIDS; STEREOISOMERISM;

EID: 0032535313     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00641-6     Document Type: Article

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11. 2P 507.3187.
12. 11. The enzyme activity was measured toward a monodispersed substrate 1 b in the presence of 3.3mM calcium chloride by using the pH-stat method at 25 °C, pH 8.2, and ionic strength 0.1.
13. 2 was performed at a constant temperature (300K) with a dielectric constant of 80 in gas phase.
14. 13. The model building and structure analysis followed by molecular mechanics and dynamics simulation were performed with Insight II 2.1.0, Program and Discover 2.9 Program Biosym Technol Inc. San Diego, USA.