Bioorganic and Medicinal Chemistry Letters p. 1427 - 1432 (1997)
Update date:2022-09-26
Topics:
Lee, Dennis
Marshall, Lisa A.
Bolognese, Brian
Adams, Jerry L.
A series of substrate analog inhibitors of 14 kDa PLA2 possessing replacements for the sn-3 phosphate moeity was prepared and evaluated. Tetrazole 26 possessed similar in vitro inhibition potency to phosphate-containing substrate analog inhibitors, but demonstrated superior cell permeability as monitored by LTC4 release in monocytes.
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