Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2

R Lucas; A Ubeda; M Payá; M Alves; E del Olmo; J L López; A San Feliciano

doi:10.1016/s0960-894x(99)00680-0

Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2

Bioorg Med Chem Lett. 2000 Feb 7;10(3):285-8. doi: 10.1016/s0960-894x(99)00680-0.

Authors

R Lucas¹, A Ubeda, M Payá, M Alves, E del Olmo, J L López, A San Feliciano

Affiliation

¹ Departmento de Farmacología, Univ. de Valencia, Burjassot, Spain.

PMID: 10698455
DOI: 10.1016/s0960-894x(99)00680-0

Abstract

We have synthesised some lipidic diamines and aminoalcohols and examined their behaviour as inhibitors of secretory and cytosolic PLA2. Some structure-activity relationships considerations have been deduced. Compound 14 was a potent and selective inhibitor of cPLA2 and compound 4 showed a dual inhibitory profile against both types of PLA2 while no cytotoxicity at 10 microM on human neutrophils or on murine macrophage line was observed for both.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amino Alcohols / chemical synthesis*
Amino Alcohols / pharmacology
Animals
Cell Line
Cytosol / enzymology*
Diamines / chemical synthesis*
Diamines / pharmacology
Humans
Lipids / chemistry
Mice
Phospholipases A / antagonists & inhibitors
Phospholipases A / metabolism*
Phospholipases A2
Recombinant Proteins / antagonists & inhibitors
Recombinant Proteins / metabolism
Structure-Activity Relationship
Substrate Specificity

Substances

Amino Alcohols
Diamines
Lipids
Recombinant Proteins
Phospholipases A
Phospholipases A2