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Umbelliferone aminoalkyl derivatives, a new class of squalene-hopene cyclase inhibitors.

Abstract：

:The synthesis is described of several aminoalkyl derivatives of coumarin, obtained in good yields under microwave or high-intensity ultrasound irradiation. These compounds proved uniformly active as inhibitors of squalene-hopene cyclase (SHC) from Alicyclobacillus acidocaldarius. Their design stemmed from our recent finding that the umbelliferone nucleus acquires inhibitory properties towards SHC when functionalized with a suitable chain such as the omega-epoxyfarnesyl group. Under our experimental conditions the most active ones, such as 7-(4'-allylmethylamino-but-2-ynyloxy)chromen-2-one (IC(50) 0.75 mM), approached the potency of anticholesteremic drug Ro 48-8071 (IC(50) 0.35 mM), an effective inhibitor of both squalene- and oxidosqualene-cyclases (OSC). Tests are in progress to determine their efficacy on different eukaryotic OSCs.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Cravotto G,Balliano G,Tagliapietra S,Palmisano G,Penoni A

doi

10.1016/j.ejmech.2004.06.010

subject

Has Abstract

pub_date

2004-11-01 00:00:00

pages

917-24

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(04)00150-3

journal_volume

39

pub_type

杂志文章

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