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Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles.

Abstract：

:The human T cell leukemia/lymphotropic virus type 1 (HTLV-I) is clinically associated with adult T cell leukemia/lymphoma, HTLV-I associated myelopathy/tropical spastic paraparesis, and a number of other chronic inflammatory diseases. To stop the replication of the virus, we developed highly potent tetrapeptidic HTLV-I protease inhibitors. In a recent X-ray crystallography study, several of our inhibitors could not form co-crystal complexes with the protease due to their high hydrophobicity. In the current study, we designed, synthesized and evaluated the HTLV-I protease inhibition potency of compounds with hydrophilic end-capping moieties with the aim of improving pharmaceutic and pharmacokinetic properties.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nguyen JT,Kato K,Hidaka K,Kumada HO,Kimura T,Kiso Y

doi

10.1016/j.bmcl.2011.02.066

subject

Has Abstract

pub_date

2011-04-15 00:00:00

pages

2425-9

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00250-2

journal_volume

21

pub_type

杂志文章

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