Synthesis of piscidinol A derivatives and their ability to inhibit HIV-1 protease.

Abstract:

:Four types of piscidinol A derivatives were synthesized and evaluated their ability to inhibit HIV-1 protease to understand their structure-activity relationships. Of these tirucallane-type triterpene derivatives, an A-seco derivative (1b) moderately inhibited human immunodeficiency virus (HIV) protease (IC50 38.2 μM). The 2,2-dimethyl succinic acid (DMS) acylated tirucallane derivatives (4b, 6a, and 7b, 50 < IC50 < 100 μM) were more inhibitory against HIV-1 PR than the others (PA, 2a, 4a, 4c-4d, 5a, 6b-6d, and 7a, IC50 > 100 μM). These findings indicated that the 2,3-seco-2,3-dioic acid (1b) and DMS-acylated tirucallane-type derivatives preferably inhibited HIV viral protease.

journal_name

J Asian Nat Prod Res

authors

Wei Y,Ma CM,Jiang TB,Du J,Zhou X,Liu GQ,Hattori M

doi

10.1080/10286020.2015.1084505

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

1079-90

issue

11

eissn

1028-6020

issn

1477-2213

journal_volume

17

pub_type

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