The University of North Carolina at Chapel Hill

Other

Biotech Research Laboratories

Biotech Research Labs, Inc.

Louis Mark Cosentino

Kuo-Hsiung Lee

Yoshiki Kashiwada

Mark Manak

Yung-Chi Cheng

Lan Xie

Hui-Kang Wang

Fumio Hashimoto

Robert Kilkulskie

Jing-Xi Xie

I-Chen Sun

Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have the following formulae:

Acylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof

Some betulinic acid and dihydrobetulinic acid acyl derivatives according to the present invention have been found to have potent anti-HIV activity. Introducing a C.sub.2 -C.sub.20 substituted or unsubstituted acyl group at the C.sub.3 -hydroxy group of betulinic acid and dihydrobetulinic acid produces the corresponding 3-O-acyl derivatives. The compounds of the present invention have the following formulae: ##STR1## where R may be a mono- or dicarboxylacyl group, substituted or unsubstituted, of from about 2 to about 20 carbon atoms, and R' may be hydrogen or a C.sub.2 -C.sub.10 substituted and unsubstituted alkyl or aryl group.

Betulinic acid and dihydrobetulinic acid derivatives and uses therefor

Disclosed herein are derivatives of 4,4'-dimethoxy-5,6,5'6'-bimethylenedioxy 2,2'-dimethoxycarbonyl biphenyl (DDB) which were synthesized and found to have anti-HIV activity. Of the compounds studied, 3,3'-dibromo DDB and 3-bromo-DDB initially exhibited the greatest anti-HIV activity.

Brominated hexahydroxybiphenyl derivatives

Growing community of inventors

Springfield, VA, United States of America

Louis Mark Cosentino