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Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease by Srinivasan R Nagarajan; Gary A De Crescenzo; Daniel P Getman; Hwang-Fun Lu; James A Sikorski; Jeffrey L Walker; Joseph J McDonald; Kathryn A Houseman; Geralyn P Kocan; Nandini Kishore; Pramod P Mehta; Christie L Funkes-Shippy; Lisa Blystone is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease about?

The human immunodeficiency virus (HIV) has been shown to be the causative agent for AIDS. The HIV virus encodes for a unique aspartyl protease that is essential for the production of enzymes and proteins in the final stages of maturation. Protease inhibitors have been useful in combating the disease. The inhibitors incorporate a variety of isosteres including the hydroxyethylurea at the protease cleavage site. We have shown that the replacement of t-butylurea moiety by benzothiazolesulfonamide provided inhibitors with improved potency and antiviral activities. Some of the compounds have shown good oral bioavailability and half-life in rats. The synthesis of benzothiazole derivatives led us to explore other heterocycles. During the course of our studies, we also developed an efficient synthesis of benzothiazole-6-sulfonic acid via a two-step procedure starting from sulfanilamide.

Who reads Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease?

Author

Srinivasan R Nagarajan; Gary A De Crescenzo; Daniel P Getman; Hwang-Fun Lu; James A Sikorski; Jeffrey L Walker; Joseph J McDonald; Kathryn A Houseman; Geralyn P Kocan; Nandini Kishore; Pramod P Mehta; Christie L Funkes-Shippy; Lisa Blystone

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2003

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)