145708-16-3Relevant articles and documents
Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease
Nagarajan, Srinivasan R.,De Crescenzo, Gary A.,Getman, Daniel P.,Lu, Hwang-Fun,Sikorski, James A.,Walker, Jeffrey L.,McDonald, Joseph J.,Houseman, Kathryn A.,Kocan, Geralyn P.,Kishore, Nandini,Mehta, Pramod P.,Funkes-Shippy, Christie L.,Blystone, Lisa
, p. 4769 - 4777 (2007/10/03)
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.
HETEROCYCLECARBONYL AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS
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, (2008/06/13)
Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
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, (2008/06/13)
PCT No. PCT/US96/00607 Sec. 371 Date Feb. 26, 1998 Sec. 102(e) Date Feb. 26, 1998 PCT Filed Jan. 18, 1996 PCT Pub. No. WO96/22287 PCT Pub. Date Jul. 25, 1996Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.