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Potent HIV protease inhibitors containing a novel (2-phenylsulfanyl-1-hydroxyethyl)amide isostere

โœ Scribed by L. Rocheblave; G. Priem; C. De Michelis; J.L. Kraus


Book ID
104261490
Publisher
Elsevier Science
Year
1999
Tongue
French
Weight
187 KB
Volume
40
Category
Article
ISSN
0040-4039

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โœฆ Synopsis


Based on the concept of bioisosterism, we report the design and synthesis of new protease inhibitors. These new compounds incorporate in their backbone the synthon 2-N-Acyl-2-Phenylsulfanyl-1-Hydroxyethyl (I) which confers on the resulting compounds both in vitro activity on MT4 infected c~lls and HIV-I protease inhibition properties.


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(Hydroxyethyl) sulfonamide HIV-1 Proteas
โœ John N. Freskos; Deborah E. Bertenshaw; Daniel P. Getman; Robert M. Heintz; Bren ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 260 KB

Abstrf, et : We have discovered a potent low molecular weight series of HIV-1 Protease inhibitors incorporating the (R)-(hydroxyethyl) sulfonamide isostere. The human immunodeficiency virus type-1 (HIV-1), the causative agent of AIDS, encodes for a unique aspartyl protease, which has been shown to