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Cn Nefinavir is the first HIV protease inhibitor for grown-ups and children. An efficient and environmentally friendly procedure for the one-pot synthesis of (3S,4aS,8aS)-2((2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyl)-N-tert-butyl-decahydroisoquinoline-3carboxamide, the intermediate of nelfinavir was described, and activating ester was applied to afford nelfinavir. Under the catalysis of potassium hydroxide, benzyl (R)-1((S)-oxiran-2-yl)-2-(phenylthio) ethyl carbamate was obtained in methanol.
Edu 3-Deazapurine nucleosides show significant antiviral potential. Within this category, carbocyclic nucleosides have shown particular promise. A particular noteworthy example is 3-deaza-5'-noraristeromycin (1). In the rational design of derivatives of 1, as a means to improve upon its antiviral scope, substituents at the C-3 position have been identified as important targets. Because of its potential relevance to syn-anti cyclopentyl side chain orientation in 1, the 3-methyl derivative (2) was sought.
A hightroughput screenening assay has been developed to evaluate inhibition of FMDV 3Cpro by the potential synthetic inhibitors. The SAR studies demonstrate the success of the inhibitor design and have provided a lead for potential-drug development. MEDI 91 Synthesis of imidazolyl substituted heterosteroidal derivatives as potent aromatase inhibitors Ranju Bansal1, Sheetal Guleria1, Rolf W Hartmann2, and Anja Palusczak2. in, (2) Pharmazeutische und Medizinische Chemie, Universitat des Saarlands Inhibition of aromatase, a cytochrome P450 enzyme, has become of much interest in the treatment of disseminated estrogen dependent breast cancer over the last three decades.