Ghosh, Arun K.; Thompson, Wayne J.; Lee, Hee Yoon; McKee, Sean P.; Munson, Peter M.; Duong, Tien T.; Darke, Paul L.; Zugay, Joan A.; Emini, Emilio A. published the artcile< Cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors>, Application of C6H10O5, the main research area is RO 318959 analog HIV protease inhibitor; cyclic sulfonlane asym synthesis HIV inhibitor; virucide sulfolanyloxycarbonylaminohydroxypropyl isoquinolinamide preparation.
Recently the use of urethanes of 3-tetrahydrofuran as P2-ligands for the S2-substrate binding site of HIV-1 protease was reported. The urethane of (S)-3-hydroxy sulfolane substantially increased the in vitro potency of inhibitors relative to the heterocycle 3-tetrahydrofuran. Furthermore, introduction of a small 2-alkyl group cis to the 3-hydroxyl group of either heterocycle system further enhances enzyme affinity. This is consistent with modeling studies using the x-ray crystal structure of the enzyme-inhibitor complex of THF derived inhibitor I and HIV-1 protease. The cis-2-iso-Pr group thus far offers optimum enhancement of the inhibitory properties of the 3-hydroxysulfolane providing an inhibitor II; for HIV-1, IC50 3 nM; for HIV-219, IC50 17 nM) of comparable in vitro antiviral potency to present clin. candidate (3S,4aS,8aS,2’R,3’S)-N-tert-butyl-2-(2′-hydroxy-4′-phenyl-3′-[[[N-(2-quinolinylcarbonyl)-L-asparaginyl]amino]butyl]-decahydroisoquinoline-3-carboxamide (Ro 31-8959), but of reduced mol. weight due to the exclusion of the P3-quinoline ligand. A stereoselective and general synthetic route to this novel class of ligands in optically pure form was developed.
Journal of Medicinal Chemistry published new progress about Antiviral agents. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Application of C6H10O5.
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