| 摘要 |
<p>The invention concerns the compounds of formula (I) wherein A and B independently are a bond or optionally substituted aminoacyl; R1 is hydrogen; an amino protecting group; or a group of formula R6Y- wherein R6 is hydrogen or an optionally substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y is -CO-; -NHCO-; NHCS-; -SO2-; -O-CO-; or -O-CS-; R2 is the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 is an optionally substituted alkyl, alkenyl, alkinyl, cyloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl group; R4 is a group of formula -OR7 or -NHR7 wherein R7 has the significance indicated above for R6; and X is -S- or -NR5- wherein R5 is hydrogen, methyl, formyl or acetyl; in free form and, where such forms exist, in salt form. They can be obtained by a process comprising epoxide ring opening, appropriate substitution and/or deprotection or saponification. They have antiviral activity, particularly HIV-1 proteinase inhibiting activity, and are thus indicated for use in the treatment of retroviral diseases.</p> |
