| 摘要 |
<p>Substantially pure diastereoisomeric compounds of formula Ia, alternatively Ib, or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, including hydrates, wherein PG is a protective group; R 1 is a radical selected from the group consisting of phenylmethyl, 4-hydroxyphenylmethyl, (1 H -indol-3-yl)methyl and (1 H -imidazol-4-yl)methyl; R 2 is a radical selected from the group consisting of -H, -CH 3 , -CH 2 SH, -CH 2 OH -CH 2 Ph, -CH 2 CO 2 H, -CH 2 CONH 2 , -CH(OH)CH 3 , -CH(CH 3 )CH 2 CH 3 , -CH(CH 3 ) 2 , -CH 2 CH(CH 3 ) 2 , -(CH 2 ) 2 SCH 3 , -(CH 2 ) 2 CO 2 H, -(CH 2 )CONH 2 , -(CH 2 ) 3 NHC(NH)NH 2 , -(CH 2 ) 4 NH 2 , imidazol-4-ylmethyl, 4-hydroxyphenylmethyl, (1 H -indol-3-yl)methyl, (1 H -imidazol-4-yl)methyl and -(CH 2 ) n -Ar; and R 3 is a radical selected from the group consisting of -O(C 1 -C 4 )alkyl, -O(C 2 -C 4 )alkenyl, -O(C 2 -C 4 )alkynyl, -O(C 1 -C 4 )alkyl-Ar, -OAr, - NR a Ar, -N(R a )[(C 1 -C 4 )alkyl-Ar], and -NR a OAr and -N(R a )[O(C 1 -C 4 )alkyl-Ar]. These compounds are inhibitors of cysteine-proteases cruzain, rhodesain and falcipain, and therefore, useful in the treatment and/or prevention of pathologies such as Chagas disease, African trypanosomiasis or malaria.</p> |
