ROBENIDINE ANALOGS AS POTENT ANTIMALARIALS AGAINST DRUG-RESISTANT PLASMODIUM FALCIPARUM
申请人:OREGON HEALTH & SCIENCE UNIVERSITY
公开号:US20220267258A1
公开(公告)日:2022-08-25
Provided herein is a compound of Formula (I):
wherein:
R
1
is selected from the group of —F, —Cl, —Br, —I, C
1
-C
6
haloalkyl, C
1
-C
6
haloalkoxy, —NO
2
, —C(H)═O, ═O, —CN, and COOR
3
;
R
2
is selected from the group of H and C
1
-C
3
alkyl; and
R
3
is selected from the group of H, C
1
-C
6
alkyl, and benzyl;
or a pharmaceutically acceptable salt, co-crystal, ester, solvate, hydrate, isomer (including optical isomers, racemates, or other mixtures thereof), tautomer, isotope, polymorph, or pharmaceutically acceptable prodrug thereof, along with pharmaceutical compositions and methods of using the compound in the treatment of malaria, particularly including drug-resistant malaria.
提供的是化合物I的公式:其中:R1选自—F,—Cl,—Br,—I,C1-C6卤代烷基,C1-C6卤代氧烷基,—NO2,—C(H)═O,═O,—CN和COOR3的组;R2选自H和C1-C3烷基;R3选自H,C1-C6烷基和苄基;或其药学上可接受的盐,共晶体,酯,溶剂合物,水合物,异构体(包括光学异构体,外消旋体或其他混合物),互变异构体,同位素,多晶形或其药学上可接受的前药,以及使用该化合物治疗疟疾的药物组合物和方法,特别是包括耐药性疟疾。