Use of avermectin derivative for increasing bioavailability and efficacy of macrocyclic lactones
申请人:INSTITUT NATIONAL DE RECHERCHE POUR L'AGRICULTURE, L'ALIMENTATION ET L'ENVIRONNEMENT
公开号:US11021508B2
公开(公告)日:2021-06-01
The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyl, (ii) X represents —CH2—CH2—, or —CH═CH—, (iii) R2 is chosen from
or an OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.
本发明涉及阿维菌素衍生物作为治疗寄生虫感染药物的用途。阿维菌素衍生物由式(I)表示,其中(i) R1 选自-CH(CH3)2、-CH(CH3)CH2CH3 或环己基构成的基团,(ii) X 代表-CH2-CH2-或-CH═CH-,(iii) R2 选自
或 OH 基团,(iv) R3 是 OH 或 NOH,(v) 当 R3 是 OH 时代表单键,当 R3 是 NOH 时代表双键。