New drug application of chain amides ccr5 receptor inhibitors

Abstract

The invention discloses a new use of a drug of a chain amide CCR5 (chemokine receptor) receptor antagonist. The new use provided by the method is the chain amide CCR5 inhibitor or an application of pharmaceutically acceptable salt in the preparation of a spermicidal drug. The structure formula of the chain amide CCR5 inhibitor is shown in formula I. An inactivating sperm in vitro test proves that the series of compounds have strong sperm killing activity; the EC50 value of the compound with the strongest activity achieves 1.5mg / ml; and the chain amide CCR5 inhibitor can develop into a preparation for in vitro contraception, or a multifunctional external preparation for resisting aids and contraception.

Description

technical field [0001] The invention relates to a new drug application of chain amide CCR5 receptor inhibitors. Background technique [0002] At present, oral contraceptives and intrauterine devices have been widely used in women of childbearing age, and achieved good results. However, for women of childbearing age who are unwilling to take oral contraceptives and use intrauterine devices, in addition to condoms used by men, spermicides can be used for contraception. At present, clinically used spermicides are mainly nonoxynol-9, octoxynol and benzalkonium chloride, etc. These drugs have better contraceptive effects, but a considerable number of people have local allergic reactions to them. Cause bacterial vaginosis, genital tract ulcer, toxic shock syndrome, uterine and vaginal epithelial shedding, etc. [0003] In addition, the widespread spread of AIDS in the world and in my country has become a serious public health problem. According to the joint report of the United...

AI Technical Summary

Problems solved by technology

At present, clinically used spermicides are mainly nonoxynol-9, octoxynol and benzalkonium chloride, etc. These drugs have better contraceptive effects, but a considerable number of people have local allergic reactions to them. Cause bacterial vaginosis, genital tract ulcer, toxic shock syndrome, uterine and vaginal epithelial shedding, etc.

Images