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吡唑化合物Win 41258-3在小鼠生殖器感染和豚鼠皮肤感染中对单纯疱疹病毒的抗病毒活性。

Antiviral activity of Win 41258-3, a pyrazole compound, against herpes simplex virus in mouse genital infection and in guinea pig skin infection.

作者信息

Pancic F, Steinberg B A, Diana G D, Carabateas P M, Gorman W G, Came P E

出版信息

Antimicrob Agents Chemother. 1981 Mar;19(3):470-6. doi: 10.1128/AAC.19.3.470.

Abstract

Win 41258-3 (4-[6-(2-chloro-4-methoxyphenoxy)hexyl]-3,5-diethyl-1H-pyrazole methane sulfonate) has in vitro and in vivo activity against herpes simplex virus types 1 and 2. In cell culture, a concentration of 2 microgram/ml produced a greater than 50% inhibition of plaque formation of herpes simplex virus type 2, and 3 microgram/ml produced a 100% reduction of herpes simplex virus type 1. Win 41258-3 was effective against herpes simplex virus types 1 and 2 in mouse genital infection after intravaginal administration. Win 41258-3 was administered to mice at 4 h postinfection with solutions containing 1.25, 2.5, 5, or 10% of the compound in saturated tampons. Therapy resulted in a high survival rate (80 to 100%) of treated animals versus 20 to 30% of placebo-treated controls. Win 41258-3 was also effective in guinea pig skin infection produced by herpes simplex virus type 1. Solutions of 2.5, 5, and 10% Win 41258-3, applied to the skin starting 24 h postinfection, resulted in rapid suppression of development of herpetic vesicles and significant reduction of the virus titers in the lesion sites.

摘要

Win 41258-3(4-[6-(2-氯-4-甲氧基苯氧基)己基]-3,5-二乙基-1H-吡唑甲磺酸盐)对1型和2型单纯疱疹病毒具有体外和体内活性。在细胞培养中,2微克/毫升的浓度对2型单纯疱疹病毒的空斑形成产生了大于50%的抑制作用,3微克/毫升的浓度使1型单纯疱疹病毒减少了100%。Win 41258-3经阴道给药后,对小鼠生殖器感染的1型和2型单纯疱疹病毒有效。在感染后4小时,将含有1.25%、2.5%、5%或10%该化合物的溶液用饱和棉球给予小鼠。治疗使治疗组动物的存活率很高(80%至100%),而安慰剂治疗的对照组存活率为20%至30%。Win 41258-3对1型单纯疱疹病毒引起的豚鼠皮肤感染也有效。在感染后24小时开始,将2.5%、5%和10%的Win 41258-3溶液应用于皮肤,导致疱疹性水疱的发展迅速受到抑制,病变部位的病毒滴度显著降低。

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