Name: 5-Bromothiazol-2-amineIn 2020 ,《Novel small molecule retrograde transport blocker confers post-exposure protection against ricin intoxication》 appeared in Acta Pharmaceutica Sinica B. The author of the article were Zhao, Xu; Li, Haixia; Li, Jia; Liu, Kunlu; Wang, Bo; Wang, Yuxia; Li, Xingzhou; Zhong, Wu. The article conveys some information:
Ricin is a highly toxic type 2 ribosome-inactivating protein (RIP) which is extracted from the seeds of castor beans. Ricin is considered a potential bioterror agent and no effective antidote for ricin exists so far. In this study, by structural modification of a retrograde transport blocker Retro-2cycl, a series of novel compounds were obtained. The primary screen revealed that compound I has an improved antiricin activity compare to pos. control. In vitro pre-exposure evaluation in Madine-Darby Canine Kidney (MDCK) cells demonstrated that compound I is a powerful anti-ricin compound with an EC50 of 41.05 nmol/L against one LC (lethal concentration, 5.56 ng/mL) of ricin. Further studies surprisingly indicated that compound I confers post-exposure activity against ricin intoxication. An in vivo study showed that 1 h post-exposure administration of compound I can improve the survival rate as well as delay the death of ricin-intoxicated mice. A drug combination of compound I with monoclonal antibody mAb4C13 rescued mice from one LD (LD) ricin challenge and the survival rate of tested animals is 100%. These results represent, for the first time, indication that small mol. retrograde transport blocker confers both in vitro and in vivo post-exposure protection against ricin and therefore provides a promising candidate for the development of anti-ricin medicines. In the part of experimental materials, we found many familiar compounds, such as 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Name: 5-Bromothiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica