On April 1, 2021, Ibanez-Escribano, Alexandra; Reviriego, Felipe; Vela, Nerea; Fonseca-Berzal, Cristina; Nogal-Ruiz, Juan Jose; Aran, Vicente J.; Escario, Jose Antonio; Gomez-Barrio, Alicia published an article.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Promising hit compounds against resistant trichomoniasis: Synthesis and antiparasitic activity of 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles. And the article contained the following:
A series of 11 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles has been prepared starting from 1-benzyl-5-nitroindazol-3-ol, and evaluated against sensitive and resistant isolates of the sexually transmitted protozoan Trichomonas vaginalis. A variety of nitroindazoles demonstrate trichomonacidal profiles with IC50 < 20μM against the metronidazole-sensitive isolate. Moreover, all these compounds submitted to cytotoxicity assays against mammalian cells exhibited low non-specific cytotoxic effects, except two compounds I and II which displayed moderate cytotoxicity (CC50 = 74.7 and 59.1μM, resp.). Those compounds with trichomonacidal effect were also evaluated against a metronidazole-resistant culture. Special mention deserve compounds III and IV, which displayed better IC50 values (1.3 and 0.5μM resp.) than that of the reference drug (IC50 MTZ = 3.0μM). The high activity of these compounds against the resistant isolate reinforces the absence of cross-resistance with the reference drug. The remarkable trichomonacidal results against resistant T. vaginalis isolates suggest the interest of 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles to be considered as good prototypes to continue in the development of new drugs with enhanced trichomonacidal activity, aiming to increase the non-existent drugs to face clin. resistance efficiently for those patients in whom therapy with 5-nitroimidazoles is contraindicated. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione
The Article related to aminoalkoxy benzyl nitroindazole preparation antiparasitic resistant trichomoniasis, antiprotozoal agents, indazole, nitrogen heterocycles, resistance, trichomonas vaginalis and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione
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