Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability was written by Liu, Yu;Liu, Zining;Cao, Xufeng;Liu, Xin;He, Huili;Yang, Yushe. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Category: piperazines This article mentions the following:
To improve antifungal activities, water solubility and bioavailability, a series of novel analogs of itraconazole-containing pyridine rings were designed and synthesized. Their antifungal activities were evaluated in vitro against six clin. important fungi by measuring the minimal inhibitory concentrations (MICs). Most of the compounds showed more potent antifungal activities than that of itraconazole. In particular, I [X = CH, X1 = N, R = CH2CHMe2, CHMe2; X = N, X1 = CH, R = CHMe2, CH2CMe2CH2OH, II] exhibited much higher solubility and bioavailability than that of itraconazole. The bioavailability of II (42.2%) was five times higher than that of itraconazole (8%) and was neg. for genetic toxicol. in the Ames test. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3Category: piperazines).
tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics