62885-88-5Relevant academic research and scientific papers
Potent Antifungal Synergy of Phthalazinone and Isoquinolones with Azoles Against Candida albicans
Mood, Aaron D.,Premachandra, Ilandari Dewage Udara Anulal,Hiew, Stanley,Wang, Fuqiang,Scott, Kevin A.,Oldenhuis, Nathan J.,Liu, Haoping,Van Vranken, David L.
, p. 168 - 173 (2017/03/06)
Four phthalazinones (CIDs 22334057, 22333974, 22334032, 22334012) and one isoquinolone (CID 5224943) were previously shown to be potent enhancers of antifungal activity of fluconazole against Candida albicans. Several even more potent analogues of these compounds were identified, some with EC50 as low as 1 nM, against C. albicans. The compounds exhibited pharmacological synergy (FIC 0.5) with fluconazole. The compounds were also shown to enhance the antifungal activity of isavuconazole, a recently FDA approved azole antifungal. Isoquinolone 15 and phthalazinone 24 were shown to be active against several resistant clinical isolates of C. albicans.
Praziquantel synthetic technology
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Paragraph 0011, (2016/11/28)
The invention discloses a praziquantel synthetic technology; beta-phenylethylamine, amino acetyl halide hydrochloride, halogenated acetaldehyde alcohol and cyclohexyl formyl chloride are used as raw materials and subjected to condensation, cyclization and acylation to synthesize praziquantel. The method has the advantages of cheap and easily available raw materials, low toxicity, safe production and simple process; amino acetyl halide hydrochloride and beta-phenylethylamine are condensed, the activity is moderate and the yield is relatively high; with reaction of halogenated aldehyde alcohol and an intermediate A, because halogen of halogenated aldehyde alcohol is easy to remove, the reaction is easy to implement, and the yield is favorable to improve; secondly, the synthetic technology has the advantages of mild synthetic reaction conditions, atmospheric pressure operation, safe operation and concise synthetic steps, and the total yield can be more than 50%; and the synthetic process has less waste emissions, pollution is low, the technology is a clean and highly efficient synthetic technology, and the production cost can be reduced by about 30%.
