- Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones
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Fluorinated aryl- and heteroaryl-substituted monohydrazones displayed excellent broad-spectrum activity against various fungal strains, including a panel of clinically relevant Candida auris strains relative to a control antifungal agent, voriconazole (VRC). These monohydrazones displayed less hemolysis of murine red blood cells than that of VRC at the same concentrations, possessed fungicidal activity in a time-kill study, and exhibited no mammalian cell cytotoxicity. In addition, these monohydrazones prevented the formation of biofilms that otherwise block antibiotic effectiveness and did not trigger the development of resistance when exposed to C. auris AR Bank # 0390 over 15 passages.
- Thamban Chandrika, Nishad,Dennis, Emily K.,Brubaker, Katelyn R.,Kwiatkowski, Stefan,Watt, David S.,Garneau-Tsodikova, Sylvie
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supporting information
p. 124 - 133
(2020/10/20)
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- The use of enaminones and enamines as effective synthons for MSA-catalyzed regioselective synthesis of 1,3,4-tri- And 1,3,4,5-tetrasubstituted pyrazoles
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In the present work, an efficient regioselective synthesis of 1,3,4-tri- and 1,3,4,5-tetrasubstituted pyrazoles via a methanesulfonic acid (MSA)-catalyzed reaction of hydrazones with enaminones or enamines is reported. Mechanistically, the formation of the title compounds involves the [2+3] cycloaddition of hydrazones with enaminones or enamines followed by aromatization with acid and oxygen. This convenient method under mild conditions with various hydrazones, enaminones, and enamines was well-tolerated to afford products in good to excellent yields. Compared with the literature methods, this strategy has advantages such as materials that are available economically, metal-free catalysis, excellent regioselectivity, and high efficiency.
- Duan, Liancheng,Zhou, Hui,Gu, Yucheng,Gong, Ping,Qin, Mingze
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supporting information
p. 16131 - 16137
(2019/11/03)
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- Synthesis, crystal structure, optical and electrochemical properties of novel diphenylether-based formazan derivatives
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In this study, formazans 5a-5h were synthesized by coupling the reactions of substituted phenylhydrazone compounds 3a-3h with diazonium salt of 4-chloro-2-phenoxybenzenamine (4). The substituted phenylhydrazones 3a-3h were obtained from the condensation o
- Turkoglu, Gulsen,Berber, Halil,Kani, Ibrahim
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supporting information
p. 2728 - 2740
(2015/04/14)
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- A new route to substituted pyrimido[5,4-e]-l,2,4-triazine-5,7(1H,6H)-diones and facile extension to 5,7(6H,8H) isomers
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A new route to substituted pyrimido[5,4-e]-l,2,4-triazine-5,7(lH,6H)-diones is outlined. The synthesis proceeds via preformed hydrazone intermediates, which are then condensed with an activated chlorouracil to build up the entire molecular framework, foll
- Turbiak, Anjanette J.,Showalter, H. D. Hollis
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experimental part
p. 4022 - 4026
(2010/03/30)
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- Parallel synthesis of pyrazolines on soluble polymer support
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An efficient and rapid parallel liquid-phase synthesis of pyrazolines has been developed. The one-pot three-components reaction of polyethylene glycol (PEG)-supported acrylate 1, aldehyde 2 and aryl hydrazine 3 in the presence of chloramine-T in methanol gave the corresponding PEG-supported pyrazolines 5. Cleavage from the support under mild conditions afforded pyrazolines 6 in good yields (69-91%) and high purities (91-100%).
- Wang, Yan-Guang,Zhang, Jian,Lin, Xu-Feng,Ding, Han-Feng
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p. 1467 - 1468
(2007/10/03)
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