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Grace A. Bennett Patricia A. Swift George B. Mullen Stanley D. Allen Jeffrey T. Mitchell Wendy E. Jones Vassil St. Georgiev 《Journal of heterocyclic chemistry》1989,26(6):1729-1734
The synthesis and antifungal activity of a novel series of 3-aryl-5-[(aryloxy)methyl]-3-[(1H-1,2,4-triazol-1-yl)-methyl]-2-methylisoxazolidines are described. The in vitro activity was evaluated in solid agar cultures against a variety of dermatophytes and yeast fungi, while in vivo activity was measured in an immune-compromised mouse model of systemic candidiasis. The activity of the title series was compared to that of ketoconazole and one derivative, the cis-3-(4-chlorophenyl)-5-(4-chlorophenyloxy)methyl analogue 5f was found to possess a similar potency in the in vivo assay. Structure-activity relationship correlations are also discussed. 相似文献
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N-Methyl-N-[(1S)-1-[(3R)-pyrrolidin-3-yl]ethyl]amine (1)(1) is a key intermediate in the preparation of premafloxacin (2), which was under development as an antibiotic for use against pathogens of veterinary importance. This paper describes the development of a practical, efficient, and stereoselective process for the preparation of 1 from isobutyl (3S)-3-[methyl[(1S)-1-phenylethyl]amino]butanoate (5c). The key steps in the synthetic sequence are an asymmetric Michael addition, which yields 5c, and a stereoselective alkylation, which yields (3S,4S)-3-allyl-1,4-dimethylazetidin-2-one (17). 相似文献
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V. A. Shadrikova E. V. Golovin E. A. Kuznetsova M. Yu. Rostova Yu. N. Klimochkin 《Russian Journal of Organic Chemistry》2016,52(10):1452-1462
Quaternary 1-[2-(adamantan-1-yl)ethyl]pyridinium bromides were reduced with sodium tetrahydridoborate in ethanol, and hydroarylation of the resulting 1-[2-(adamantan-1-yl)ethyl]-1,2,3,6-tetrahydropyridines with benzene in trifluoromethanesulfonic acid afforded phenylpiperidines with preferentially equatorial orientation of the phenyl substituent. 相似文献
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Voloboev S. N. Andreev A. V. Mkrtchyan A. S. Navrotskii M. B. Novakov I. A. Orlinson B. S. Son V. V. 《Russian Chemical Bulletin》2016,65(5):1336-1340
Russian Chemical Bulletin - A number of new N-[(adamantan-1-yl)methyl]aniline derivatives, which can be considered as conformationally labile analogues of synthetic adaptogen Bromantan, were... 相似文献
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Ketalization of benzophenones with epichlorohydrin or 3-chloropropane-1,2-diol gave 2,2-diaryl-4-chloromethyl-1,3-dioxolanes,
which were used to alkylate sodium salts of imid-azole or 1,2,4-triazole. The resulting 1-[(2,2-diaryl-1,3-dioxolan-4-yl)methyl]-1H-azoles exhibit high fungicidal activities.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 940–944, May, 2007. 相似文献
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I. A. Novakov A. S. Babushkin A. A. Vernigora I. A. Kirillov M. B. Navrotskii B. S. Orlinson S. N. Voloboev 《Russian Journal of General Chemistry》2016,86(12):2599-2605
Using the Leuckart–Wallach reaction, novel conformationally flexible structural analogs of Bromantane drug have been synthesized from 3-haloadamantane-1-carbaldehydes. Basic hydrolysis of the prepared compounds has been studied as a model of one of the pathways of their transformations in vivo. 相似文献
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I. M. Sakhautdinov I. R. Batyrshin A. A. Fatykhov V. M. Yumabaeva K. Yu. Suponitskii M. Yu. Antipin M. S. Yunusov 《Journal of Structural Chemistry》2013,54(2):383-387
The structure of methyl 4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-1-methyl-1H-pyrazol-5-carboxylate is determined by X-ray crystallography and further used to elucidate the structure of methyl 4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-1-methyl-1H-pyrazol-3-carboxylate, using the data of homo- and heteronuclear 2D NMR correlation spectroscopy. 相似文献
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L. Ignatovich V. Romanov J. Spura J. Popelis I. Domracheva I. Shestakova 《Chemistry of Heterocyclic Compounds》2012,47(12):1502-1508
Novel 3-[(methyl)bis(5-trialkylsilylfuran-2-yl)silyl]propylamines have been synthesized by a hydrosilylation reaction of aliphatic
and heterocyclic N-allylamines in the presence of the Speier's catalyst. The effects of the structure of the amine and the alkyl substituent
at the silicon atom on the cytotoxicity of the compounds have been studied. 相似文献
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Song Y Zhang L Huizhong Shi D Xie J Zhao G 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2008,70(4):943-952
The solid phase FT-IR and FT-Raman spectra of 1-[6-(4-chlorophenyl)-1-[(6-chloropyridin-3-yl)methyl]-2-[(6-chloropyridin-3-yl)methylsulfanyl]-4-methyl-1,6-dihydropyrimidin-5-yl]ethanone (C25H21Cl3N4OS) were recorded in the region 4000-400 and 3500-100cm(-1), respectively. The vibrational spectra have been computed using density functional theory (B3LYP) and ab initio molecular orbital calculation (HF) with 6-31G(d, p) basis sets. A close agreement was achieved between the observed and calculated frequency by employing normal coordinate calculations. The observed and simulated spectra were found to be well comparable. 相似文献
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D’yachenko V. S. Burmistrov V. V. Butov G. M. 《Russian Journal of Organic Chemistry》2019,55(11):1679-1685
Russian Journal of Organic Chemistry - Ethyl [(adamantan-1-yl)alkylene(phenylene)amino]oxoacetates and N1,N2-bis[(adamantan-1-yl)-alkylene(phenylene)oxamides were prepared in yields of 72–87... 相似文献
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Masterova N. S. Ryabova S. Yu. Alekseeva L. M. Shashkov A. S. Chernyshev V. V. Granik V. G. 《Russian Chemical Bulletin》2009,58(9):1973-1980
Russian Chemical Bulletin - Reactions of 3-acetoxy-2-(2,2-dicyanovinyl)indole with hydrazine hydrate and methyl-and phenylhydrazines afforded new indolin-3-one derivatives, namely,... 相似文献
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Krinochkin A. P. Guda M. R. Kopchuk D. S. Shtaitz Ya. K. Starnovskaya E. S. Savchuk M. I. Rybakova S. S. Zyryanov G. V. Chupakhin O. N. 《Russian Journal of Organic Chemistry》2021,57(4):675-677
Russian Journal of Organic Chemistry - Methyl 3-(3,6-diaryl-1,2,4-triazin-5-ylamino)thiophen-2-carboxylates were synthesized in 70–75% yield by solvent-free reaction of methyl... 相似文献
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George B. Mullen Patricia A. Swift David M. Marinyak Stanley D. Allen Jeffrey T. Mitchell C. Richard Kinsolving Vassil St. Georgiev 《Helvetica chimica acta》1988,71(4):718-732
The synthesis and antifungal activity of a novel series of 3-aryl-5-[(aryloxy)alkyl]-3-[(1H-imidazol-1-yl)-methyl]-2-methylisoxazolidines and related compounds, are discussed. The synthesis of the title compounds was accomplished via a 1,3-dipolar cycloaddition of α-substituted ketonitrones with l-alkenyl phenyl ethers (Scheme 2 and 3). The compounds were evaluated for in vitro antifungal activity in solid agar cultures against a broad variety of yeast and systemic mycoses and dermatophytes. While antifungal activity was evident throughout the series, in general, derivatives having halogen atom(s) in either or both aryl rings demonstrated the highest potency, especially against Trichophyton rubrum and Candida albicans. The dichloro analog 20 (PR 967-248) was found to possess the most useful activity. Its minimum inhibitory concentration (MIC) values ranged between 0.2 and 2.0 μg/ml, as compared to 0.2–20.0 μg/ml for the standard drug ketoconazole (4). 相似文献
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A reaction of methyl 2-(4-allyl-2-methoxyphenoxy)acetate with adamantan-2-amine and (adamantan-1-yl)methylamine in butanol leads, together with the target amides, to the formation of butyl ester of the corresponding acid, which is resistant to aminolysis. 相似文献
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