- An efficient catalytic asymmetric route to 1-aryl-2-imidazol-1-yl-ethanols
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The asymmetric hydrogenation of 1-aryl-2-imidazol-1-yl-ethanones offers a concise route to homochiral 1-aryl-2-imidazol-1-yl-ethanols. Catalytic asymmetric transfer hydrogenation with formic acid using [(R,R)-TsDPEN] Ru(Cymene)Cl as precatalyst was shown to be effective in this transformation. Preliminary process development showed that the hydrogenation could be carried out under mild conditions at a molar substrate-to-catalyst (S/C) ratio of 1000-2000.
- Lennon, Ian C.,Ramsden, James A.
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Read Online
- Reactivity of functionally substituted azoles towards electrophiles. Novel synthesis of thienylazoles and phenylazoles
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Phenacyl bromide reacted with imidazole 1a and 1,2,4-triazole 1b to yield the respective azolylacetophenones 1c,d. These reacted with phenyl isothiocyanate and phenacyl bromide yielding thienylazoles 4a,b. Reaction of 1c,d with dimethylformamide dimethyla
- Abdel-Megid, Mohamed
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Read Online
- Asymmetric transfer hydrogenation of heterocycle-containing acetophenone derivatives using N-functionalised [(benzene)Ru(II)(TsDPEN)] complexes
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The application of enantiomerically-pure ruthenium(II) catalysts containing N - functionalised TsDPEN ligand to the asymmetric transfer hydrogenation of 15 examples of α-heterocyclic acetophenone derivatives is reported. Products of up to 99% ee were formed.
- Barrios-Rivera, Jonathan,Xu, Yingjian,Clarkson, Guy J.,Wills, Martin
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supporting information
(2021/12/02)
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- Synthesis of aliphatic α-ketoamides from α-substituted methyl ketones: Via a Cu-catalyzed aerobic oxidative amidation
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α-Ketoamides are an important key functional group and have been used as versatile and valuable intermediates and synthons in a variety of functional group transformations. Synthetic methods for making aryl α-ketoamides as drug candidates have been greatly improved through metal-catalyzed aerobic oxidative amidations. However, the preparation of alkyl α-ketoamides through metal-catalyzed aerobic oxidative amidations has not been reported because generating α-ketoamides from aliphatic ketones with two α-carbons theoretically provides two distinct α-ketoamides. Our strategy is to activate the α-carbon by introducing an N-substituent at one of the two α-positions. The key to this strategy is how heterocyclic compounds such as triazoles and imidazoles affect the selectivity of the synthesis of the alkyl α-ketoamides. From this basic concept, and by optimizing the reaction and elucidating the mechanism of the synthesis of aryl α-ketoamides via a copper-catalyzed aerobic oxidative amidation, we prepared fourteen aliphatic α-ketoamides in high yields (48-84%). This journal is
- Cha, Hyojin,Chai, Jin Young,Chi, Dae Yoon,Kim, Hyeong Baik
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supporting information
p. 4320 - 4326
(2021/05/31)
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- One pot synthesis of α-N-heteroaryl ketone derivatives from aryl ketones using aqueous NaICl2
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A simple and efficient method for the synthesis of α-heteroaryl ketones from aryl ketones and amine using aqueous sodium dichloroiodate is established. This method is mild, operationally simple, has a short reaction time, and easy workup procedure to afford the corresponding α-N-heteroaryl ketone derivatives in moderate to good yield.
- Ghodse, Shrikant M.,Hatvate, Navnath T.,Telvekar, Vikas N.
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supporting information
(2021/12/08)
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- Diaryl-containing imidazole compound and preparation method and medical application thereof
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The invention discloses a diaryl-containing imidazole compound. The invention further discloses application of the diaryl-containing imidazole compound to preparation of drugs for preventing or treating Alzheimer's disease. The inventor screens butyrylcholine esterase and IDO1 as carriers for inhibiting the activity to evaluate the effect of the diaryl imidazole compound to treat Alzheimer's disease, and finds that the diaryl imidazole compound has good in vitro activity, and can be further developed as a precursor substance for performing the Alzheimer's disease resistant effect by inhibitingthe activity of cholinesterase. (The formula is shown in the description).
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Paragraph 0192; 0195; 0196
(2019/02/21)
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- α-N-Heteroarylation and α-Azidation of Ketones via Enolonium Species
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Enolonium species, resulting from the umpolung of ketone enolates by Koser's hypervalent iodine reagents activated by boron trifluoride, react with a variety of nitrogen heterocycles to form α-aminated ketones. The reactions are mild and complete in 4-5 h. Additionally, α-azidation of the enolonium species takes place using trimethylsilyl azide as a convenient source of azide nucleophile.
- More, Atul A.,Pathe, Gulab K.,Parida, Keshaba N.,Maksymenko, Shimon,Lipisa, Yuriy B.,Szpilman, Alex M.
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p. 2442 - 2447
(2018/02/23)
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- New azole derivatives showing antimicrobial effects and their mechanism of antifungal activity by molecular modeling studies
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Azole antifungals are potent inhibitors of fungal lanosterol 14α demethylase (CYP51) and have been used for eradication of systemic candidiasis clinically. Herein we report the design, synthesis, and biological evaluation of a series of 1-phenyl/1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethanol esters. Many of these derivatives showed fungal growth inhibition at very low concentrations. Minimal inhibition concentration (MIC) value of 15 was 0.125?μg/mL against Candida albicans. Additionally, some of our compounds, such as 19 (MIC: 0.25?μg/mL), were potent against resistant C.?glabrata, a fungal strain less susceptible to some first-line antifungal drugs. We confirmed their antifungal efficacy by antibiofilm test and their safety against human monocytes by cytotoxicity assay. To rationalize their mechanism of action, we performed computational analysis utilizing molecular docking and dynamics simulations on the C.?albicans and C.?glabrata CYP51 (CACYP51 and CGCYP51) homology models we built. Leu130 and T131 emerged as possible key residues for inhibition of CGCYP51 by 19.
- Do?an, ?nci Selin,Sara?, Selma,Sari, Suat,Kart, Didem,E?siz G?khan, ?ebnem,Vural, ?mran,Dalkara, Sevim
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p. 124 - 138
(2017/03/02)
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- A METAL FREE PROCESS FOR THE PREPARATION OF ALPHA-SUBSTITUTED CARBONYL COMPOUNDS FROM ALKENES
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The present invention discloses a novel metal free process for the regioselective synthesis of α-substituted carbonyl compounds of formula I from alkene, X is selected from the following compounds (A, B).
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Page/Page column 20-21
(2017/06/19)
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- Substituted imidazole-1-vinyl compound and use thereof
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The invention relates to a substituted imidazole-1-ethylene compound as well as a preparation and an application thereof. The substituted imidazole-1-ethylene compound is a compound shown as a formula I, or salts thereof formed with medicinal acids or bases. According to the antifungal activity test performed on eight clinical fungi by the compound provided in the invention, a good fungus killing effect is achieved. The compound can serve as a novel broad-spectrum antifungal activity compound and is developed into antifungal medicines, disinfectants or feed additives.
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Paragraph 0053-0056
(2016/10/27)
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- Discovery of in vitro antitubercular agents through in silico ligand-based approaches
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The development of new anti-tubercular agents represents a constant challenge mostly due to the insurgency of resistance to the currently available drugs. In this study, a set of 60 molecules were selected by screening the Asinex and the ZINC collections and an in house library by means of in silico ligand-based approaches. Biological assays in Mycobacterium tuberculosis H37Ra ATCC 25177 strain highlighted (±)-1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethyl-4-(3,4-dichlorophenyl)piperazine-1-carboxylate (5i) and 3-(4-chlorophenyl)-5-(2,4-dimethylpyrimidin-5-yl)-2-methylpyrazolo[1.5-a]pyrimidin-7(4H)-one (42) as the most potent compounds, having a Minimum Inhibitory Concentration (MIC) of 4 and 2 μg/4g/mL respectively. These molecules represent a good starting point for further optimization of effective anti-TB agents.
- De Vita, Daniela,Pandolfi, Fabiana,Cirilli, Roberto,Scipione, Luigi,Di Santo, Roberto,Friggeri, Laura,Mori, Mattia,Fiorucci, Diego,Maccari, Giorgio,Christopher, Robert Selwyne Arul,Zamperini, Claudio,Pau, Valentina,De Logu, Alessandro,Tortorella, Silvano,Botta, Maurizio
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p. 169 - 180
(2016/06/09)
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- Regioselective oxo-amination of alkenes and enol ethers with N-bromosuccinimide-dimethyl sulfoxide combination: A facile synthesis of α-amino-ketones and esters
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An unprecedented conversion of alkenes and enol ethers to the corresponding α-imido carbonyl compounds with excellent regioselectivity and yields has been developed. This oxo-amination process employs readily available N-bromosuccinimide (NBS) and secondary amines as N-sources and dimethyl sulfoxide (DMSO) as the oxidant and also leads to the production of amino alcohols in a single step on reduction, thus broadening the scope of this operationally simple reaction. For the first time, the formation of reactive Me2S+-O-Br species generated by the interaction of NBS with DMSO has been proven.
- Prasad, Pragati K.,Reddi, Rambabu N.,Sudalai, Arumugam
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supporting information
p. 500 - 503
(2016/02/18)
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- ANTIFUNGAL COMPOUNDS OF (ARYLALKYL) AZOLE DERIVATIVES IN THE STRUCTURE OF OXIME ESTER
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This invention is related to the antifungal compounds having azole structure in Formula (1), and hydrates, solvates, pharmaceutically acceptable salts or geometric isomers thereof. Formula (1)
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Page/Page column 7
(2015/04/15)
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- Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
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Indoleamine 2,3-dioxygenase 1 (IDO1) is a key regulator of immune responses and therefore an important therapeutic target for the treatment of diseases that involve pathological immune escape, such as cancer. Here, we describe a robust and sensitive high-throughput screen (HTS) for IDO1 inhibitors using the Prestwick Chemical Library of 1200 FDA-approved drugs and the Maybridge HitFinder Collection of 14,000 small molecules. Of the 60 hits selected for follow-up studies, 14 displayed IC50 values below 20 μM under the secondary assay conditions, and 4 showed an activity in cellular tests. In view of the high attrition rate we used both experimental and computational techniques to identify and to characterize compounds inhibiting IDO1 through unspecific inhibition mechanisms such as chemical reactivity, redox cycling, or aggregation. One specific IDO1 inhibitor scaffold, the imidazole antifungal agents, was chosen for rational structure-based lead optimization, which led to more soluble and smaller compounds with micromolar activity.
- R?hrig, Ute F.,Majjigapu, Somi Reddy,Chambon, Marc,Bron, Sylvian,Pilotte, Luc,Colau, Didier,Van Den Eynde, Beno?t J.,Turcatti, Gerardo,Vogel, Pierre,Zoete, Vincent,Michielin, Olivier
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p. 284 - 301
(2014/08/05)
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- Synthesis of (Z)-N-alkenylazoles and pyrroloisoquinolines from α-N-azoleketones through Pd-catalyzed tosylhydrazone cross-couplings
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Azoles reacting in tandem: The ortho-stereodirecting effect is the key to the stereoselective synthesis of (Z)-N-alkenylazoles I through the tosylhydrazide-mediated Pd-catalyzed cross-coupling reaction of α-N-azoleacetophenones with ortho-substituted aryl halides and nonaflates (see scheme). Additionally, the preorganization of the alkene allowed for the development of an auto-tandem reaction involving an intramolecular C-H arylation leading to pyrroloisoquinolines II. Copyright
- Florentino, Lucia,Aznar, Fernando,Valdes, Carlos
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supporting information
p. 10506 - 10510
(2013/08/23)
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- Imidazole incorporated semicarbazone derivatives as a new class of anticonvulsants: Design, synthesis and in-vivo screening
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A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synthetic route and characterized by spectral analysis (IR, 1H NMR, 13C NMR and Mass). The anticonvulsant activity of the synthesized compounds was determined using doses of 30, 100, and 300 mg kg-1 against maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Six compounds exhibited protection in both models and 2-(1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethylidene)-N-p- tolylsemicarbazone emerged as the most active compound of the series without any neurotoxicity and significant CNS depressant effect. Liver enzyme estimations (SGOT, SGPT, Alkaline phosphatase) of the compound also showed no significant change in the enzymes levels. Moreover, it caused 80% elevation of γ-amino butyric acid (GABA) levels in the whole mice brain, thus indicating that it could be a promising candidate in designing of a potent anticonvulsant drug.
- Amir, Mohammad,Ali, Israr,Hassan, Mohd. Zaheen
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p. 571 - 580
(2013/07/28)
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- Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)- 1-phenylethanol derivatives
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A new series of aromatic ester and carbamate derivatives of 2-(1H-imidazol-1-yl)-1-phenylethanol were synthesized and evaluated for their antifungal activity towards Candida albicans and non-albicans Candida species strains. The aromatic biphenyl ester derivatives 6a-c were more active than the reference compound fluconazole. 6c possesses a MIC mean values of 1.7 ± 1.4 μg mL-1 vs C. albicans and 1.9 ± 2.0 μg mL -1 vs non-albicans Candida species strains. The racemic mixtures of 6a, b were purified to afford the pure enantiomers. The (-) isomers were up to 500 times more active than (+) isomers. (-)-6a and (-)-6b were thirty and ninety times more active than fluconazole towards C. krusei strain respectively. The racemates of 6a-c showed low cytotoxicity against human monocytic cell line (U937) with 6a demonstrating a CC50 greater than 128 μg mL -1.
- De Vita, Daniela,Scipione, Luigi,Tortorella, Silvano,Mellini, Paolo,Di Rienzo, Barbara,Simonetti, Giovanna,D'Auria, Felicia Diodata,Panella, Simona,Cirilli, Roberto,Di Santo, Roberto,Palamara, Anna Teresa
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body text
p. 334 - 342
(2012/04/10)
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- Structure-cytotoxicity relationship of a novel series of miconazole-like compounds
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In the current study, two novel classes of the carboacyclic nucleosides having miconazole-like scaffolds as imidazole- and pyrimidine-based compounds were examined for their cytotoxic properties. The aim was to establish a relation between cytotoxic activ
- Yousefi, Reza,Khalafi-Nezhad, Ali,Panahi, Farhad,Soltani Rad, Mohammad Navid,Behrouz, Somayeh,Esmaili, Mansoore,Ghaffari, Sayed Mahmoud,Moosavi-Movahedi, Ali Akbar,Niazi, Ali
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p. 1921 - 1928,8
(2020/07/30)
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- Synthesis of some novel hydrazono acyclic nucleoside analogues
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The syntheses of novel hydrazono acyclic nucleosides similar to miconazole scaffolds are described. In this series of acyclic nucleosides, pyrimidine as well as purine and other azole derivatives replaced the imidazole function in miconazole and the ether
- Rad, Mohammad N. Soltani,Behrouz, Somayeh,Khalafi-Nezhad, Ali
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experimental part
(2010/08/03)
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- 2-Aryl-3-(1H-azol-1-yl)-1H-indole derivatives: A new class of antimycobacterial compounds - Conventional heating in comparison with MW-assisted synthesis
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2-Aryl-3-(1H-imidazol-1-yl and 1H-1,2,4-triazol-1-yl)-1H-indole derivatives were synthesized and tested for their in-vitro antifungal and antimycobacterial activities. These indole derivatives were devoid of antifungal activity against the tested strains of Candida spp. Yet, they exhibited an interesting antitubercular activity against Mycobacterium tuberculosis reference strain H37Rv.
- Zampieri, Daniele,Mamolo, Maria Grazia,Laurini, Erik,Scialino, Giuditta,Banfi, Elena,Vio, Luciano
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scheme or table
p. 716 - 722
(2010/07/04)
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- Design and synthesis of some novel oxiconazole-like carboacyclic nucleoside analogues, as potential chemotherapeutic agents
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The syntheses of some novel carboacyclic nucleosides, 17a-17o, containing oxiconazole-like scaffolds, are described (Schemes 1-3). In this series of carboacyclic nucleosides, pyrimidine as well as purine and other imidazole derivatives were employed as an imidazole successor in oxiconazole. These compounds could be prepared in good yields by using two different strategies (Schemes 1 and 2). Due to Scheme 1, the N-coupling of nucleobases with 2-bromoacetophenones was attained for 18a-18e, and their subsequent oximation affording 19a-19e and finally O-alkylation with diverse alkylating sources resulted in the products 17a-17g, 17n, and 17o. In Scheme 2, use of 2-bromoacetophenone oximes 20, followed by N-coupling of nucleobases, provided 19f-19j whose final O-alkylation produced 17h-17m (Scheme 2). For the rational interpretation of the dominant formation of (E)-oxime ethers rather than (Z)-oxime isomers, PM3 semiempirical quantum-mechanic calculations were discussed and the calculations indicated a lower heat of formation for (E)-isomers.
- Rad, Mohammad Navid Soltani,Khalafi-Nezhad, Ali,Behrouz, Somayeh
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experimental part
p. 1760 - 1774
(2009/12/06)
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- Antifungal and antimycobacterial activity of 1-(3,5-diaryl-4,5-dihydro-1H-pyrazol-4-yl)-1H-imidazole derivatives
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1-(3,5-Diaryl-4,5-dihydro-1H-pyrazol-4-yl)-1H-imidazole derivatives were synthesized and tested for their in vitro antifungal and antimycobacterial activities. These imidazole derivatives showed an excellent antifungal activity against a clinical strain of Candida albicans and an interesting antitubercular activity againstMycobacterium tuberculosis H37Rv reference strain.
- Zampieri, Daniele,Mamolo, Maria Grazia,Laurini, Erik,Scialino, Giuditta,Banfi, Elena,Vio, Luciano
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p. 4516 - 4522
(2008/09/21)
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- Novel N,S-phenacyl protecting group and its application for peptide synthesis
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The phenacyl group can be introduced onto amino and thio groups by N,S-alkylation reactions. Conversely, these groups are removed rapidly by employing magnesium in acetic acid. This protecting group was successfully applied to a short peptide synthesis of Boc-L-Cys-Gly-OMe. Georg Thieme Verlag Stuttgart.
- Tang, Guo,Ji, Tao,Hu, An-Fu,Zhao, Yu-Fen
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experimental part
p. 1907 - 1909
(2009/04/11)
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- The "reverse-tethered" ruthenium (II) catalyst for asymmetric transfer hydrogenation: Further applications
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The attachment of a tethering group from the basic nitrogen atom to the arene ligand of a ruthenium(II) catalyst greatly improves its ability to catalyze asymmetric transfer hydrogenation (ATH) reactions. In this paper, we describe further applications of this versatile system to an extended substrate range.
- Morris, David J.,Hayes, Aidan M.,Wills, Martin
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p. 7035 - 7044
(2007/10/03)
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- Heteroditopic imino N-heterocyclic carbenes and their sulfur, selenium, and tungsten tetracarbonyl derivatives
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New heterditopic imino N-heterocyclic carbenes for use as chelating ligands in homogeneous catalysis are the focus of this contribution. The synthesis of the corresponding imidazolium precursors is accomplished in three steps by alkylation of imidazole wi
- Steiner, Georg,Kopacka, Holger,Ongania, Karl-Hans,Wurst, Klaus,Preishuber-Pfluegl, Peter,Bildstein, Benno
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p. 1325 - 1333
(2007/10/03)
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- Copper carbenoid mediated N-alkylation of imidazoles and its use in a novel synthesis of bifonazole
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1H-Imidazoles are readily N-alkylated by a Cu(acac)2 mediated reaction with α-diazocarbonyl compounds or with diazoalkanes generated in situ from the corresponding p-toluensulfonyl hydrazones. The antifungal agent bifonazole was prepared by the latter method. Graphical Abstract.
- Cuevas-Ya?ez, Erick,Serrano, Juan Manuel,Huerta, Gloria,Muchowski, Joseph M.,Cruz-Almanza, Raymundo
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p. 9391 - 9396
(2007/10/03)
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- Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: Preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods
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New analogues of the previously described 3-aryl pyridone KOR agonists have been synthesised by parallel synthetic methods, both in solution- and with solid-phase chemistry, making use of the well known and versatile Mitsunobu, Suzuki and Buchwald reactions. Opioid receptor binding data for the compounds produced is reported.
- Semple, Graeme,Andersson, Britt-Marie,Chhajlani, Vijay,Georgsson, Jennie,Johansson, Magnus J.,Rosenquist, Asa,Swanson, Lars
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p. 1141 - 1145
(2007/10/03)
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- A new series of miconazole analogs: Synthesis and in vitro antifungal and antimycobacterial activities
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The synthesis and antimicrobial activity of new miconazole analogs are reported. All compounds showed good antimycobacterial activity; some of them were also active against some strains of Candida albicans and Candida sp.. Of the synthesized compounds, two showed good activity both against some strains of Mycobacterium and some strains of Candida. Structure-activity relationships are discussed.
- Fioravanti, Rossella,Biava, Mariangela,Porretta, Giulio Cesare,Lampis, Giorgio,Deidda, Delia,Pompei, Raffaello
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p. 162 - 175
(2007/10/03)
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- Synthesis and antifungal activity of novel (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes
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A novel series of (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes IIIa-n were synthesized by condensation of substituted 1,3-dioxolan-4-ylmethyl p-toluenesulfonates 4 with 1-(hydroxyimino)-1-aryl-2-heterocyclylethanes 5.Compounds IIIa-n were found to have effective in vitro antifungal activity when evaluated against the pathogenic fungi Candida albicans, Aspergillus flavus and Fusarium solani with MIC (minimum inhibitory concentration values of 10 μg*ml-1 for IIIa-l and 5 μg*ml-1 for IIIm,n. antifungal activity / 1,3-dioxolane / ethylideneaminooxy / imidazole / 1,2,4-triazole
- Baji, H.,Flammang, M.,Kimny, T.,Gasquez, F.,Compagnon, P. L.,Delcourt, A.
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p. 617 - 626
(2007/10/02)
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- Substituted (1,2-Diarylethyl)amide Acyl-CoA:Cholesterol Acyltransferase Inhibitors: Effect of Polar Groups on in Vitro and in Vivo Activity
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Substituted (1,2-diarylethyl)amides have been prepared and evaluated for their ability to inhibit microsomal acyl-CoA:cholesterol acyltransferase activity in vitro and to lower hepatic cholesteryl ester content in vivo in a cholesterol-fed hamster.Simple unsubstituted (diarylethyl)amides were potent inhibitors in vitro but showed poor activity in vivo.Introduction of polar groups at specific locations on the diarylethylamine moiety decreased in vitro activity but increased in vivo activity.Both effects were highly structure dependent, suggesting specific interactions which were mediating activity in each model.Optimization of these opposing effects led to compounds which were potent in both models.
- Clader, John W.,Berger, Joel G.,Burrier, Robert E.,Davis, Harry R.,Domalski, Martin,et al.
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p. 1600 - 1607
(2007/10/02)
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- Hofmann-type elimination in the efficient N-alkylation of azoles: Imidazole and benzimidazole
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A simple and efficient preparation of 1-substituted 1H-azoles (imidazole and benzimidazole) has been developed, which involves a selective Hofmann-type elimination of the 2-cyanoethyl group from the azolium salts obtained by the reaction of halides with 1H-imidazole-1-propanenitrile and 1H-benzimidazole-1-propanenitrile. Overall yields of 1-substituted 1H-azoles decreased in the order: primary alkyl halides ≥ allylhalides ≥ secondary alkyl halides ≥ benzyl halides > α-keto halides, in relation to the alkylating agent, and imidazole ≥ benzimidazole, in relation to the azole, respectively.
- Horvath
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p. 102 - 106
(2007/10/02)
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- Research on antibacterial and antifungal agents. X. Synthesis and antimicrobial activities of 1-phenyl-2-(1H-azol-1-yl) ethane derivatives. Anticonvulsant activity of 1-(4-methylphenyl)-2-(1H-imidazol-1-yl) ethanol.
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The synthesis and antimicrobial activity of new phenylazolylethane derivatives are reported.Antimicrobial data in comparison with those obtained with miconazole, fluconazole, enilconazole, imazalil sulfate, pipemidic acid and minocycline showed that tested compounds generally possessed poor or weak activity.Toxicity and anticonvulsant activity of 1-(4-methylphenyl)-2-(1H-imidazol-1-yl)ethanol and structural likeness to Denzimol were also tested.The obtained results showed interesting anticonvulsant activity but only on the supraspinal region. azoles / antifungal / anticonvulsant agent
- Porretta, G. C.,Fioravanti, R.,Biava, M.,Cirilli, R.,Simonetti, N.,et al.
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p. 749 - 760
(2007/10/02)
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- An improved and convenient procedure for the synthesis of 1-substituted imidazoles
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1-Protected imidazoles, such as 1-acetyl- and 1-benzoylimidazoles, react with various halides, such as benzyl, allyl, α-keto, and alkyl halides, to give 1-protected-3-substituted imidazolium salts in high yields. The resultant imidazolium salts are easily deprotected by treatment with water or alcohols to give the corresponding 1-substituted imidazoles in excellent yields. In this reaction the yields of 1-substituted imidazoles vary with the kinds of halides used and/or with the protecting groups, and the yields increase in the following order: benzyl halides≥allyl halides~α-keto halides>alkyl halides, and acetyl≥benzoyl>ethoxycarbonyl>diethoxymethyl>trimethylsilyl>tosyl.
- Kamijo,Yamamoto,Harada,Iizuka
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p. 1213 - 1221
(2007/10/02)
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- 1,2,4-Triazole-containing compounds and their use as pesticides
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Plant fungicidal compounds of formula: STR1 WHEREIN R1 is hydrogen, or nitro, R3 is alkyl, furyl, thienyl or phenyl, R4 is hydrogen, halogen, nitro, phenyl, alkoxy or alkyl, n is 1, 2 or 3, and Z is C = O or a derivative t
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