- Synthesis of new tetracyclic azaheteroaromatic cores via auto-tandem Pd-catalyzed and one-pot Pd- and Cu-catalyzed double C-N bond formation
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Inter- and intramolecular transition metal-catalyzed amination of 2-chloro-3-iodopyridine and 2,3-dibromopyridine, respectively, with benzodiazinamines yielded six hitherto unknown tetracyclic azaheteroaromatic cores. C-N bond formation was achieved via auto-tandem (Pd-catalyst) as well as one-pot (sequential use of a Pd- and Cu-catalyst) catalysis.
- Rauws, Tom R.M.,Biancalani, Claudio,De Schutter, Joris W.,Maes, Bert U.W.
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- Zn(II) complexes of (E)-4-(2-(pyridin-2-ylmethylene)hydrazinyl)quinazoline in combination with non-steroidal anti-inflammatory drug sodium diclofenac: Structure, DNA binding and photo-cleavage studies, antioxidant activity and interaction with albumin
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The interaction of the novel quinazoline (E)-4-(2-(pyridin-2-ylmethylene)hydrazinyl)quinazoline (L) with Zn2+ was performed in the absence or presence of the non-steroidal anti-inflammatory drug sodium diclofenac (Nadicl) and resulted in the fo
- Kakoulidou, Chrisoula,Gritzapis, Panagiotis S.,Hatzidimitriou, Antonios G.,Fylaktakidou, Konstantina C.,Psomas, George
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- One-pot three-component synthesis of 2-substituted 4-aminoquinazolines
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A facile and rapid synthesis of the title compounds via one-pot reaction of 2-aminobenzonitrile, orthoesters and ammonium acetate under solvent-free and microwave condition is described.
- Rad-Moghadam, Kurosh,Samavi, Laleh
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- Novel compound or pharmaceutically acceptable salt thereof and pharmaceutical composition for prevention or treatment of disease caused by influenza virus infection containing the same as an active ingredient
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The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active component for preventing or treating diseases related with influenza virus infection. The novel compound represented by chemical formula 1 has remarkable antivirus activity against influenza virus without cytotoxicity to human cells and thus has little side effects to human bodies. Therefore, the pharmaceutical composition having the same as an active component can be usefully used for preventing or treating diseases which occur through influenza virus infection such as flu, cold, sore throat, bronchitis, pneumonia, avian influenza, swine flu, goat flu, etc.COPYRIGHT KIPO 2016
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Paragraph 0680; 0682
(2016/10/07)
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- Microwave-assisted thermal decomposition of formamide: A tool for coupling a pyrimidine ring with an aromatic partner
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Rapid and efficient generation of CO and NH3 in the reaction mixture via microwave-assisted thermal decomposition of formamide may represent a significant improvement over existing methods for coupling a pyrimidine ring with an aromatic partner. This work aims at alerting readers on the probability to observe interesting phenomena and reactions when this very powerful heating mode is associated with thermally unstable reagents.
- Loidreau, Yvonnick,Besson, Thierry
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p. 4852 - 4857
(2011/08/06)
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- Synthesis of a new isomer of creatinine and its use in the preparation of the food mutagen 2-amino-1-methyl-6-phenyl-1H-imidazo[4,5-b]pyridine (PHIP)
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Base-induced cyclization of N′-cyanomethyl-N′-methylurea gives 1-methyl-4-amino-imidazol-2-one, this in turn is condensed with 3-hydroxy-2-phenylacrolein to yield an imidazo[4,5-b]pyridine which is converted into 2-amino-1-methyl-6-phenyl-1H-imidazo[4,5-b]pyridine (PHIP).
- Bergman, Jan
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scheme or table
p. 5631 - 5632
(2011/02/22)
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- Inhibitors of apoptosis in lymphocytes: Synthesis and biological evaluation of compounds related to pifithrin-α
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The chemoprotection of cells from apoptosis induced by toxins or ionizing radiation could be important for biodefense and in the treatment of acute injuries. We describe a series of small heterocycles, including fused benzothiazoles, benzimidazoles, and related compounds, that abrogate thymocyte apoptosis induced by dexamethasone and γ-irradiation. To optimize the protective activity of the previously reported pifithrin-α (PFT-α, 1), various derivatives and analogues of this and the corresponding ring-closed imidazobenzothiazole (IBT, 39) were synthesized. The aromatic analogues of 39 were more protective than 39, while the aromatic analogues of 1 were not active. Compound 19 containing a pyrrolidinyl substituent on the phenyl ring provided potent antiapoptotic activity (EC50 of 1.31 μM compared to 4.16 μM for 1). Modification of aromatic 39 with a pyrrolidinyl para substituent (compound 60) enhanced the activity, lowering the EC50 to 0.35 μM. Also, 60 provided significant protection against γ-irradiation-induced apoptosis, as expected. Compounds 19 and 60 may be promising for potential clinical development.
- Barchéchath, Sylvie D.,Tawatao, Rommel I.,Corr, Maripat,Carson, Dennis A.,Cottam, Howard B.
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p. 6409 - 6422
(2007/10/03)
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- A new application of diphenylphosphorylazide (DPPA) reagent: Convenient transformations of quinolin-4-one, pyridin-4-one and quinazolin-4-one derivatives into the 4-azido and 4-amino counterparts
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Herein, we describe a transformation of the oxo-function of a series of quinolin/pyridin/quinazolin-4-ones into 4-azido and thence into 4-amino derivatives in moderate yields by a very short and convenient new procedure using DPPA (diphenylphosphoryl azide) as reagent. A mechanism for this interesting new application of DPPA is suggested based on the identification of some of the intermediates.
- Aizikovich, Alexander,Kuznetsov, Vladimir,Gorohovsky, Sofia,Levy, Amalia,Meir, Simha,Byk, Gerardo,Gellerman, Garry
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p. 4241 - 4243
(2007/10/03)
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- Isoquinoline and quinazoline urea analogues as antagonists for the human-adenosine A3 receptor
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Isoquinoline and quinazoline urea derivatives were found to bind to human adenosine AS receptors. Series of N-phenyl-N'-quinazolin-4-ylurea derivatives and N-phenyl-N'-isoquinolin-1-ylurea derivatives were synthesized and tested in radioligand binding ass
- Van Muijlwijk-Koezen, Jacqueline E.,Timmerman, Henk,Van Der Goot, Henk,Menge, Wiro M. P. B.,Von Drabbe Künzel, Jacobien Frijtag,De Groote, Miriam,Ijzerman, Adriaan P.
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p. 2227 - 2238
(2007/10/03)
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- Heterocyclic Compounds with a Bridgehead Nitrogen Atom. Synthesis in the Imidazoquinazoline Series
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The structures of imidazoquinazolines were reexaminated and established by spectroscopic studies with the aid of high-field 1H and 13C nmr and mass spectra.In acidic media, 3 reacts to give the products of electrophilic substitution reaction and ring opening compound 5, leading to the imidazobenzotriazine ring.
- Gueiffier, A.,Viols, H.,Chapat, J. P.,Chavignon, O.,Teulade, J. C.,Dauphin, G.
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p. 421 - 425
(2007/10/02)
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- Urea cycle: Chemical simulation of arginine biosynthesis
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We have successfully simulated the salient features of the urea cycle. In this effort an appropriately protected ornithine was transformed to citrulline, via use of a novel amide transfer reagent; the citrulline, in turn, was converted into argininosuccinate which necessitated a new activation procedure to enable acceptance of dimethyl aspartate. Fragmentation of argininosuccinate under carefully controlled conditions afforded arginine. The final step in the cycle, namely, the hydrolysis of arginine to urea and ornithine, has already been accomplished. Amino group transfer from aspartate has also been demonstrated in the conversion of hypoxanthine to adenine.
- Ranganathan,Rathi
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p. 2351 - 2354
(2007/10/02)
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- On the Amination of Azaheterocycles. A New Procedure for the Introduction of an Amino Group
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A new method of amination of diazines and triazines, using potassium amide, liquid ammonia and potassium permanganate, has been described.
- Hara, Hiroshi,Plas, Henk C. van der
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p. 1285 - 1287
(2007/10/02)
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