- Preparation and application of novel quinolizine pH fluorescence molecular probe
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The invention discloses a novel quinolizine pH fluorescence molecular probe which has brand-new action mechanism as shown in the specification, wherein a skeleton structure is 4H-quinolizine-4-imine as shown in the compound in the formula II, C-N bond in
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Paragraph 0018
(2018/04/03)
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- PHARMACEUTICAL COMPOUND
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Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5/
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Page/Page column 92
(2016/03/14)
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- COMPOUNDS AND MATRICES FOR USE IN BONE GROWTH AND REPAIR
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Compositions of small molecules, matrices, and isolated cells including methods of preparation, and methods for differentiation, transdifferentiation, and proliferation of animal cells into the osteoblast blast cell lineage were described. Examples of ost
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Paragraph 0367
(2016/03/05)
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- Synthesis and cytotoxic evaluation of some new 1-(6- chloropyridazin-3-Yl)-3-H/Alkyl-4-phenyl-1H-pyrazol- 5-amines and their derivatives
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Synthesis of new 1-(6-chloropyridazin-3-yl)-3-H/alkyl-4-phenyl-1H-pyrazol-5-amines (3) was accomplished by the reaction of 3-chloro-6-hydrazinopyridazine (1) with differently substituted β-ketonitriles (2) under reflux in ethanol. Subsequently, a series of 6-amino derivatives (4, 5 and 6) was synthesized by amino-de-halogenation of 3 with secondry cyclic amines e.g. pyrrolidine, piperidine and morpholine respectively. Structures of all the compounds were established by IR, NMR (1H, 13C and 19F) and mass spectral data, and elemental analysis. All the compounds were screened for their cytotoxic effects against three cancer cell lines (SB-ALL, NALM-6, MCF-7) using colorimetric MTT assay.
- Mamta,Aggarwal, Ranjana,Smith, Jessie,Sadana, Rachna
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- Copper-catalyzed N-aryl-β-enaminonitrile synthesis utilizing isocyanides as the nitrogen source
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A novel synthetic protocol for N-aryl-β-enaminonitriles, which are useful building blocks for heterocycle synthesis, was developed using isocyanides as the nitrogen source. Using copper-catalyzed one-step reactions between isocyanides and benzyl cyanides under mild conditions, diverse N-aryl-β-enaminonitriles could be synthesized in excellent yields and with high atom-efficiency. N-Alkyl-β-enaminonitriles were also synthesized in good yields. A mechanism involving an imidoyl-copper intermediate was proposed based on mechanistic studies and previous reports. In addition, we demonstrated that a synthesized N-aryl-β-enaminonitrile could be utilized for the synthesis of a β-keto nitrile compound and 3-aminopyrazole.
- Kim, Seoksun,Hong, Soon Hyeok
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p. 1004 - 1012
(2015/03/30)
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- Catalytic α-monoallylation of aryl acetonitriles
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α-Cyano aldehydes undergo selective transition-metal-catalyzed monoallylation to provide α-allylated nitriles. The transformation leads to linear substitution products with palladium catalysts or branched allylated nitriles using an iridium catalyst. Faci
- Maji, Tapan,Tunge, Jon A.
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supporting information
p. 5072 - 5075
(2014/12/11)
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- β-Amination of saturated nitriles through palladium-catalyzed dehydrogenation, 1,4-addition, and re-dehydrogenation
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Amination at the β-position of 2-arylpropionitriles through catalytic dehydrogenation occurred by using [PdCl2(PMe3) 2] catalyst and bromobenzene. This is the first catalytic reaction involving the direct dehydrogenation of saturated nitriles.
- Ueno, Satoshi,Maeda, Ryohei,Yasuoka, Shohei,Kuwano, Ryoichi
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supporting information
p. 40 - 42
(2013/02/25)
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- Phenylpyrazolo[1,5-a]quinazolin-5(4 H)-one: A suitable scaffold for the development of noncamptothecin topoisomerase i (Top1) inhibitors
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In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted
- Taliani, Sabrina,Pugliesi, Isabella,Barresi, Elisabetta,Salerno, Silvia,Marchand, Christophe,Agama, Keli,Simorini, Francesca,La Motta, Concettina,Marini, Anna Maria,Di Leva, Francesco Saverio,Marinelli, Luciana,Cosconati, Sandro,Novellino, Ettore,Pommier, Yves,Di Santo, Roberto,Da Settimo, Federico
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supporting information
p. 7458 - 7462
(2013/10/21)
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- Discovery and characterization of a novel 7-aminopyrazolo[1,5-a]pyrimidine analog as a potent hepatitis C virus inhibitor
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We describe a novel 7-aminopyrazolo[1,5-a]pyrimidine (7-APP) derivative as a potent hepatitis C virus (HCV) inhibitor. A series of 7-APPs was synthesized and evaluated for inhibitory activity against HCV in different cell culture systems. The synthesis and preliminary structure-activity relationship study of 7-APP are reported.
- Hwang, Jong Yeon,Windisch, Marc Peter,Jo, Suyeon,Kim, Keumhyun,Kong, Sunju,Kim, Hyoung Cheul,Kim, Soohyun,Kim, Heeyoung,Lee, Myung Eun,Kim, Youngmi,Choi, Jihyun,Park, Dong-Sik,Park, Eunjung,Kwon, Jeongjin,Nam, Jiyoun,Ahn, Sujin,Cechetto, Jonathan,Kim, Junwon,Liuzzi, Michel,No, Zaesung,Lee, Jinhwa
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p. 7297 - 7301
(2013/02/23)
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- Esters of 2-phenylalkanenitriles and antifungal compositions containing them
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Esters of 2-phenylalkanenitriles, such as 3-acetoxy-2-(2-chloro-5-(difluoromethoxy)phenyl)propanenitrile and 3-acetoxy-2-(4-chlorophenyl)propanenitrile, and compositions containing such esters, are useful as fungicides at very low concentrations.
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Page/Page column 7
(2008/12/06)
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- Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes
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CDPPB [3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide] was recently described as the first centrally active, positive allosteric modulator of rat and human metabotropic glutamate receptor (mGluR) mGluR5 subtype. We explored the structural requirements for potentiation of glutamate-induced calcium release in naturally expressed mGluR5 in cultured rat astrocytes and increasing affinity for the allosteric antagonist binding site by evaluating 50 analogues of CDPPB. In the fluorometric calcium assay, CDPPB exhibited an EC50 value of 77 ± 15 nM in potentiating mGluR 5-mediated responses in cortical astrocytes and a Ki value of 3760 ± 430 nM in displacing [3H]methoxyPEPy binding in membranes of cultured HEK-293 cells expressing rat mGluR5. The structure-activity relationships showed that electronegative aromatic substituents in the para-position of the benzamide moiety of CDPPB increase potency. Both binding and functional activities were further increased with a halogen atom in the ortho-position of the 1-phenyl ring. These effects of substitution do not match those of either aromatic ring of MPEP [2-methyl-6-(phenylethynyl)-pyridine] for the antagonist allosteric binding site. Combination of the optimal substituents and aromatic positions resulted in 4-nitro-N-(1-(2-fluorophenyl)-3-phenyl-1H-pyrazol-5-yl)benzamide (VU-1545) showing Ki = 156 ± 29 nM and EC50 = 9.6 ± 1.9 nM in the binding and functional assays, respectively.
- De Paulis, Tomas,Hemstapat, Kamondanai,Chen, Yelin,Zhang, Yongqin,Saleh, Samir,Alagille, David,Baldwin, Ronald M.,Tamagnan, Gilles D.,Conn, P. Jeffrey
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p. 3332 - 3344
(2007/10/03)
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- Pyrazolotriazine compounds
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Pyrazolotriazine compounds of the formula: STR1 wherein R1 is OH or alkanoyloxy; R2 is H, OH, or SH; R3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) STR2 R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) STR3 or (xx) STR4 (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.
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- (Substituted-phenyl)-1,2,4-triazolo[4,3-a]-pyrimidines and (substituted-phenyl)-1,2,4-triazolo[1,5-a]pyrimidines
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This disclosure describes substituted 1,2,4-triazolo[1,5-a]pyrimidines and substituted 1,2,4-triazolo[4,3-a]pyrimidines which possess anxiolytic activity.
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