- Synthesis of new 2,4-diaryl-6-methyl-5-nitropyrimidines as antibacterial and antioxidant agents
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A new series of 2,4-diaryl-6-methyl-5-nitropyrimidines (5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i) were synthesized in good yields by Suzuki-Miyaura coupling of 2,4-dichloro-6-methyl-5-nitropyrimidine (3) with various aryl boronic esters (4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i) in the presence of 1,1′- bis(diphenylphosphino)ferrocene dichloropalladium(II) (Pd(dppf) 2Cl2). Further, antibacterial and antioxidant properties were screened for the title compounds 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i. Most of the compounds possessed significant activity against Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis and Gram-negative bacteria Escherichia coli and Klebsiella pneumoniae. The antioxidant activity of the title compounds showed significant antioxidant activity when compared with vitamin C.
- Sura, Mallikarjun Reddy,Peddiahgari, Vasu Govardhana Reddy,Bhoomireddy, Rajendra Prasad Reddy,Vadde, Rama Krishna
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Read Online
- NITRATION
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The present invention relates to a process for preparing a nitrated compound, comprising the step of reacting a compound (A) comprising at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein said heteroaromatic ring comprises at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I) wherein Y is selected from the group consisting of hydrogen and nitro.
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Page/Page column 36; 37; 49; 39; 54
(2020/05/28)
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- Ethanol compound used as FGFR inhibitor
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The invention discloses an ethanol compound used as a FGFR inhibitor. The invention provides the compound as shown in a formula I which is described in the specification or a pharmaceutically acceptable salt thereof, a preparation method for the compound and application of the compound as a medicine to treatment of cancers.
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Paragraph 0031
(2017/03/17)
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- SAR studies on a novel series of human cytomegalovirus primase inhibitors
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A novel series of imidazolylpyrimidines were found to possess inhibitory activity against the human CMV UL70 primase. Extensive SAR studies on an HTS lead led to potent, orally bioavailable compounds with anti-CMV IC50 values of 150 nM in both
- Chen,Adrian,Cushing,DiMaio,Liang,Mayorga,Miao,Peterson,Powers,Spector,Stein,Wright,Xu,Ye,Jaen
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p. 2188 - 2192
(2008/02/03)
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- Discovery of a novel series of inhibitors of human cytomegalovirus primase
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Infection by human cytomegalovirus (hCMV) remains a potent threat to susceptible people throughout the world. We have discovered a series of imidazolyl-pyrimidine compounds, which were found to be irreversible inhibitors of the hCMV UL70 primase based on
- Cushing,Adrian,Chen,DiMaio,Doughan,Flygare,Liang,Mayorga,Miao,Mellon,Peterson,Powers,Spector,Stein,Wright,Xu,Ye,Jaen
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p. 4879 - 4883
(2007/10/03)
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- Synthesis and antiproliferative activity of 2,6-diamino-9-benzyl-9- deazapurine and related compounds
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Treatment of 6-bromomethyl- or 6-dibromomethyl-5-nitropyrimidine-2,4- diamine with KCN gave the same product - (2,6-diamino-5-nitropyrimidinyl) acetonitrile. Benzylation of the nitrile took place on the α-carbon to the cyano group preferentially affording
- Otmar, Miroslav,Masojidkova, Milena,Votruba, Ivan,Holy, Antonin
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p. 3187 - 3195
(2007/10/03)
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- 2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel CRF-1 receptor antagonists
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The discovery, synthesis and structure-activity studies of a novel series of 2-arylpyrimidin-4-ones as CRF-1 receptor antagonists is described. These compounds are structurally simple and display appropriate physical properties for CNS agents
- Hodgetts, Kevin J.,Yoon, Taeyoung,Huang, Jianhua,Gulianello, Michael,Kieltyka, Andrzej,Primus, Renee,Brodbeck, Robbin,De Lombaert, Stephane,Doller, Dario
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p. 2497 - 2500
(2007/10/03)
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- Addition of lithiated 9-deazapurine derivatives to a carbohydrate cyclic imine: Convergent synthesis of the aza-C-nucleoside immucillins
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Means have been developed for the synthesis and addition of 9-deaza-9-lithiopurine derivatives to the carbohydrate-derived cyclic imine 6 in facile convergent syntheses of biologically active aza-C-nucleosides.
- Evans,Furneaux,Hutchison,Kezar,Morris, Jr.,Schramm,Tyler
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p. 5723 - 5730
(2007/10/03)
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- Inhibitors of nucleoside metabolism
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The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof. The present invention also provides the use of the above compounds as pharmaceuticals, pharmaceutical compositions containing the compounds and processes for preparing the compounds.
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