- Synthesis of novel 1, 2, 4-triazolopyrimidines and their evaluation as antimicrobial agents
-
Abstract: 7-aminopyrimidin-5(1H)-one (5) was utilized as a starting material for the preparation of new, Schiff bases (13–19), amides 23, 24, imide 25, as well as thiourea derivatives 30–33 incorporating the triazolopyrimidines nucleus in their molecules. Structural elucidations for the new compounds were based upon compatible microanalytical and spectroscopic measurement. Biological evaluation indicated that compounds 23, 31, 33, 32, and 30 possess promising antimicrobial activities. Graphical Abstract: [InlineMediaObject not available: see fulltext.]
- Abu-Hashem, Ameen A.,Hussein, Hoda A. R.,Abu-zied, Khadeja M.
-
-
Read Online
- Synthesis and Antimicrobial Activity of Some Novel Quinoline, Chromene, Pyrazole Derivatives Bearing Triazolopyrimidine Moiety
-
7-Amino-3-phenyl-[1,2,4]triazolo [4,3-a] pyrimidin-5(1H)-one (5) was utilized as key intermediate for the synthesis of some new, quinolines 9, 10, 11, 12, 13, 14 and 18, 19, 20, acrylonitrile 25 and 28, coumarin 26, and pyrazoles 31, 32, 33, 34 incorporating triazolopyrimidines. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H NMR, and mass spectral data. Representative compounds of the synthesized products were tested and evaluated as antimicrobial. Compounds 25, 28, 31, 32, 33, and 34 are the most promising.
- Abu-Hashem,Gouda
-
-
Read Online
- NEW PYRIMIDINE DERIVATIVES FOR PREVENTION AND TREATMENT OF GRAM-NEGATIVE BACTERIAL INFECTION, CONTAMINATION AND FOULING
-
New pyrimidine derivatives together with a membrane penetrating agent, optionally with a detectable isotope and pharmaceutical composition for use in treatment or prevention of Gram-negative bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of Gram-negative biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. New pyrimidine derivatives together with a membrane penetrating agent; for use as radiotracer in diagnosing or prognosing Gram-negative bacterial infection in a host mammal.
- -
-
Page/Page column 110
(2020/10/28)
-
- Pyrimidinone derivative, preparation method thereof and application thereof in resisting mycobacterium tuberculosis infection
-
The invention discloses a pyrimidinone derivative, a preparation method thereof and an application thereof in resisting mycobacterium tuberculosis infection. The structure of the pyrimidinone derivative is shown as a formula I, wherein R1, m, X, Y, Z, R2
- -
-
Paragraph 0157-0162
(2020/11/25)
-
- PYRIMIDINE DERIVATIVES FOR PREVENTION AND TREATMENT OF BACTERIAL INFECTIONS
-
New pyrimidine derivatives of formula (I), optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. New pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. New pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.
- -
-
Page/Page column 98
(2019/09/04)
-
- NOVEL N2, N4, N7, 6-TETRASUBSTITUTED PTERIDINE-2,4,7-TRIAMINE AND 2, 4, 6, 7-TETRASUBSTITUTED PTERIDINE COMPOUNDS AND METHODS OF SYNTHESIS AND USE THEREOF
-
Compounds as immune system modulators bearing a pteridine core are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing autoimmunity disease using the same are described.
- -
-
Page/Page column 0305; 0306
(2016/03/16)
-
- Chemical synthesis of some novel 6-aminouracil-2-thiones and their glycoside analogues
-
6-AMINOURACIL-2-THIONE (1) and its 5-bromo derivative 2 underwent alkylation yielding their respective S-alkyl products 4a-j. The reaction of compound 1 and aldehydes in the presence of chloroacetic acid afforded the respective thiazolopyrimidinyl acetamides 7a-d. The C-glycosides 8a, b and 9c-e were successfully prepared through condensing compound 1 and the appropriate sugar in the presence of chloroacetic acid. The behavior of certain S-alkyl derivative 4 towards amines and hydrazines was also studied. Structure elucidations for the new products were supported by compatible chemical and spectral measurements.
- Gaafar,Aly,Abu-Zied, Khadiga M.,Abdel-Rahman, Asmaa E.,Helmy
-
p. 779 - 797
(2017/04/17)
-
- New approach to synthesize symmetrical and unsymmetrical 6-(N-Alkyl(Aryl)amino)-and 6-(N, N-dialkyl(Aryl)amino)-2,4-bis(Alkyl(Aryl)Thio) pyrimidines as anti-platelet agents
-
A new and straightforward procedure has been developed for the preparation of symmetrical and unsymmetrical 6-(N-alkyl(aryl)amino)-and 6-(N,N- bisalkyl(aryl)amino)-2,4-bis(alkyl(aryl)thio)pyrimidines. The two identical or different alkylthio groups were s
- Liu, Guocheng,Xu, Jiaxi,Yu, Mingwu,Chen, Ning,Zhang, Si,Ding, Zhongren,Du, Hongguang
-
scheme or table
p. 650 - 659
(2012/06/01)
-
- MATERIALS AND METHODS FOR IMMUNOASSAY OF PTERINS
-
Methods of assaying for (i) a pterin by immunoassay employing a pterin as capture agent, (ii) neopterin by chemiluminescent microparticle immunoassay (CMIA) employing an anti-neopterin antibody (Ab) as capture agent, (iii) neopterin by an immunoassay (IA) employing an acridinium (Acr)-labeled anti-neopterin Ab as conjugate, and (iv) neopterin by an IA employing Acr-labeled neopterin as tracer; an Acr-labeled anti-neopterin Ab; a conjugate/complex comprising anti-neopterin Ab and a carrier scaffold; a conjugated pterin; a conjugate comprising an Acr-labeled pterin and a carrier scaffold; an immunogen comprising neopterin and a carrier protein; a conjugate comprising such an immunogen and an Acr compound; an immunogen comprising a carrier protein and a neopterin hapten; a conjugate comprising such an immunogen and an Acr compound; a kit for assaying a pterin comprising a pterin as a capture agent and instructions for IA; and a kit for assaying neopterin comprising an anti-neopterin Ab as a capture agent and instructions for CMIA, neopterin comprising an Acr-labeled anti-neopterin Ab as a conjugate and instructions for IA, or Acr-labeled neopterin as a tracer and instructions for IA.
- -
-
-
- AZOLOPYRIDINE AND AZOLOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF
-
Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
- -
-
Page/Page column 114-115
(2012/03/26)
-
- Novel synthesis approach and antiplatelet activity evaluation of 6-alkylamino-2,4-dialkyl(aryl)thiopyrimidines
-
A new and efficient procedure has been designed for the preparation of 6-alkylamino-2,4-dialkyl(aryl)thiopyrimidines. The first alkylthio group was introduced into the pyrimidine ring by S-alkylation. The introduction of the second one was successfully ac
- Liu, Guocheng,Xu, Jiaxi,Park, Ki Chul,Chen, Ning,Zhang, Si,Ding, Zhongren,Wang, Feng,Du, Hongguang
-
experimental part
p. 5156 - 5161
(2011/07/31)
-
- 6-Amino-2-mercapto-3H-pyrimidin-4-one derivatives as new candidates for the antagonism at the P2Y12 receptors
-
P2Y12 plays an important role in platelet aggregation, which makes it an interesting target for antithrombotic agents. Compounds that antagonize P2Y12 include the active metabolites of thienopyridines and molecules that are structurally related to ATP, which is an antagonist of P2Y12. During the last few years, our group has been working on the development of P2Y12 receptors antagonists that are based on an extremely simple chemical structure, the 6-amino-2-mercapto-3H-pyrimidin-4-one, variously substituted at the sulfur and oxygen functions. This nucleus represents the simplified combination of two known P2Y12 antagonists: the active metabolite of the thienopyridines and ATP derivatives. The effects of the synthesized compounds were tested on ADP-induced human platelet aggregation, using light transmission aggregometry. None of the tested compounds induced platelet aggregation, while some of them, at concentration of 10-4 M, partially inhibited platelet aggregation induced by ADP 10-6 M. The most potent compound, 6b, antagonized the inhibitory effect of 2-methylthio-ADP on the forskolin-induced accumulation of cyclic-AMP in CHO FlpIN cells expressing recombinant human P2Y12-receptors. In addition, none of the tested compounds, including 6b, interfered with ligand binding to P1 receptors. Our results suggest that some of the synthesized compounds are specific antagonists of P2 receptors, and in particular of P2Y12 and suggest that further development of this structurally new series of compounds as P2Y12 receptors antagonists is recommended.
- Crepaldi, Pamela,Cacciari, Barbara,Bonache, Maria-Cruz,Spalluto, Giampiero,Varani, Katia,Borea, Pier Andrea,Kuegelgen, Ivar von,Hoffmann, Kristina,Pugliano, Mariateresa,Razzari, Cristina,Cattaneo, Marco
-
experimental part
p. 4612 - 4621
(2009/10/23)
-
- Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists
-
A number of derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine (5) were synthesized and biologically evaluated as A3 adenosine receptor (A3 AR) antagonists. The new compounds were designed as open chain analogues of a triazolopyrimidinone derivative displaying submicromolar affinity for the A3 AR, which had been previously identified using a 3D database search. Substituents R, R′, and R″ attached to the parent compound 5 were chosen according to factorial design and stepwise lead optimization approaches, taking into account the essentially hydrophobic nature of the A3 AR binding site. As a result, 5m (R = n-C3H 7, R′ = 4-ClC6H4CH2, R″ = CH3) was identified among the pyrimidine derivatives as the ligand featuring the best combination of potency and selectivity for the target receptor. This compound binds to the A3 AR with a Ki of 3.5 nM and is devoid of appreciable affinity for the A1, A 2A, and A2B ARs.
- Cosimelli, Barbara,Greco, Giovanni,Ehlardo, Marina,Novellino, Ettore,Da Settimo, Federico,Taliani, Sabrina,La Motta, Concettina,Bellandi, Marusca,Tuccinardi, Tiziano,Martinelli, Adriano,Ciampi, Osele,Trincavelli, Maria Letizia,Martini, Claudia
-
p. 1764 - 1770
(2008/12/22)
-
- Antitumor studies. Part 3: Design, synthesis, antitumor activity, and molecular docking study of novel 2-methylthio-, 2-amino-, and 2-(N-substituted amino)-10-alkyl-2-deoxo-5-deazaflavins
-
Various novel 10-alkyl-2-deoxo-2-methylthio-5-deazaflavins have been synthesized by reaction of 6-(N-alkylanilino)-2-methylthiopyrimidin-4(3H)-ones with Vilsmeier reagent. The similar 2-(N-substituted amino) derivatives were prepared by nucleophilic replacement reaction of the 2-methylthio moiety by appropriate amines. The 2-oxo derivatives (i.e., 5-deazaflavins) were obtained by acidic hydrolysis of the 2-methylthio derivatives. The antitumor activities against CCRF-HSB-2 and KB cells and the antiviral activities against HSV-1 and HSV-2 have been investigated in vitro, and many compounds showed promising antitumor activities. Furthermore, AutoDock molecular docking into PTK has been done for lead optimization of these compounds as potential PTK inhibitors. Whereas, the designed 2-deoxo-5-deazaflavins connected with amino acids at the 2-position exhibited the good binding affinities into PTK with more hydrogen bonds.
- Ali, Hamed I.,Ashida, Noriyuki,Nagamatsu, Tomohisa
-
p. 6336 - 6352
(2008/03/18)
-
- Hit-to-Lead studies: The discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists
-
A Hit-to-Lead optimisation programme was carried out on a high throughput screening hit, the thiazolopyrimidine 1, resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 29.
- Baxter, Andrew,Cooper, Anne,Kinchin, Elizabeth,Moakes, Kerry,Unitt, John,Wallace, Alan
-
p. 960 - 963
(2007/10/03)
-
- Syntheses of highly functionalised 6-substituted pteridines.
-
Methods for the synthesis of polyfunctional 6-substituted pteridines from the corresponding 6-aldehydes are described. Alkene, ester, ketone, amide, cyano, oxime, bromo, methoxy and dihydroxy functional groups have all been introduced principally through
- Guiney, Donie,Gibson, Colin L,Suckling, Colin J
-
p. 664 - 675
(2007/10/03)
-
- Tricyclic base analogues
-
Nucleoside analogues have structure (2) wherein Q is H or a sugar moiety or sugar analogue or a modified sugar or a nucleic backbone or backbone analogue, W is an alkylene or alkenylene chain of 0-5 carbon atoms, any of which may carry a substituent R8, X is O or N or NR12or CR10, X′ is O or S or N, provided that when X′ is O or S, then X is C, Y is CH or N, R6is NH2or SMe or SO2Me or NHNH2, each of R7and R8is independently H or F or alkyl or alkenyl or aryl or acyl or a reporter moiety, R12is independently H or alkyl or alkenyl or aryl or acyl or a reporter moiety, and R10is H or ═O or F or alkyl or aryl or a reporter moiety.
- -
-
-