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Nucleosides, Nucleotides & Nucleic Acids 2020SUMMARYIn June 2019, the Purine and Pyrimidine Society (PPS) organized the 18 biennial symposium on Purine and Pyrimidine Metabolism at the International Agency for...
SUMMARYIn June 2019, the Purine and Pyrimidine Society (PPS) organized the 18 biennial symposium on Purine and Pyrimidine Metabolism at the International Agency for Research on Cancer in Lyon, France. This meeting went over 3 days and gathered students and researchers working in various specialties such as inborn errors, hyper- and hypouricemia and gout, cancer, enzymology, and cardiovascular diseases to exchange and discuss recent advances in the field of purine and pyrimidine metabolism. Here, we give an overview of oral presentations given during the symposium.
Topics: Disease; Humans; Purines; Pyrimidines
PubMed: 32182157
DOI: 10.1080/15257770.2020.1730891 -
Pest Management Science Aug 2015A series of novel pyrazolylpyrimidine derivatives were designed, synthesised and characterised by IR, (1) H NMR, (13) C NMR, mass spectroscopy and elemental analysis....
BACKGROUND
A series of novel pyrazolylpyrimidine derivatives were designed, synthesised and characterised by IR, (1) H NMR, (13) C NMR, mass spectroscopy and elemental analysis. The herbicidal activities of 30 pyrazolylpyrimidine derivatives were assessed.
RESULTS
Nine compounds caused good herbicidal activity for Pennisetum alopecuroides L. Among them, N-ethyl-6-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-pyrimidin-4-amine exhibited the strongest inhibitory activity against the root growth of P. alopecuroides, with an IC50 of 1.90 mg L(-1) . 2-Methyl-4-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-6-(prop-2-yn-1-yloxy)pyrimidine produced the highest inhibition of chlorophyll level in seedlings of P. alopecuroides (IC50 = 3.14 mg L(-1) ).
CONCLUSION
The structure-activity relationship indicated that the alkynyloxy group at the 6-position on the pyrimidine ring played a very important role for bleaching activities. When the alkynyloxy group was replaced by alkoxy, amino, alkylthio and alkylsulfonyl groups, the bleaching activities of the compounds were diminished. However, the compounds substituted by an amino at the 6-position of the pyrimidine ring exhibited excellent inhibition activities against weed root growth.
Topics: Brassica; Carotenoids; Chlorophyll; Herbicides; Pennisetum; Plant Roots; Pyrazoles; Pyrimidines; Seedlings; Structure-Activity Relationship; Weed Control
PubMed: 25256846
DOI: 10.1002/ps.3918 -
Nucleosides, Nucleotides & Nucleic Acids Jun 2008
Topics: Humans; Purines; Pyrimidines
PubMed: 18600501
DOI: 10.1080/15257770802135620 -
European Journal of Medicinal Chemistry Jul 2012Two groups of hybrid compounds: the quinazolinone-dihydropyrimidines and quinazolinone-pyrimidines, were synthesized. The starting derivative 3 was reacted with...
Two groups of hybrid compounds: the quinazolinone-dihydropyrimidines and quinazolinone-pyrimidines, were synthesized. The starting derivative 3 was reacted with chloroacetyl chloride to give intermediate 5 which was condensed with the 2-mercaptopyrimidines 4a-c affording compounds 6a-c. These latter compounds underwent hydrolysis and N-alkylation reactions to give the dihydropyrimidine derivatives 7a-c and 8a-f, respectively. The chloro derivatives 9a-c subsequently reacted with various anilines furnishing compounds 10a-i. The anti-inflammatory activity of the synthesized compounds were evaluated using the carrageenan-induced rat paw oedema model and ulcer indices for the most active compounds were calculated. Five compounds were found more active and less ulcerogenic than diclofenac particularly compound 10 g (IC(50) = 116.73 μmol/kg; ulcer index = 11.38). Compound 10 g was also 2-fold more selective inhibitor of COX-2 than COX-1.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Chemistry Techniques, Synthetic; Edema; Female; Male; Pyrimidines; Quinazolinones; Rats; Ulcer
PubMed: 22551678
DOI: 10.1016/j.ejmech.2012.03.050 -
Bioorganic & Medicinal Chemistry Dec 2006All the nine 1,3-dialkylated-pyrimidin-2,4-diones investigated are active against all the 59 human tumor cell lines. Compounds 2, 3, 4, and 6 show significant...
All the nine 1,3-dialkylated-pyrimidin-2,4-diones investigated are active against all the 59 human tumor cell lines. Compounds 2, 3, 4, and 6 show significant anti-cancer activities at some specific cell lines while compounds 7 and 9 exhibit anti-cancer activities against more number of cell lines. The structure-activity relationship studies indicate that the presence of piperidine/pyrrolidine at the end of C-6 chain, benzoyl group at C-5, and benzyl groups at N-1, N-3 of the pyrimidine ring increases the anti-cancer activities of these molecules.
Topics: Antineoplastic Agents; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Neoplasms; Piperidines; Propanolamines; Pyrimidines; Pyrimidinones; Pyrrolidines; Structure-Activity Relationship
PubMed: 16949293
DOI: 10.1016/j.bmc.2006.08.025 -
Molecules (Basel, Switzerland) Nov 2020A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare...
A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55'DC. Among them, compounds ethyl 6-(5-(-tolylcarbamoyl)pyrimidin-2-yl)nicotinate () and ethyl 6-(5-((3,4-difluorophenyl)carbamoyl)pyrimidin-2-yl)nicotinate () show the best activities with IC values of 45.69 μM and 45.81 μM, respectively. Furthermore, the study of anti-fibrosis activity was evaluated by Picro-Sirius red staining, hydroxyproline assay and ELISA detection of Collagen type I alpha 1 (COL1A1) protein expression. Our study showed that compounds and effectively inhibited the expression of collagen, and the content of hydroxyproline in cell culture medium in vitro, indicating that compounds and might be developed the novel anti-fibrotic drugs.
Topics: Animals; Cell Line, Tumor; Cell Proliferation; Collagen Type I; Collagen Type I, alpha 1 Chain; Enzyme-Linked Immunosorbent Assay; Fibrosis; Hepatic Stellate Cells; Inhibitory Concentration 50; Prolyl Hydroxylases; Pyrimidines; Rats
PubMed: 33182574
DOI: 10.3390/molecules25225226 -
Acta Poloniae Pharmaceutica 2015In this study, a series of syntheses was conducted on the pyrimidine system, obtaining bisulfite carboxyl derivatives 4 and hydroxy derivatives 5. In addition, a series...
In this study, a series of syntheses was conducted on the pyrimidine system, obtaining bisulfite carboxyl derivatives 4 and hydroxy derivatives 5. In addition, a series of syntheses were carried out as a result of which both alkyl and aromatic amines were obtained. Then, the attempt was made to cyclize these amines in the Mannich reaction to pyrimido[4,5-d]pyrimidines 11, 12. After determination of chemical structure using physicochemical tests, also by means of crystallographic tests, all the newly obtained derivatives underwent microbiological tests on bacterial strains and fungi. The most interesting results of the microbiological tests are included later in the study.
Topics: Anti-Bacterial Agents; Antifungal Agents; Bacteria; Fungi; Microbial Sensitivity Tests; Pyrimidines
PubMed: 25850201
DOI: No ID Found -
European Journal of Medicinal Chemistry Nov 2008A number of derivatives of isoxazolo[4,5-d]pyrimidine were prepared with structures similar to that of purine. Condensation of the hydrazide of...
A number of derivatives of isoxazolo[4,5-d]pyrimidine were prepared with structures similar to that of purine. Condensation of the hydrazide of 4-amino-5-benzoylisoxazolo-3-carboxylic acid 2 with ethyloxalyl chloride followed by cyclization gave 3-oxdiazolo-[1,3,4]-4-amino-5-benzoylisoxazole 7 which, upon cyclization with acetonitrile followed by reactions with different amines, gave derivatives of isoxazolo[4,5-d]pyrimidine 9 and 10d-g. Compounds 8g and 10f were tested for their effects on the immune response in the mouse model. Both compounds significantly inhibited the humoral immune response in vivo to sheep erythrocytes at a dose of 100 microg, whereas in the delayed type hypersensitivity assay a suppressive activity was shown only by compound 10f. In addition, compound 8g inhibited and compound 10f stimulated the proliferative response of mouse splenocytes to concanavalin A. The results indicated that compound 10f was a universal inhibitor of the immune response, while compound 8g selectively suppressed the humoral immune response.
Topics: Animals; Cell Line, Tumor; Cell Proliferation; Drug Evaluation, Preclinical; Female; Humans; Isoxazoles; Male; Mice; Models, Molecular; Molecular Structure; Pyrimidines; Spleen
PubMed: 18358570
DOI: 10.1016/j.ejmech.2008.01.035 -
Bioorganic & Medicinal Chemistry Letters Mar 2014A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class,...
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.
Topics: Amidohydrolases; Amino Alcohols; Analgesics; Animals; Binding Sites; Brain; Catalytic Domain; Disease Models, Animal; Enzyme Inhibitors; Half-Life; Humans; Molecular Docking Simulation; Neuralgia; Protein Binding; Pyrimidines; Rats; Structure-Activity Relationship
PubMed: 24513048
DOI: 10.1016/j.bmcl.2014.01.064 -
The Journal of General Physiology May 1950The distribution of purines and pyrimidines in desoxypentose nucleic acids prepared from a variety of animal and plant sources has been studied. 1. The nucleic acids...
The distribution of purines and pyrimidines in desoxypentose nucleic acids prepared from a variety of animal and plant sources has been studied. 1. The nucleic acids were prepared from calf thymus, calf kidney, sheep spleen, horse spleen, chicken erythrocyte, turtle erythrocyte, trout sperm, shad testes, sea urchin sperm, wheat germ, and Pneumococcus Type III. 2. Separate hydrolyses were carried out for the determination of purines and pyrimidines. These procedures permitted nearly quantitative recovery of nucleic acid phosphorus in many of the preparations examined. 3. In the case of those preparations where a quantitative recovery was obtained it can be concluded that no bases other than adenine, guanine, thymine, and cytosine were present in appreciable amounts. 4. The distribution of purines and pyrimidines in all the nucleic acids studied renders the tetranucleotide hypothesis untenable. 5. The results of the analyses have indicated no great differences in the composition of these nucleic acids with respect to purines and pyrimidines.
Topics: Adenine; Animals; Cattle; Cytosine; Guanine; Horses; Nucleic Acids; Purines; Pyrimidines; Sheep; Thymine
PubMed: 15422104
DOI: 10.1085/jgp.33.5.497