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Pyrimidine derivatives
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Ebook "Photofunctionalization of molecular switch based on pyrimidine ring rotation in copper complexes" provides a detailed description of photofunctionalization of molecular switch based on pyrimidine ring rotational isomerization in copper complexes bearing two bidentate ligands. The most important features of this work focus on the properties associated with the rotational isomerization based on the two possible coordination geometries at the copper center derived from two nitrogen atoms on the unsymmetrically substituted pyrimidine ring.
131p
nhanphanguyet
28-01-2024
3
2
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In our continuing search for bioactive molecules, we collected a Streptomyces fradiae strain cultured from a prickly pen shell sample obtained at Van Phong, Khanh Hoa province, Vietnam. The ethyl acetate extract of Streptomyces fradiae G650 exhibited the strong inhibition against a panel of gram-positive bacteria including Enterococcus faecalis ATCC 29212, Staphylococcus aurerus ATCC 25923, Bacillus cereus ATCC 14579, and the yeast Candida albicans with the MIC values of 8, 32, 32, 8 µg/mL, respectively.
8p
viannee
02-08-2023
6
3
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3-Substituted-1-phenyl-1H -pyrazolo[3,4-d]pyrimidin-4-amines 2a–c were synthesized by treating 5-aminopyrazole-4-carbonitriles 1a–c with formamide. The reactivity of compounds 1a–c towards some cyclic anhydrides was studied. The condensation of 5-aminopyrazole-4-carbonitrile 1b with triethylorthoformate gives imidate 7b, which reacts with a series of primary amines and leads to pyrazolo[3,4-d]pyrimidine-4-amines 9 and 10. The reaction of imidate 7b with ammonia and hydroxylamine afforded pyrazolopyrimidine 2b and pyrazolo[3,4-d]pyrimidin-5-(4H)-ol 11, respectively.
12p
langthannam
29-12-2021
13
0
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The reasonable shifts in FT-IR and NMR spectral signals of the complexes with respect to the free ligand confirm good coordination of the Schiff-base ligand with the metal through imine nitrogen and oxygen atoms of Schiff base moiety. The Schiff-base ligand and the complexes were screened for antimicrobial activity and fluorescent behaviour. From the analytical and spectral data, the stoichiometry was found to be 1:2 for all the complexes. An octahedral structure was proposed. All the complexes were found to be active against bacteria and fungi.
10p
langthannam
29-12-2021
12
0
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The cyclocondensation of 2-amino-5,6,7,8-tetrahydro-4H -cyclohepta[b] selenophene-3-carbonitrile (1) with formic acid and formamide gave the selenophenopyrimidine 15 and selenophenopyrimidone 6 derivatives. The reaction of 6 with phosphorus oxychloride produced 4-chloro-6,7,8,9-tetrahydro-5H -cyclohepta[4,5] seleno[2,3-d]pyrimidine (12), the key compound for our nucleophilic substitution reactions.
10p
langthannam
29-12-2021
6
0
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A series of 1,4-phenylene-bis-chalcones 3a–3h were synthesized by the reaction of terephthalaldehyde with substituted arylketones in this study. The novel 1,4-phenylene-bis-pyrimidine-2-amine derivatives 5a–5h were obtained by the addition of guanidine hydrochloride to 1,4-phenylene-bis-chalcone 3a–3h in ethanolic KOH under reflux conditions. The structure of the compounds was explained by means of IR, 1H NMR, 13C NMR, and elemental analyses. The anticancer activities of 3a–3h and 5a–5h were investigated against rat brain tumor cells and human uterus carcinoma in vitro.
9p
langthannam
29-12-2021
7
0
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Multicomponent reaction of dimedone or 1,3-dimethylbarbituric acid and malononitrile with a series of bis(indoline-2,3-diones) afforded the corresponding bis(2-amino-7,7-dimethyl-2’,5-dioxo-5,6,7,8-tetrahydrospiro[chromene4,3’-indoline]-3-carbonitrile) and bis(7’-amino-1’,3’-dimethyl-2,2’,4’-trioxo-1’,2’,3’,4’-tetrahydrospiro[indoline-3,5’-pyrano [2,3-d]pyrimidine]-6’-carbonitrile) derivatives in good to excellent yield.
10p
langthannam
29-12-2021
1
0
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A straightforward method for the preparation of benzo[4,5]imidazo[1,2-a]pyrimidine derivatives catalysed by an acidic deep eutectic solvent from choline chloride (ChCl) and phenol via the Biginelli reaction of 2-aminobenzimidazole, ethyl acetoacetate, and aldehydes has been developed under metal- and solvent-free conditions. The desired products were obtained in moderate to good yield (49-79%) and the DESs were known as an economical and environmentally friendly catalyst.
3p
princessmononoke
29-11-2021
11
1
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Twenty-five new hydroxy- and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20–34) and 4,6-diarylpyrimidine-2(1H)-thiol derivatives (35–44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1- one compounds (1–19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20–44) were evaluated with regard to their α-glucosidase activity. However, only compounds 22–25, 27, 31, 34, 35, 37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC50 values of the active compounds ranged between 2.36 and 13.
16p
tudichquannguyet
29-11-2021
9
1
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Pyrimidine derivatives are well known due to their remarkable pharmacological potential in various fields of science, and they are also present in some natural substances like DNA and RNA. These scaffolds manifest diversified biological activities such as antimicrobial, antiinflammatory, anti-HIV, antitubercular, antitumor, antineoplastic, and antimalarial. A pyrimidine ring is constructed when chalcones, amidines, guanidine, nitriles, isocyanates, urea, thiourea, and aminopyrazoles undergo condensation, coupling, or cyclization reactions.
38p
tudichquannguyet
29-11-2021
11
1
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A fast and efficient method for the synthesis of naphthopyranopyrimidinones derivatives in excellent yields was developed through cyclocondensation reaction between previously prepared pyrimidinic hydrazides and some electrophilic species such as 2,4-pentanedione, 2,5-hexanedione, cyclic anhydrides, and phenylthioisocyanate under microwave irradiation. Compared to the conventional methods applied, it was found that better yields and shorter reaction times were achieved using microwave-assisted synthesis.
17p
tudichquannguyet
29-11-2021
6
1
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In addition to experimental studies, a computational approach was carried out to study the geometrical parameters, electron densities, and UV-Vis absorption spectra of sulfadiazine and SDCYS adduct in water. Calculated (B3LYP/6-311++G(d,p) level) and experimental UV-Vis absorption spectra of the compounds were found to be in good agreement in water. The computational study suggests that cysteine bound to the C(5) on the pyrimidine ring via SH-group nucleophilic attack.
27p
tudichquannguyet
29-11-2021
6
1
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This work introduces a new additive named 4,4’-trimethylenedipiperidine for the practical and ecofriendly preparation of ethyl 5-amino-7-(4-phenyl)-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate derivatives. This chemical is commercially available and easy to handle. It also possesses a low melting point and a broad liquid range temperature, high thermal stability, and good solubility in water. Based on green chemistry principles, the reaction was performed in a) a mixture of green solvents i.e.
12p
tudichquannguyet
29-11-2021
14
1
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Quinoline moiety is an important scaffold in the field of drug discovery and drug development, with a wide range of pharmacological activities. Quinoline derivatives are potent inhibitors for reverse transcriptase, which is responsible for the conversion of single-stranded viral RNA into double-stranded viral DNA.In the present study, we have designed and synthesized 2 series, namely pyrazoline and pyrimidine containing quinoline derivatives as non nucleoside reverse transcriptase inhibitors (NNRTIs).
46p
tudichquannguyet
29-11-2021
5
1
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A series of novel imidazo[1,2-a]pyrimidine containing tri/tetrasubstituted imidazole derivatives (1-10) has been synthesized via sequential two-step, one-pot, multicomponent reaction using imidazo[1,2-a]pyrimidine-2-carbaldehyde, benzil, primary amines, and ammonium acetate catalyzed by p-toluenesulfonic acid under microwave-assisted conditions. The results showed that target compounds can be obtained from a wide range of primary amines bearing different functional groups with moderate to good yields (46%-80%) under optimum reaction conditions.
34p
tudichquannguyet
29-11-2021
16
0
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Heterocyclic pyrimidine nucleus, which is an essential base component of the genetic material of deoxyribonucleic acid, demonstrated various biological activities. A series of bis-pyrimidine Schiff bases were synthesized and screened for its antimicrobial and anticancer potentials.
16p
vijiraiya2711
27-05-2020
14
1
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A series of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives 10(a–f), 12(a–c) and 14(a–c) were synthesized and characterized by FTIR, 1 H-NMR, mass spectral and elemental analysis.
11p
vijiraiya2711
27-05-2020
11
1
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Heterocyclic compounds offer a high degree of structural diversity and have proven to be broadly and economically useful as therapeutic agents. Comprehensive research on diverse therapeutic potentials of heterocycles compounds has confirmed their immense significance in the pathophysiology of diseases.
29p
vijiraiya2711
27-05-2020
11
1
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A series of thiazolopyrimidine derivatives have been synthesized via multicomponent reaction and tested for biological activities. This research aims to develop a new synthetic method of poly fused pyrimidines under microwave irradiation.
14p
vijiraiya2711
27-05-2020
8
1
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Chalcones are intent in the daily diet as a favorable chemotherapeutic compound; on the other hand thiophene moiety is present in a large number of bioactive molecules having diverse biological effciency.
8p
vijiraiya2711
27-05-2020
9
1
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