97693-26-0Relevant academic research and scientific papers
Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives
Fargualy, Ahmed M.,Habib, Nargues S.,Ismail, Khadiga A.,Hassan, Ahmed M. M.,Sarg, Marwa T. M.
, p. 276 - 295 (2013/10/01)
Some novel pyrimidine-5-carbonitrile derivatives bearing various substituent have been synthesized. The structures of target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tumor cell lines. Five representative active anticancer compounds 6a, 6c, 6d, 17a and 18a were subjected to docking using MOE program on the 3D structure of two enzymes, namely; thymidylate synthase and dihydrofolate reductase. The antimicrobial activities of the synthesized compounds were tested against Staphylococcus aureus, Pseudomonas aeruginosa, Shigella flexneri and Candida albicans. Compounds 2c, 7a and 9c showed broad spectrum antimicrobial activity.
Synthesis of some dihydropyrimidine-based compounds bearing pyrazoline moiety and evaluation of their antiproliferative activity
Awadallah, Fadi M.,Piazza, Gary A.,Gary, Bernard D.,Keeton, Adam B.,Canzoneri, Joshua C.
, p. 273 - 279 (2013/11/19)
Two series of 2-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-1-methyl-6-oxo-4- phenyl-1,6-dihydropyrimidine-5-carbonitriles 5a-h and 4-(4-chlorophenyl)-2-(3,5- diaryl-4,5-dihydropyrazol-1-yl)-1-methyl-6-oxo-1,6-dihydropyrimidine-5- carbonitriles 6a-h were synthesized via a cyclocondensation reaction of the corresponding 2-hydrazinopyrimidines 3a,b with the appropriate 2-propen-1-ones 4a-h. The target compounds were screened for their antiproliferative activity against A 549 (lung), HT 29 (colon), MCF 7 and MDA-MB 231 (breast) cell lines. The two most susceptible cell lines were the colon (HT 29) and breast (MDA-MB 231). Generally, the 4-unsubstitutedphenylpyrimidine derivatives 5a-h were more active than their 4-chlorophenylpyrimidine analogs 6a-h. Compounds 5e and 5g, showed high activity against three of the cell lines. The most active compound 5c possessed IC50 = 1.76 μM against A 549 cell line.
Reaction of pyrimidinonethione derivatives: Synthesis of N-methyl-2-hydrizinopyrimidine-4-one, thiazolo[3,4-b] N-methylpyrimidinone; 2-(1-pyrazolonyl) N-methylpyrimidine-4-one and 2-hydrazino-N-methyl pyrimidine-4-one derivatives
Al-Shara'ey, Abdullah A. Al-Karim
, p. 547 - 552 (2007/10/03)
6-Aryl-5-cyano-4-pyrimidinone-2-thion derivatives 1a-c reacted with methyl iodide (1:2) to give the corresponding 2-S,N-dimethyl pyrimidine-4-one derivatives 2a-c. Compounds 2a-c were in turn, reacted with hydrazine hydrate to give the sulfur free reaction products 3a-c. These reaction products were taken as the starting materials for the synthesis of several new heterocyclic derivatives. Reaction of 3a-c with acetic anhydride and formic acid gave pyrimido triazines 4a-c and 7a-c, respectively. Their reactions with active methylene containing reagents gave the corresponding 2-(1-pyrazonyl)-N-methyl pyrimidine derivatives 9a-c and 10a-c, respectively. Their reactions with aromatic aldehydes afforded the corresponding 2-hydrazono pyrimidine derivatives 11a-c. The structure of these reactions products were established based on both elemental analysis and spectral data studies.
Synthesis and biological evaluation of some new 3,4-dihydropyrimidin-4-ones
Modha, Jayesh,Datta, Neela,Parekh, Hansa
, p. 641 - 646 (2007/10/03)
Condensation of 5-cyano-2-hydrazino-3-N-methyl-6-phenyl/p-chlorophenyl-3,4-dihydropyrimidin-4 -one (3a and 3b) with 2,4-bisalkyl/arylamino-6-chloro-s-triazine (4) gave the corresponding 2,4-bisalkyl/arylamino-6-[5′-cyano-3′-N-methyl]-6′-phenyl/p -chlorophenyl-3′,4′-dihydropyrimidin-4′-one-2′-yl-hyd razino-s-triazines (5a-n and 6a-n). The compounds 4 have been prepared by the condensation of cyanuric chloride and different alkyl/aryl amines. The reaction between 5-cyano-3-N-methyl-2-methylthio-6-phenyl/p-chlorophenyl-3,4-dihydropyrimidin- 4-one (2a and 2b) with hydrazine hydrate furnished 3a and 3b, respectively. The condensation of 6-phenyl/p-chlorophenyl/5-cyano-2-mercapto-3,4-dihydropyrimidin-4-one (1a and 1b) with methyl iodide yielded 2a and 2b, respectively. All the products have been evaluated in vitro for their antimicrobial activity against several microbes and antitubercular activity against Mycobacterium tuberculosis H37 Rv. Copyright
A One-Step Synthesis of 2-Methylthio-6-oxopyrimidine Derivatives: Preparation of Fused Pyrimidinones
Hussain, S. M.,El-Barbary, A. A.,Mansour, S. A.
, p. 169 - 171 (2007/10/02)
Condensation of a ternary mixture of ethyl cyanoacetate, S-methylisothiourea and aromatic aldehydes in pyridine afforded directly the 4-aryl-5-cyano-6-oxopyrimidines IV in good yields.Alkylation of IV with alkyl halides in alkaline medium yielded the 1-al
