- A green approach for the synthesis of benzazolyl pyrimidinyl carbamothioates under ultrasonication and their antimicrobial activity
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A library of benzazolyl pyrimidinyl carbamothioates were prepared by the reaction of benzazolyl carbonothioates with pyrimidinyl-2-amine in the presence of an ionic liquid- 1-butyl-3-methylimidazolium hydroxide ([bmim]OH) under ultrasonication at a frequency of 35?kHz and tested for antimicrobial activity. Chloro- and nitro-substituted benzothiazolyl/benzimidazolyl pyrimidinyl carbamothioates displayed prominent antibacterial activity against Bacillus subtilis, while nitro-substituted benzothiazolyl/benzimidazolyl pyrimidinyl carbamothioates showed excellent antifungal activity against Aspergilus niger. Graphic abstract: [Figure not available: see fulltext.].
- Kayathi, Narendra Babu,Panga, Siva Sankar,Adivireddy, Padmaja,Venkatapuram, Padmavathi
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p. 2931 - 2943
(2021/07/26)
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- Photocatalytic synthesis of 2-amino-4,6-diarylpyrimidines using nanoTiO2
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Photocatalytic synthesis of 2-amino-4,6-diarylpyrimidines was carried out by using nano TiO2. The method follows a green route by avoiding the use of toxic organic solvents and tedious experimental conditions. Compared with conventional methods the present strategy offers excellent yield under UV irradiation for a period of 20 min in ethanolic medium. Only a small quantity of nanocatalyst (1 mol%) is sufficient to achieve the completion of the reaction. The nanocatalyst can be reused up to four reaction cycles without much loss in the activity.
- E. P., Aparna,K. S., Devaky,Mathew, Divya,N, Rakesh,Thomas, Ashly
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- Iron Catalyzed Synthesis of Pyrimidines Under Air
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Herein we report an iron-catalyzed multicomponent dehydrogenative functionalization of alcohols to pyrimidines under atmospheric conditions. Using a well-defined Fe(II)-complex featuring redox noninnocent 2-phenylazo-(1,10-phenanthroline) ligand, as a cat
- Mondal, Rakesh,Sinha, Suman,Das, Siuli,Chakraborty, Gargi,Paul, Nanda D.
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supporting information
p. 594 - 600
(2019/12/15)
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- Ultrasound-mediated synthesis, biological evaluation, docking and in vivo acute oral toxicity study of novel indolin-2-one coupled pyrimidine derivatives
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The work reports ultrasound-mediated greener synthesis of 11 novel 3-(4-(4-chlorophenyl)-6-(substituted phenyl/heteryl)pyrimidin-2-ylimino)indolin-2-one (7a–7k) derivatives. The synthesized derivatives were evaluated for their in vitro anticancer activity against a panel of selected human cancer cell lines of breast (MCF-7), cervix (HeLa), prostate (PC-3) and lung (A-549). Among the tested compounds, 7b exhibited most promising in vitro anticancer activity against HeLa, PC-3 and A-549 with GI50 value 15.38, 19.67 and 4.37?μM, respectively. The compounds (7a–7k) were also screened for induction of apoptosis and morphological changes in cancer cells at their GI50 concentration. The treatment of HeLa, PC-3 and A549 cancer cells with 7b and treatment of MCF-7 cancer cells with 7h showed apoptosis and morphological changes such as cell shrinkage, cell wall deformation and reduced number of viable cells. The compound 7b has shown almost 5.00 times more selectivity for PC-3 cancer cell lines in comparison to the RWPE-1 normal prostate epithelial cells. Molecular docking study has been carried out, which replicates results of biological activity in cases of initial hits 7b, 7c and 7d, suggesting that these compounds have a potential to become lead molecules in the drug discovery process. In silico ADMET study was performed for predicting pharmacokinetic properties and toxicity profile of the synthesized compounds and expressed good oral drug-like behaviour. An in vivo acute oral toxicity study was performed using Swiss albino mice for the most active compounds 7b and 7c, and results indicate that the compounds are non-toxic in nature.
- Nikalje, Anna Pratima G.,Tiwari, Shailee V.,Sangshetti, Jaiprakash N.,Damale, Manoj D.
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p. 3031 - 3059
(2018/02/06)
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- Synthesis of Benzazolyl Pyrimidines Under Ultrasonication and Their Antimicrobial Activity
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(1) The benzoxazolyl/benzothiazolyl/benzimidazolyl pyrimidines were prepared under ultrasonication in the presence of pyridine/dimethylaminopyridine and triethylamine. (2) Better yields were recorded in 4-(N,N-dimethylamino)pyridine and Et3N. (3) The presence of electron withdrawing chloro, bromo, and nitro substituents enhanced antimicrobial activity (13c, 13e, 14e: minimum inhibitory concentration?=?6.25?μg/well against Bacillus subtilis; 13e, 14e: minimum inhibitory concentration?=?6.25?μg/well against Aspergillus niger).
- Kayathi, Narendra Babu,Sowmya, Donthamsetty V.,Adivireddy, Padmaja,Venkatapuram, Padmavathi
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p. 1024 - 1032
(2018/02/21)
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- Synthesis and Antimicrobial Activity of Azolyl Pyrimidines
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A new class of azolyl pyrimidines linked by diamino sulfone moiety was prepared and studied their antimicrobial activity. Chloro-substituted and nitro-substituted thiazolyl pyrimidines (9c and 9e) showed excellent antibacterial activity against Bacillus subtilis, while imidazolyl pyrimidines (10c and 10e) exhibited promising antifungal activity against Aspergillus niger.
- Butta, Ragavendra,Donthamsetty V, Sowmya,Adivireddy, Padmaja,Venkatapuram, Padmavathi
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p. 524 - 530
(2017/02/03)
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- Synthesis, characterization of 4,6-disubstituted aminopyrimidines and their sulphonamide derivatives as anti-Amoebic agents
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The present study describes the synthesis and anti-Amoebic activity of 4,6-disubstituted aminopyrimidines (1b-10b) and their sulphonamide derivatives (1-20). All the desired compounds were characterized by spectral data and their purity was confirmed by e
- Siddiqui, Shadab Miyan,Azam, Amir
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p. 2976 - 2984
(2014/05/06)
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- Synthesis and evaluation of some novel [1,2,4]triazolo[1,5-α] pyrimidine derivatives for anticancer activity
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A series of 7-(4-chlorophenyl)-2-phenyl-1,7-dihydro [1,2,4] triazolo [1,5α] pyrimidine 4a-l have been synthesized and evaluated for anticancer activity. The newly synthesized compounds have been characterized by IR, 1H NMR and elemental analyse
- Pattan, Shashikant,Hole, Mangesh,Pattan, Jayshri,Dengale, Santosh,Shinde, Hemlata,Muluk, Rekha,Nirmal, Sunil,Jadhav, Ravindra
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experimental part
p. 774 - 779
(2012/07/03)
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- Synthesis of 2-amino-4,6-diarylpyrimidines using inorganic solid support under microwave and ultrasound irradiation and their antibacterial activity
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An expeditious method for the exclusive one-pot synthesis of 2-amino-4,6-diarylpyrimidines (3a-i) is described by the condensation of variously substituted chalcones (1a-i) with guanidine nitrate using inorganic solid support under microwave or ultrasound
- Chpudhary, Prakash C.,Sharma, Hari Om,Punjabi, Pinki B.,Verma
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p. 209 - 212
(2013/09/24)
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- Anti-bacterial and anti-leishmanial studies of 4, 6-diarylpyrimidin-2- amines
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Seven new chalcones along with nine already reported ones were synthesized from aryl aldehydes and substituted acetophenones by Claisen-Schmidt condensation. Each chalcone was treated with guanidine hydrochloride followed by oxidation with H2O
- Bukhari, Mujahid Hussain,Siddiqui, Hamid Latif,Ashraf, Chaudhary Muhammad,Hussain, Tanvir
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p. 720 - 725
(2012/06/18)
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- Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists
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Two regioisomeric series of diaryl 2- or 4-amidopyrimidines have been synthesized and their adenosine receptor affinities were determined in radioligand binding assays at the four human adenosine receptors (hARs). Some of the ligands prepared herein exhib
- Yaziji, Vicente,Rodríguez, David,Gutiérrez-De-Terán, Hugo,Coelho, Alberto,Caama?o, Olga,García-Mera, Xerardo,Brea, José,Loza, María Isabel,Cadavid, María Isabel,Sotelo, Eddy
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supporting information; experimental part
p. 457 - 471
(2011/04/15)
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- Synthesis and characterization of some new 2-amino-4-(4′-substituted) -6-(4″-substituted)diphenyl pyrimidines
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Synthesis and characterization of some novel 2-amino-4-(4′- substituted)-6-(4″-substituted)diphenyl pyrimidines has been carried out by the conversion of variably substituted acetophenones and benzaldehydes into corresponding chalcones followed by cyclization with guanidine hydrochloride in the presence of an oxidizing agent.
- Hasan, Aurangzeb,Khaleeq, Musfirah,Riaz, Uzma
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p. 5581 - 5587
(2012/08/07)
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- Efficient and facile three-component reaction for the synthesis of 2-amine-4,6-diarylpyrimidine under solvent-free conditions
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An efficient and convenient multicomponent reaction for the preparation of 2-amine-4,6-diarylpyrimidine by aromatic aldehydes, aromatic ketones, and guanidine carbonate in the presence of sodium hydroxide under solvent-free conditions is reported. The sho
- Zhuang, Qiya,Han, HongXia,Wang, Suhui,Tu, Shuajiang,Rong, Liangce
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experimental part
p. 516 - 522
(2009/06/20)
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