- MRGX Receptor Antagonists
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The invention relates to a method for preventing or treating a disease or disorder that is associated with the MrgX2 receptor. The invention also relates to MrgX2 antagonists and physiologically acceptable salts thereof. The invention also relates to pharmaceutical compositions and dosage forms comprising an MrgX2 antagonist.
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Paragraph 0299; 0306; 0307
(2021/05/07)
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- Copper-Catalyzed Domino Synthesis of Benzo[4,5]imidazo[1,2-a]pyrimidin-4(10H)-ones using Cyanamide as a Building Block
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An efficient and practical copper-catalyzed domino synthesis of benzo[4,5]imidazo[1,2-a]pyrimidin-4(10H)-ones has been developed. The protocol uses N-(2-halophenyl)-3-alkylpropiolamides and cyanamide as the starting materials, inexpensive copper(I) iodide and pipecolinic acid as the catalyst and ligand, and the corresponding products were obtained in moderate to good yields.
- Lou, Zhenbang,Wu, Xudong,Yang, Haijun,Zhu, Changjin,Fu, Hua
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p. 3961 - 3968
(2016/01/25)
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- Microwave assisted synthesis of dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4- ones; Synthesis, in vitro antimicrobial and anticancer activities of novel coumarin substituted dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-ones
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The present article describes the synthesis of dihydrobenzo[4,5]imidazo[1, 2-a]pyrimidin-4-one (2a-h) under microwave irradiation. The product was obtained in excellent yield (74-94%) in a shorter reaction time (2 min). These molecules (2a, b) further reacted with various substituted 4-bromomethylcoumarins (3a-f) to yield a new series of coumarin substituted dihydrobenzo[4,5]imidazo[1,2-a] pyrimidin-4-ones (4a-h). The structure of all the synthesized compounds were confirmed by spectral studies and screened for their in vitro antibacterial activity against three Gram-positive bacteria viz., Staphylococcus aureus, Enterococcus faecalis, Streptococcus mutans and three Gram-negative bacteria viz., Escherichia coli, Klebsiella pneumonia, Pseudomonas aeruginosa and antifungal activity against Candida albicans, Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus, Fusarium oxysporum, Penicilliumchrysogenum and anticancer activity against Dalton's Ascitic Lymphoma (DAL) cell line. In general, all the compounds possessed better antifungal properties than antibacterial properties. The coumarin substituted dihydrobenzo[4,5]imidazo[1,2- a]pyrimidin-4-one (4g) (R = i-Pr, R1 = 6-Cl) was found to be the most potent cytotoxic compound (88%) against Dalton's Ascitic Lymphoma cell line at the concentration of 100 μg/mL.
- Puttaraju, Kallimeledoddi B.,Shivashankar, Kalegowda,Chandra,Mahendra,Rasal, Vijaykumar P.,Venkata Vivek, Ponnuru N.,Rai, Khushboo,Chanu, Maibam Beebina
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p. 316 - 322
(2013/10/08)
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- Studies on Ketene and Its Derivatives. CXXII. Reaction of Haloketenes with 1,3-Diaza-1,3-diene Compounds
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The reaction of haloketenes with 1,3-diaza-1,3-diene compounds, prepared by condensation of 2-amino-heterocycles with aromatic aldehydes, gave the cycloadducts, fused pyrimidones (6-17).However haloketenes underwent the cycloaddition with 2-(p-anisy
- Niwa, Ryuji,Katagiri, Nobuya,Kato, Tetsuzo
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p. 4149 - 4153
(2007/10/02)
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