51746-85-1Relevant academic research and scientific papers
SUBSTITUTED IMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00322, (2021/04/01)
The invention provides substituted imidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
Synthesis and Antibacterial Activity of Novel 4″-O-desosaminyl clarithromycin derivatives with 11, 12-arylalkyl side chains
Zhao, Zhe-Hui,Zhu, Di,Zhang, Xiao-Xi,Luo, Zhi-Gang,Lei, Ping-Sheng
, p. 1 - 9 (2018/04/24)
A series of novel 4″-O-desosaminyl clarithromycin derivatives with 11, 12-arylalkyl side chains was synthesized by coupling 6-deoxy-desosamine donors (18, 19) with 4″-OH of compounds 5a–c. The activities of the target compounds were tested against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed activities against macrolide sensitive and resistant pathogens, and compounds 21d and 21e displayed significant improvement of activities against resistant pathogens.
PROCESSES FOR THE SYNTHESIS OF SUBSTITUTED UREA COMPOUNDS
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Page/Page column 32; 33, (2015/10/05)
The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, (Formula IIa) the process comprising the reaction of an imidazolyl intermediate of Formula IIa', with a carbamoyl halide of the formula: R1R2NC(=O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa' is prepared by oxidation of the derivative of R5 and R6, R6-C(=O)CH2R5 to form a glyoxal intermediate R6-C(=O)(C=O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa', and wherein the compound substituents are as defined herein.
A convenient synthesis of 4(5)-(hetero)aryl-1H-imidazoles via microwave-assisted Suzuki-Miyaura cross-coupling reaction
Vichier-Guerre, Sophie,Dugué, Laurence,Pochet, Sylvie
supporting information, p. 6347 - 6350 (2014/12/10)
A simple and rapid access to a variety of 4(5)-arylated imidazoles via palladium-catalyzed Suzuki-Miyaura cross-coupling reaction is described. Coupling parameters were screened for efficient C-4 arylation of N-unprotected 4-iodoimidazole with a broad range of boronic acids under microwave irradiation. Twenty-one imidazole derivatives were synthesized in modest to excellent yields in short reaction times.
One-pot synthesis of 2-alkyl-4(5)-aryl-1H-imidazoles from 1-aryl-2-bromoethanones, ammonium carbonate and aliphatic carboxylic acids
Liu, Cong,Nie, Yijiao,Yao, Guowei,Dai, Rongji,Deng, Yulin
, p. 208 - 210 (2014/05/06)
A simple and efficient protocol for the preparation of 2-alkyl-4(5)-aryl- 1H-imidazoles starting from α-bromo aryl methyl ketones and aliphatic carboxylic acids in the presence of ammonium carbonate has been developed.
PROCESS FOR THE SYNTHESIS OF SUBSTITUTED UREA COMPOUNDS
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, (2014/02/16)
A process for preparing a substituted urea compound of Formula II or Formula I, or a pharmaceutically acceptable salt or ester thereof, Formula II, Formula I the process comprising the reaction of an intermediate of Formula II' or Formula 1', Formula II',
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase
Kumar, Sanjeev,Jaller, Daniel,Patel, Bhumika,LaLonde, Judith M.,DuHadaway, James B.,Malachowski, William P.,Prendergast, George C.,Muller, Alexander J.
experimental part, p. 4968 - 4977 (2009/07/11)
Indoleamine 2,3-dioxygenase (IDO) is emerging as an important new therapeutic target for the treatment of cancer, chronic viral infections, and other diseases characterized by pathological immune suppression. With the goal of developing more potent IDO in
A new boronic-acid based strategy to synthesize 4(5)-(het)aryl-1H-imidazoles
Primas, Nicolas,Mahatsekake, Clément,Bouillon, Alexandre,Lancelot, Jean-Charles,Oliveira Santos, Jana Sopkovà-de,Lohier, Jean-Fran?ois,Rault, Sylvain
, p. 4596 - 4601 (2008/09/20)
This paper describes the synthesis of a new N-THP protected 5-(1H)-imidazolyl boronic acid pinacol ester and its use in Suzuki cross-coupling reactions with a wide range of (het)aryl halides to provide 4(5)-(het)aryl-1H-imidazoles.
NOVEL OXAZOLIDINONE COMPOUNDS AS ANTIINFECTIVE AGENTS
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Page/Page column 81, (2009/01/20)
The present invention relates to novel oxazolidinone compounds of formula (I) with antibacterial activity, their pharmaceutically acceptable salts, their stereoisomers, their prodrugs, pharmaceutical compositions comprising the same and to their use as therapeutic agents
5-Substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6
Denton, Travis T.,Zhang, Xiaodong,Cashman, John R.
, p. 224 - 239 (2007/10/03)
A series of 5- and 6-substituted and unsubstituted 3-heteroaromatic analogues of nicotine were synthesized in an effort to delineate the structural requirements for selectively inhibiting human cytochrome P-450 (CYP) 2A6, the major nicotine metabolizing enzyme. Thiophene, substituted thiophene, furan, substituted furan, imidazole, substituted imidazole, pyridine, substituted pyridine, thiazole, and quinoline moieties were used to replace the N-methylpyrrolidine ring of nicotine. Bromo and methyl groups were introduced at the 5-position of the pyridine ring and fluoro, chloro, and methoxy groups were placed at the 6-position of the pyridine ring in order to explore the structure-activity relationship (SAR) of inhibition of CYP2A6. The inhibitory activity of the most potent CYP2A6 inhibitors on the functional activity of human cytochrome P450s 3A4, 2E1, 2B6, 2C9, 2C19, and 2D6 was also examined to determine inhibitor selectivity. We identified 36 compounds that were more potent than nicotine at inhibition of coumarin 7-hydroxylase (CYP2A6) activity. We also found a number of compounds to be highly selective for the inhibition of human CYP2A6 versus the other human CYPs examined.
