The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Alakananda Hajra - One of the best experts on this subject based on the ideXlab platform.
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visible light organic photoredox catalyzed c h alkoxylation of Imidazopyridine with alcohol
Journal of Organic Chemistry, 2017Co-Authors: Golam Kibriya, Sadhanendu Samanta, Sourav Jana, Susmita Mondal, Alakananda HajraAbstract:The visible light-mediated C-3 alkoxylation of Imidazopyridines with alcohols has been achieved using rose bengal as an organic photoredox catalyst at room temperature. Widely abundant air acts as the terminal oxidant that avoids the use of a stoichiometric amount of peroxo compounds. A wide range of functional groups could be tolerated under the reaction conditions to produce C(sp2)–H alkoxylated products in high yields.
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diacetoxy iodobenzene mediated oxidative c h amination of Imidazopyridines at ambient temperature
Journal of Organic Chemistry, 2017Co-Authors: Susmita Mondal, Sadhanendu Samanta, Sourav Jana, Alakananda HajraAbstract:(Diacetoxy)iodobenzene (PIDA)-mediated direct oxidative C–H amination for the synthesis of 3-amino substituted Imidazopyridines has been achieved under metal-free conditions at room temperature in short reaction times. This methodology is also applicable for the regioselective amination of indolizines. Experimental results suggest that the reaction likely proceeds through a radical pathway.
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(Diacetoxy)iodobenzene-Mediated Oxidative C–H Amination of Imidazopyridines at Ambient Temperature
2017Co-Authors: Susmita Mondal, Sadhanendu Samanta, Sourav Jana, Alakananda HajraAbstract:(Diacetoxy)iodobenzene (PIDA)-mediated direct oxidative C–H amination for the synthesis of 3-amino substituted Imidazopyridines has been achieved under metal-free conditions at room temperature in short reaction times. This methodology is also applicable for the regioselective amination of indolizines. Experimental results suggest that the reaction likely proceeds through a radical pathway
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Visible Light Organic Photoredox-Catalyzed C–H Alkoxylation of Imidazopyridine with Alcohol
2017Co-Authors: Golam Kibriya, Sadhanendu Samanta, Sourav Jana, Susmita Mondal, Alakananda HajraAbstract:The visible light-mediated C-3 alkoxylation of Imidazopyridines with alcohols has been achieved using rose bengal as an organic photoredox catalyst at room temperature. Widely abundant air acts as the terminal oxidant that avoids the use of a stoichiometric amount of peroxo compounds. A wide range of functional groups could be tolerated under the reaction conditions to produce C(sp2)–H alkoxylated products in high yields
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Regioselective synthesis of nitrosoimidazoheterocycles using tert-butyl nitrite
Organic & biomolecular chemistry, 2015Co-Authors: Kamarul Monir, Sourav Jana, Monoranjan Ghosh, Pallab Mondal, Adinath Majee, Alakananda HajraAbstract:A simple and practical method has been developed for the regioselective nitrosylation of Imidazopyridines via C(sp2)–H bond functionalization using tert-butyl nitrite under mild reaction conditions in a short time. A library of 3-nitrosoImidazopyridines with broad functionalities was synthesized in near quantitative yields. The present protocol is also applicable to imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole.
Steven B Coffey - One of the best experts on this subject based on the ideXlab platform.
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route selection and optimization in the synthesis of two Imidazopyridine inhibitors of dgat 2
Organic Process Research & Development, 2018Co-Authors: Scott Bader, Gary E Aspnes, Jianwei Bian, Steven B Coffey, Shawn Cabral, Qifang Li, Matthew S. Dowling, Michael Herr, Dilinie P Fernando, Wenhua JiaoAbstract:The scalable syntheses of two Imidazopyridine inhibitors of the enzyme diacylglycerol acyltransferase 2 (DGAT-2) are described. 6-Chloro-3-nitro-2-aminopyridine was the starting material for the convergent synthesis of the central Imidazopyridine ring. Differentiation in reactivity of the C2- and C3-nitrogen substituents on the pyridine ring and the development of mild cyclodehydration conditions to form the imidazole ring were critical problems that were addressed to deliver a 3-kg batch of compound 1 (PF-06424439) and a 0.1-kg batch of compound 2 (PF-06450561).
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discovery and optimization of Imidazopyridine based inhibitors of diacylglycerol acyltransferase 2 dgat2
Journal of Medicinal Chemistry, 2015Co-Authors: Kentaro Futatsugi, Gary E Aspnes, Scott Bader, Jianwei Bian, Philip A. Carpino, Shawn Cabral, Daniel W Kung, David Hepworth, Markus Boehm, Steven B CoffeyAbstract:The medicinal chemistry and preclinical biology of Imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2) is described. A screening hit 1 with low lipophilic efficiency (LipE) was optimized through two key structural modifications: (1) identification of the pyrrolidine amide group for a significant LipE improvement, and (2) insertion of a sp3-hybridized carbon center in the core of the molecule for simultaneous improvement of N-glucuronidation metabolic liability and off-target pharmacology. The preclinical candidate 9 (PF-06424439) demonstrated excellent ADMET properties and decreased circulating and hepatic lipids when orally administered to dyslipidemic rodent models.
Sourav Jana - One of the best experts on this subject based on the ideXlab platform.
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visible light organic photoredox catalyzed c h alkoxylation of Imidazopyridine with alcohol
Journal of Organic Chemistry, 2017Co-Authors: Golam Kibriya, Sadhanendu Samanta, Sourav Jana, Susmita Mondal, Alakananda HajraAbstract:The visible light-mediated C-3 alkoxylation of Imidazopyridines with alcohols has been achieved using rose bengal as an organic photoredox catalyst at room temperature. Widely abundant air acts as the terminal oxidant that avoids the use of a stoichiometric amount of peroxo compounds. A wide range of functional groups could be tolerated under the reaction conditions to produce C(sp2)–H alkoxylated products in high yields.
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diacetoxy iodobenzene mediated oxidative c h amination of Imidazopyridines at ambient temperature
Journal of Organic Chemistry, 2017Co-Authors: Susmita Mondal, Sadhanendu Samanta, Sourav Jana, Alakananda HajraAbstract:(Diacetoxy)iodobenzene (PIDA)-mediated direct oxidative C–H amination for the synthesis of 3-amino substituted Imidazopyridines has been achieved under metal-free conditions at room temperature in short reaction times. This methodology is also applicable for the regioselective amination of indolizines. Experimental results suggest that the reaction likely proceeds through a radical pathway.
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(Diacetoxy)iodobenzene-Mediated Oxidative C–H Amination of Imidazopyridines at Ambient Temperature
2017Co-Authors: Susmita Mondal, Sadhanendu Samanta, Sourav Jana, Alakananda HajraAbstract:(Diacetoxy)iodobenzene (PIDA)-mediated direct oxidative C–H amination for the synthesis of 3-amino substituted Imidazopyridines has been achieved under metal-free conditions at room temperature in short reaction times. This methodology is also applicable for the regioselective amination of indolizines. Experimental results suggest that the reaction likely proceeds through a radical pathway
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Visible Light Organic Photoredox-Catalyzed C–H Alkoxylation of Imidazopyridine with Alcohol
2017Co-Authors: Golam Kibriya, Sadhanendu Samanta, Sourav Jana, Susmita Mondal, Alakananda HajraAbstract:The visible light-mediated C-3 alkoxylation of Imidazopyridines with alcohols has been achieved using rose bengal as an organic photoredox catalyst at room temperature. Widely abundant air acts as the terminal oxidant that avoids the use of a stoichiometric amount of peroxo compounds. A wide range of functional groups could be tolerated under the reaction conditions to produce C(sp2)–H alkoxylated products in high yields
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Regioselective synthesis of nitrosoimidazoheterocycles using tert-butyl nitrite
Organic & biomolecular chemistry, 2015Co-Authors: Kamarul Monir, Sourav Jana, Monoranjan Ghosh, Pallab Mondal, Adinath Majee, Alakananda HajraAbstract:A simple and practical method has been developed for the regioselective nitrosylation of Imidazopyridines via C(sp2)–H bond functionalization using tert-butyl nitrite under mild reaction conditions in a short time. A library of 3-nitrosoImidazopyridines with broad functionalities was synthesized in near quantitative yields. The present protocol is also applicable to imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole.
Guang Liang - One of the best experts on this subject based on the ideXlab platform.
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Inhibition of inflammation and oxidative stress by an Imidazopyridine derivative X22 prevents heart injury from obesity.
Journal of cellular and molecular medicine, 2016Co-Authors: Yuanyuan Qian, Gaozhi Chen, Yali Zhang, Peng Zhong, Kesong Peng, Xuemei Chen, Guang LiangAbstract:Inflammation and oxidative stress plays an important role in the development of obesity-related complications and cardiovascular disease. Benzimidazole and Imidazopyridine compounds are a class of compounds with a variety of activities, including anti-inflammatory, antioxidant and anti-cancer. X22 is an Imidazopyridine derivative we synthesized and evaluated previously for anti-inflammatory activity in lipopolysaccharide-stimulated macrophages. However, its ability to alleviate obesity-induced heart injury via its anti-inflammatory actions was unclear. This study was designed to evaluate the cardioprotective effects of X22 using cell culture studies and a high-fat diet rat model. We observed that palmitic acid treatment in cardiac-derived H9c2 cells induced a significant increase in reactive oxygen species, inflammation, apoptosis, fibrosis and hypertrophy. All of these changes were inhibited by treatment with X22. Furthermore, oral administration of X22 suppressed high-fat diet-induced oxidative stress, inflammation, apoptosis, hypertrophy and fibrosis in rat heart tissues and decreased serum lipid concentration. We also found that the anti-inflammatory and anti-oxidative actions of X22 were associated with Nrf2 activation and nuclear factor-kappaB (NF-κB) inhibition, respectively, both in vitro and in vivo. The results of this study indicate that X22 may be a promising cardioprotective agent and that Nrf2 and NF-κB may be important therapeutic targets for obesity-related complications.
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Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives
2013Co-Authors: Gaozhi Chen, Zhiguo Liu, Xiaoou Shan, Lili Jiang, Yunjie Zhao, Zhiguo Feng, Shulin Yang, Yali Zhang, Guang LiangAbstract:Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and Imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the Imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds X10, X12, X13, X14, and X15 inhibited TNF-α and IL-6 release in a dose-dependent manner, and X12 showed no cytotoxicity in hepatic cells. Furthermore, X12 exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new Imidazopyridines with potential therapeutic effects in acute inflammatory diseases
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Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives
ACS Medicinal Chemistry Letters, 2012Co-Authors: Gaozhi Chen, Zhiguo Liu, Zhang Yali, Xiaoou Shan, Lili Jiang, Yunjie Zhao, Zhiguo Feng, Shulin Yang, Guang LiangAbstract:Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and Imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the Imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds X10, X12, X13, X14, and X15 inhibited TNF-α and IL-6 release in a dose-dependent manner, and X12 showed no cytotoxicity in hepatic cells. Furthermore, X12 exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new Imidazopyridines with potential therapeutic effects in acute inflammatory diseases.
Susmita Mondal - One of the best experts on this subject based on the ideXlab platform.
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visible light organic photoredox catalyzed c h alkoxylation of Imidazopyridine with alcohol
Journal of Organic Chemistry, 2017Co-Authors: Golam Kibriya, Sadhanendu Samanta, Sourav Jana, Susmita Mondal, Alakananda HajraAbstract:The visible light-mediated C-3 alkoxylation of Imidazopyridines with alcohols has been achieved using rose bengal as an organic photoredox catalyst at room temperature. Widely abundant air acts as the terminal oxidant that avoids the use of a stoichiometric amount of peroxo compounds. A wide range of functional groups could be tolerated under the reaction conditions to produce C(sp2)–H alkoxylated products in high yields.
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diacetoxy iodobenzene mediated oxidative c h amination of Imidazopyridines at ambient temperature
Journal of Organic Chemistry, 2017Co-Authors: Susmita Mondal, Sadhanendu Samanta, Sourav Jana, Alakananda HajraAbstract:(Diacetoxy)iodobenzene (PIDA)-mediated direct oxidative C–H amination for the synthesis of 3-amino substituted Imidazopyridines has been achieved under metal-free conditions at room temperature in short reaction times. This methodology is also applicable for the regioselective amination of indolizines. Experimental results suggest that the reaction likely proceeds through a radical pathway.
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(Diacetoxy)iodobenzene-Mediated Oxidative C–H Amination of Imidazopyridines at Ambient Temperature
2017Co-Authors: Susmita Mondal, Sadhanendu Samanta, Sourav Jana, Alakananda HajraAbstract:(Diacetoxy)iodobenzene (PIDA)-mediated direct oxidative C–H amination for the synthesis of 3-amino substituted Imidazopyridines has been achieved under metal-free conditions at room temperature in short reaction times. This methodology is also applicable for the regioselective amination of indolizines. Experimental results suggest that the reaction likely proceeds through a radical pathway
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Visible Light Organic Photoredox-Catalyzed C–H Alkoxylation of Imidazopyridine with Alcohol
2017Co-Authors: Golam Kibriya, Sadhanendu Samanta, Sourav Jana, Susmita Mondal, Alakananda HajraAbstract:The visible light-mediated C-3 alkoxylation of Imidazopyridines with alcohols has been achieved using rose bengal as an organic photoredox catalyst at room temperature. Widely abundant air acts as the terminal oxidant that avoids the use of a stoichiometric amount of peroxo compounds. A wide range of functional groups could be tolerated under the reaction conditions to produce C(sp2)–H alkoxylated products in high yields