The Experts below are selected from a list of 261 Experts worldwide ranked by ideXlab platform
Sunil N. Chavan - One of the best experts on this subject based on the ideXlab platform.
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Substituent Effect on Absorption and Fluorescence Properties of Thieno[3, 2-c]Pyridine Derivatives
Journal of Fluorescence, 2017Co-Authors: Sunil N. Chavan, Raghunath B. Toche, Satish M. ChavanAbstract:New substituted thieno[3,2- c ]pyridine derivatives 5 were synthesized by the reaction of 3-bromo-4-chlorothieno[3,2- c ]pyridine 1 with Cyclic Amine 2, which further on Suzuki reaction with boronic acids 4 converted to corresponding 3-arylthieno[3,2- c ]pyridine 5 . Substituent R^3 has predominant effect on fluorescence properties of thienopyridines. However, the electron donor Amine at C_4 has no effect on fluorescence properties of thienopyridines. Graphical Abstract New thieno[3,2-c]pyridine derivatives were synthesized from 3-bromo-4-chlorothieno[3,2-c]pyridine and Cyclic Amines, which by on Suzuki reaction with boronic acids converted to corresponding 3-arylthieno[3,2-c]pyridine. Substituent R3 has predominant effect on fluorescence properties of thienopyridines. However, the electron donor Amine at C4 has no effect on fluorescence properties of thienopyridines
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Synthesis and Study the Effect of Donor-Acceptor Substituent on Fluorescence Behavior of Thieno[3, 2-c]pyridine Derivatives
Journal of Fluorescence, 2014Co-Authors: Raghunath B. Toche, Sunil N. ChavanAbstract:4-Hetero-1-yl-2-bromothieno[3,2-c]pyridines 3(a–d) were synthesized by the reaction of 2-bromo-4-chlorothieno[3,2-c]pyridine (1) and Cyclic Amine 2(a–d) , which on Suzuki coupling with substituted boronic acids 4(a–f) exclusively converted to corresponding 4-hetero -1-yl-2-arylthieno [3,2-c] pyridine 5(a–x) in good yields. The effect of donor-acceptor substituent on absorption emission properties and fluorescent quantum yield of new thienopyridine derivatives 5(a-x) were studied.
Raghunath B. Toche - One of the best experts on this subject based on the ideXlab platform.
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Substituent Effect on Absorption and Fluorescence Properties of Thieno[3, 2-c]Pyridine Derivatives
Journal of Fluorescence, 2017Co-Authors: Sunil N. Chavan, Raghunath B. Toche, Satish M. ChavanAbstract:New substituted thieno[3,2- c ]pyridine derivatives 5 were synthesized by the reaction of 3-bromo-4-chlorothieno[3,2- c ]pyridine 1 with Cyclic Amine 2, which further on Suzuki reaction with boronic acids 4 converted to corresponding 3-arylthieno[3,2- c ]pyridine 5 . Substituent R^3 has predominant effect on fluorescence properties of thienopyridines. However, the electron donor Amine at C_4 has no effect on fluorescence properties of thienopyridines. Graphical Abstract New thieno[3,2-c]pyridine derivatives were synthesized from 3-bromo-4-chlorothieno[3,2-c]pyridine and Cyclic Amines, which by on Suzuki reaction with boronic acids converted to corresponding 3-arylthieno[3,2-c]pyridine. Substituent R3 has predominant effect on fluorescence properties of thienopyridines. However, the electron donor Amine at C4 has no effect on fluorescence properties of thienopyridines
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Synthesis and Study the Effect of Donor-Acceptor Substituent on Fluorescence Behavior of Thieno[3, 2-c]pyridine Derivatives
Journal of Fluorescence, 2014Co-Authors: Raghunath B. Toche, Sunil N. ChavanAbstract:4-Hetero-1-yl-2-bromothieno[3,2-c]pyridines 3(a–d) were synthesized by the reaction of 2-bromo-4-chlorothieno[3,2-c]pyridine (1) and Cyclic Amine 2(a–d) , which on Suzuki coupling with substituted boronic acids 4(a–f) exclusively converted to corresponding 4-hetero -1-yl-2-arylthieno [3,2-c] pyridine 5(a–x) in good yields. The effect of donor-acceptor substituent on absorption emission properties and fluorescent quantum yield of new thienopyridine derivatives 5(a-x) were studied.
Satish M. Chavan - One of the best experts on this subject based on the ideXlab platform.
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Substituent Effect on Absorption and Fluorescence Properties of Thieno[3, 2-c]Pyridine Derivatives
Journal of Fluorescence, 2017Co-Authors: Sunil N. Chavan, Raghunath B. Toche, Satish M. ChavanAbstract:New substituted thieno[3,2- c ]pyridine derivatives 5 were synthesized by the reaction of 3-bromo-4-chlorothieno[3,2- c ]pyridine 1 with Cyclic Amine 2, which further on Suzuki reaction with boronic acids 4 converted to corresponding 3-arylthieno[3,2- c ]pyridine 5 . Substituent R^3 has predominant effect on fluorescence properties of thienopyridines. However, the electron donor Amine at C_4 has no effect on fluorescence properties of thienopyridines. Graphical Abstract New thieno[3,2-c]pyridine derivatives were synthesized from 3-bromo-4-chlorothieno[3,2-c]pyridine and Cyclic Amines, which by on Suzuki reaction with boronic acids converted to corresponding 3-arylthieno[3,2-c]pyridine. Substituent R3 has predominant effect on fluorescence properties of thienopyridines. However, the electron donor Amine at C4 has no effect on fluorescence properties of thienopyridines
Osamu Onomura - One of the best experts on this subject based on the ideXlab platform.
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Electrochemical Deallylation of α‐Allyl Cyclic Amines and Synthesis of Optically Active Quaternary Cyclic Amino Acids
Chemistry: A European Journal, 2010Co-Authors: Peter G. Kirira, Masami Kuriyama, Osamu OnomuraAbstract:: Electrochemical oxidation of alpha-allylated and alpha-benzylated N-acylated Cyclic Amines by using a graphite anode easily affords the corresponding alpha-methoxylated products with up to 76 % yield. Ease of oxidation was affected by the type of electrode, the size of Cyclic Amine, and the nature of the protecting group. This method was successfully applied to the synthesis of optically active N-acylated alpha-alkyl-alpha-amino acid esters with up to 99 % ee.
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Electrochemical deallylation of ??-allyl Cyclic Amines and synthesis of optically active quaternary Cyclic amino acids
Chemistry - A European Journal, 2010Co-Authors: Peter G. Kirira, Masami Kuriyama, Osamu OnomuraAbstract:Electrochemical oxidation of alpha-allylated and alpha-benzylated N-acylated Cyclic Amines by using a graphite anode easily affords the corresponding alpha-methoxylated products with up to 76 % yield. Ease of oxidation was affected by the type of electrode, the size of Cyclic Amine, and the nature of the protecting group. This method was successfully applied to the synthesis of optically active N-acylated alpha-alkyl-alpha-amino acid esters with up to 99 % ee.
Gregory Lamonte - One of the best experts on this subject based on the ideXlab platform.
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mutations in the plasmodium falciparum Cyclic Amine resistance locus pfcarl confer multidrug resistance
Mbio, 2016Co-Authors: Gregory Lamonte, Melanie Wree, Christin Reimer, Marie Nachon, Victoria C Corey, Peter Gedeck, David Plouffe, Alan Du, Nelissa Figueroa, Bryan K S YeungAbstract:ABSTRACT Mutations in the Plasmodium falciparum Cyclic Amine resistance locus (PfCARL) are associated with parasite resistance to the imidazolopiperazines, a potent class of novel antimalarial compounds that display both prophylactic and transmission-blocking activity, in addition to activity against blood-stage parasites. Here, we show that pfcarl encodes a protein, with a predicted molecular weight of 153 kDa, that localizes to the cis-Golgi apparatus of the parasite in both asexual and sexual blood stages. Utilizing clustered regularly interspaced short palindromic repeat (CRISPR)-mediated gene introduction of 5 variants (L830V, S1076N/I, V1103L, and I1139K), we demonstrate that mutations in pfcarl are sufficient to generate resistance against the imidazolopiperazines in both asexual and sexual blood-stage parasites. We further determined that the mutant PfCARL protein confers resistance to several structurally unrelated compounds. These data suggest that PfCARL modulates the levels of small-molecule inhibitors that affect Golgi-related processes, such as protein sorting or membrane trafficking, and is therefore an important mechanism of resistance in malaria parasites. IMPORTANCE Several previous in vitro evolution studies have implicated the Plasmodium falciparum Cyclic Amine resistance locus (PfCARL) as a potential target of imidazolopiperazines, potent antimalarial compounds with broad activity against different parasite life cycle stages. Given that the imidazolopiperazines are currently being tested in clinical trials, understanding their mechanism of resistance and the cellular processes involved will allow more effective clinical usage.
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plasmodium falciparum Cyclic Amine resistance locus pfcarl a resistance mechanism for two distinct compound classes
ACS Infectious Diseases, 2016Co-Authors: Pamela Magistrado, Gregory Lamonte, Melanie Wree, Victoria C Corey, Amanda K Lukens, Erika Sasaki, Stephan Meister, Elizabeth A Winzeler, Dyann F WirthAbstract:MMV007564 is a novel antimalarial benzimidazolyl piperidine chemotype identified in cellular screens. To identify the genetic determinant of MMV007564 resistance, parasites were cultured in the presence of the compound to generate resistant lines. Whole genome sequencing revealed distinct mutations in the gene named Plasmodium falciparum Cyclic Amine resistance locus (pfcarl), encoding a conserved protein of unknown function. Mutations in pfcarl are strongly associated with resistance to a structurally unrelated class of compounds, the imidazolopiperazines, including KAF156, currently in clinical trials. Our data demonstrate that pfcarl mutations confer resistance to two distinct compound classes, benzimidazolyl piperidines and imidazolopiperazines. However, MMV007564 and the imidazolopiperazines, KAF156 and GNF179, have different timings of action in the asexual blood stage and different potencies against the liver and sexual blood stages. These data suggest that pfcarl is a multidrug-resistance gene rat...
