- The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives
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A series of new arylamino quinoline derivatives was designed based on the quinine and mefloquine scaffolds and evaluated in vitro for antiplasmodial and antimycobacterial activities. A number of these compounds exhibited significant activity against the d
- Tukulula, Matshawandile,Little, Susan,Gut, Jiri,Rosenthal, Philip J.,Wan, Baojie,Franzblau, Scott G.,Chibale, Kelly
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- Development of novel quinoline-based sulfonamides as selective cancer-associated carbonic anhydrase isoform ix inhibitors
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A new series of quinoline-based benzenesulfonamides (QBS) were developed as potential carbonic anhydrase inhibitors (CAIs). The target QBS CAIs is based on the 4-anilinoquinoline scaffold where the primary sulphonamide functionality was grafted at C4 of t
- Shaldam, Moataz,Nocentini, Alessio,Elsayed, Zainab M.,Ibrahim, Tamer M.,Salem, Rofaida,El-Domany, Ramadan A.,Capasso, Clemente,Supuran, Claudiu T.,Eldehna, Wagdy M.
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- Synthesis of novel 3,4,6-trisubstituted quinolines enabled by a Gould-Jacobs cyclization
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A Gould-Jacobs cyclization enabled the synthesis of several novel, so far undescribed 3,4,6-trisubstituted quinoline derivatives. They all bear substituents which are well-suited for further transformations, e.g. carboxylic acid or ester functions, haloge
- Trah, Stephan,Lamberth, Clemens
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p. 794 - 796
(2017/03/31)
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- Differential characterization using readily accessible NMR experiments of novel N- and O-alkylated quinolin-4-ol, 1,5-naphthyridin-4-ol and quinazolin-4-ol derivatives with antimycobacterial activity
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During the construction of bioactive molecules, regioselective alkylation of heterocyclic, N/O ambident nucleophiles is a frequently encountered synthetic transformation. In this framework, specific attention is required to unambiguously determine the str
- Pitta, Eleni,Balabon, Olga,Rogacki, Maciej K.,Gómez, Jesús,Cunningham, Fraser,Joosens, Jurgen,Augustyns, Koen,van der Veken, Pieter,Bates, Robert
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p. 890 - 901
(2016/10/25)
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- Highly efficient thermal cyclization reactions of alkylidene esters in continuous flow to give aromatic/heteroaromatic derivatives
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Intramolecular thermal cyclization and benzannulation reactions of the Gould-Jacobs and Conrad-Limpach types were performed in a designed continuous flow reactor system at temperatures in the range of 300-360°C and under high pressure conditions (100-160 bar) with very short residence times (0.45-4.5 min) in tetrahydrofuran as a low-boiling point solvent. Substituted heteroaromatic compounds including pyridopyrimidinones and hydroxyquinolines were synthesized in moderate to high yields. Application of the reaction conditions also allows the synthesis of naphthol and biphenyl derivatives. The procedure involves an easy work-up and the non-batchwise preparative synthesis method is suitable for automation.
- Lengyel, László,Nagy, Tibor Zs.,Sipos, Gellért,Jones, Richard,Dormán, Gy?rgy,ürge, László,Darvas, Ferenc
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p. 738 - 743
(2012/03/08)
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- Preparation of quinoline hexose analogs as novel chloroquine-resistant malaria treatments (1). Synthesis of 4-hydroxyquinoline-β-glucosides
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Quinoline hexose analogs are expected to be useful as novel agents for treatment of chloroquine-resistant malaria. Here, we report preparation of 4-hydroxy quinoline-β-glucosides from anilines in 4 steps.
- Suzuki, Hiroshi,Aly, Nagwa S. M.,Wataya, Yusuke,Kim, Hye-Sook,Tamai, Ikumi,Kita, Masaki,Uemura, Daisuke
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p. 821 - 824
(2008/02/13)
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- Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: Synthesis and preliminary SAR analysis
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In an attempt to search for a new class of antibacterial agents, we have discovered a series of pyrazole analogs that possess good antibacterial activity for Gram-positive and Gram-negative organisms via inhibition of type II bacterial topoisomerases. We have investigated the structure-activity relationships of this series, with an emphasis on the length and conformation of the linker. This work led to the identification of tetrahydroindazole analogs, such as compound 1, as the most potent class of compounds.
- Gomez, Laurent,Hack, Michael D.,Wu, Jiejun,Wiener, John J.M.,Venkatesan, Hari,Santillan Jr., Alejandro,Pippel, Daniel J.,Mani, Neelakandha,Morrow, Brian J.,Motley, S. Timothy,Shaw, Karen Joy,Wolin, Ronald,Grice, Cheryl A.,Jones, Todd K.
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p. 2723 - 2727
(2008/02/03)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 31
(2010/11/25)
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- Assembly of 4-aminoquinolines via palladium catalysis: A mild and convenient alternative to SNAr methodology
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4-Aminoquinolines, classically prepared via SNAr chemistry from an amine and 4-haloquinoline, are important scaffolds in medicinal chemistry. Interest in these compounds prompted us to explore palladium catalysis as an alternative to the existing methods for their preparation. Initial results followed by an iterative screening paradigm confirmed Pd(OAc)2/ DPEphos/K3PO4 as a mild and convenient alternative for the formation of the C-N bond in 4-aminoquinolines. A description of the screen and the scope of this methodology are discussed herein.
- Margolis, Brandon J.,Long, Kimberly A.,Laird, Dana L. T.,Ruble, J. Craig,Pulley, Shon R.
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p. 2232 - 2235
(2007/10/03)
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- NOVEL COMPOUNDS HAVING AN ANTI-BACTERIAL ACTIVITY
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The present invention describes novel anti-bacterial compounds of formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase.
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Page/Page column 88-89
(2010/10/20)
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- A novel synthesis of substituted quinolines using ring-closing metathesis (RCM): Its application to the synthesis of key intermediates for anti-malarial agents
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A method for synthesizing substituted quinolines using ruthenium-catalyzed ring-closing metathesis as a key step has been developed. Substituted 1,2-dihydroquinolines, 4-silyloxy-1,2-dihydroquinoline and 4-methoxy-1,2- dihydroquinoline, were successfully synthesized in excellent yields via ene-ene metathesis and silyl or alkyl enol ether-ene metathesis, respectively. The synthetic intermediates of the antimalarial agents quinine, chloroquine, and PPMP-quinine hybrid were efficiently synthesized by this methodology.
- Theeraladanon, Chumpol,Arisawa, Mitsuhiro,Nishida, Atsushi,Nakagawa, Masako
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p. 3017 - 3035
(2007/10/03)
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- Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them
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Heterocyclylalkylpiperidine derivatives of general formula (I) in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.
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- Synthesis of novel heterocycles related to the dynemicin A ring skeleton
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Studies directed towards the construction of the CDE ring framework of dynemycin A (1) are reported. A series of quinoline based dienophiles containing an activating group (e.g. 5), reacted with acyclic dienes (e.g. 4) in a Diels-Alder fashion under incre
- Nicolaou,Gross,Gross, Jonathan L.,Kerr,Kerr, Michael A.
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p. 735 - 746
(2007/10/03)
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