- Synthesis of new pyrazolo[4,3-c]quinolin-3-one derivatives and some oxazolo[4,5-c]quinoline-2,4-diones
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The new pyrazolo[4,3-c]quinolin-3-one derivatives 3a-c and 6a-c were prepared by the following three steps: first the preparation of ethyl 4- hydroxyquinoline-3-carboxylate derivatives 1 and 4 by reaction of isatoic anhydrides and ethyl malonate and ethyl acetoacetate respectively, then chloration of 1 and 4 with phosphorus oxychloride to give 2 and 5 and finally the condensation of 2 and 5 with hydrazine and its derivatives. In addition, the successful synthesis of oxazolo[4,5-c]quinoline-2,4-diones 9a-f are reported.
- Ismaili, Lhassane,Refouvelet, Bernard,Robert, Jean Francois
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- Novel potent 5-HT3 receptor ligands based on the pyrrolidone structure: Synthesis, biological evaluation, and computational rationalization of the ligand-receptor interaction modalities
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Novel conformationally constrained derivatives of classical 5-HT3 receptor antagonists were designed and synthesized with the aim of probing the central 5-HT3 receptor recognition site in a systematic way. The newly-synthesized compo
- Cappelli, Andrea,Anzini, Maurizio,Vomero, Salvatore,Mennuni, Laura,Makovec, Francesco,Doucet, Edith,Hamon, Michel,Menziani,De Benedetti, Pier G.,Giorgi, Gianluca,Ghelardini, Carla,Collina, Simona
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- Discovery of plasmodium vivax N -myristoyltransferase inhibitors: Screening, synthesis, and structural characterization of their binding mode
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N-Myristoyltransferase (NMT) is a prospective drug target against parasitic protozoa. Herein we report the successful discovery of a series of Plasmodium vivax NMT inhibitors by high-throughput screening. A high-resolution crystal structure of the hit com
- Goncalves, Victor,Brannigan, James A.,Whalley, David,Ansell, Keith H.,Saxty, Barbara,Holder, Anthony A.,Wilkinson, Anthony J.,Tate, Edward W.,Leatherbarrow, Robin J.
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p. 3578 - 3582
(2012/06/01)
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- THERAPEUTIC PYRAZOLOQUINOLINE UREA DERIVATIVES
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The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment
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Page/Page column 20
(2009/01/20)
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- Structure-activity relationship of quinoline derivatives as potent and selective α2c-adrenoceptor antagonists
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Starting from two acridine compounds identified in a high-throughput screening campaign (1 and 2, Table 1), a series of 4-aminoquinolines was synthesized and tested for their properties on the human α2- adrenoceptor subtypes (α2A, α2B, and α2C). A number of compounds with good antagonist potencies against the α2C-adrenoceptor and excellent subtype selectivities over the other two subtypes were discovered. For example, (R)-{4-[4-(3,4-dimethylpiperazin-1-yl)phenylamino]quinolin-3-yl}methanol 6j had an antagonist potency of 8.5 nM against, and a subtype selectivity of more than 200-fold for, the α2c-adrenoceptor. Investigation of the structure-activity relationship identified a number of structural features, the most critical of which was an absolute need for a substituent in the 3-position of the quinoline ring. The 3-position on the piperazine ring was also found to play an appreciable role, as substitutions in that position exerted a significant and stereospecific beneficial effect on the α2C- adrenoceptor affinity and potency. Replacing the piperazine ring proved difficult, with 1,4-diazepanes representing the only viable alternative.
- H?glund, Iisa P. J.,Silver, Satu,Engstr?m, Mia T.,Salo, Harri,Tauber, Andrei,Kyyr?nen, Hanna-Kaisa,Saarenketo, Pauli,Hoffrén, Anna-Marja,Kokko, Kurt,Pohjanoksa, Katariina,Sallinen, Jukka,Savola, Juha-Matti,Wurster, Siegfried,Kallatsa, Oili A.
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p. 6351 - 6363
(2007/10/03)
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