- Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
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A series of new boron-containing benzoxaborole compounds was designed and synthesized for a continuing structure-activity relationship (SAR) investigation to assess the antimalarial activity changes derived from side-chain structural variation, substituent modification on the benzene ring and removal of boron from five-membered oxaborole ring. This SAR study demonstrated that boron is required for the antimalarial activity, and discovered that three fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles (9, 14 and 20) have excellent potencies (IC50 0.026-0.209 μM) against Plasmodium falciparum.
- Zhang, Yong-Kang,Plattner, Jacob J.,Freund, Yvonne R.,Easom, Eric E.,Zhou, Yasheen,Ye, Long,Zhou, Huchen,Waterson, David,Gamo, Francisco-Javier,Sanz, Laura M.,Ge, Min,Li, Zhiya,Li, Lingchao,Wang, Hailong,Cui, Han
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p. 1299 - 1307
(2012/03/26)
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- A new synthesis of 8-hydroxy-2-di-n-propylamino-tetralin (8-OH-DPAT)
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A new synthesis method for 8-OH-DPAT, a specific agonist at the 5-HT(1A) serotonin receptor, is described. It employs the Curtius degradation of a tetralin carboxylic acid easily prepared from (2-methoxy benzyl) succinic acid by Friedel-Craft cyclisation.
- Langlois,Gaudy
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p. 1723 - 1734
(2007/10/02)
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- Synthesis of Tetrahydrobenzophenazines as Anthracyclinone N-Isosteres
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The anthracycline p-quinone unit has been replaced by a 1,4-di-N-oxide function in the first synthesis of a 7,9-dideoxyanthracyclinone hetero isostere. 4,11-Dimethoxy-9-(methoxycarbonyl)-7,8,9,10-tetrahydrobenzophenazine was synthesized and converted t
- Tracy, Michael,Acton, Edward M.
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p. 5116 - 5124
(2007/10/02)
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- Studies on Gibberellin Synthesis. Assembly of an Ethanophenanthrenoid Lactone and Conversion into a Gibbane Derivative
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Diazoketone (13), prepared by standard methods from 5-formyl-8-methoxy-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid (7), was cyclized in trifluoroacetic acid to dienone (1) which underwent intramolecular 1,4-conjugate addition to afford the ethanophena
- Mander, Lewis N.,Pyne, Stephen G.
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p. 1899 - 1911
(2007/10/02)
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