- Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines
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A novel series of extended DAPI analogues were prepared by insertion of either a carbon-carbon triple bond (16a-d) or a phenyl group (21a,b and 24) at position-2. The new amidines were evaluated in vitro against both Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.). Five compounds (16a, 16b, 16d, 21a, 21b) exhibited IC50 values against T. b. r. of 9 nM or less which is two to nine folds more effective than DAPI. The same five compounds exhibited IC50 values against P. f. of 5.9 nM or less which is comparable to that of DAPI. The fluorescence properties of these new molecules were recorded, however; they do not offer any advantage over those of DAPI.
- Farahat, Abdelbasset A.,Kumar, Arvind,Say, Martial,Barghash, Alaa El-Din M.,Goda, Fatma E.,Eisa, Hassan M.,Wenzler, Tanja,Brun, Reto,Liu, Yang,Mickelson, Leah,Wilson, W. David,Boykin, David W.
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scheme or table
p. 557 - 566
(2010/04/29)
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- Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles
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3,5-Bis(4-amidinophenyl)isoxazole (3) - an analogue of 2,5-bis(4- amidinophenyl)furan (furamidine) in which the central furan ring is replaced by isoxazole - and 42 novel analogues were prepared by two general synthetic pathways. The 43 isoxazole derivati
- Patrick, Donald A.,Bakunov, Stanislav A.,Bakunova, Svetlana M.,Kumar, E.V.K. Suresh,Lombardy, Richard J.,Jones, Susan Kilgore,Bridges, Arlene S.,Zhirnov, Oksana,Hall, James Edwin,Wenzler, Tanja,Brun, Reto,Tidwell, Richard R.
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p. 2468 - 2485
(2008/02/03)
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- Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition
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The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
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Page/Page column 23
(2010/11/08)
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- Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles
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Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.
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Page/Page column 24-28; 41
(2010/11/24)
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- Total synthesis of stephanotic acid methyl ester
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The methyl ester of the naturally occurring macrocyclic pentapeptide stephanotic acid, containing an unusual β-substituted α-amino acid with a tryptophan C-6 to leucine β-carbon link, has been synthesized. The key steps include the formation of this amino acid through a thioxo-oxazolidine intermediate and a Horner-Wadsworth-Emmons reaction using a phosphonoglycine, derived by a dirhodium(II)-catalyzed N-H insertion reaction, to give a dehydroamino acid and subsequent rhodium(I)-catalyzed asymmetric hydrogenation to introduce the modified tryptophan residue.
- Bentley, David J.,Slawin, Alexandra M. Z.,Moody, Christopher J.
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p. 1975 - 1978
(2007/10/03)
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- Microwave assisted Leimgruber-Batcho reaction for the preparation of indoles, azaindoles and pyrroylquinolines
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The development of enhanced conditions for Lewis acid catalysed Leimgruber-Batcho indole synthesis using microwave acceleration is described. This approach has permitted the preparation of a variety of heteroaromatic enamine intermediates in good yield and high purities. Subsequent catalytic hydrogenation reactions, under various conditions including the use of a solid-phase encapsulated catalyst, furnish the corresponding indole derivatives in good yields.
- Siu, Jason,Baxendale, Ian R.,Ley, Steven V.
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p. 160 - 167
(2007/10/03)
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- Intermediates for indoles
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Ortho-nitrotoluenes are condensed with formamide acetals to yield the corresponding otho-nitro-β-aminestyrenes which undergo cyclization upon reduction to yield indoles.
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