Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors agai...
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| Formato: | Capítulo de libro |
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2005
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| Acceso en línea: | Registro en Scopus DOI Handle Registro en la Biblioteca Digital |
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| LEADER | 09922caa a22012857a 4500 | ||
|---|---|---|---|
| 001 | PAPER-3885 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518203321.0 | ||
| 008 | 190411s2005 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-25444525132 | |
| 024 | 7 | |2 cas |a geranyltransferase, 37277-79-5, 50812-36-7; Antiprotozoal Agents; Diphosphonates; farnesyl pyrophosphatase, EC 3.6.1.-; Fatty Acids; Pyrophosphatases, EC 3.6.1.- | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a BMCLE | ||
| 100 | 1 | |a Szajnman, S.H. | |
| 245 | 1 | 0 | |a Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase |
| 260 | |c 2005 | ||
| 270 | 1 | 0 | |m Rodriguez, J.B.; Departamento de Química Orgánica, Facultad de Ciencias Exactas Y Naturales, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina; email: jbr@qo.fcen.uba.ar |
| 506 | |2 openaire |e Política editorial | ||
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| 520 | 3 | |a We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at low micromolar level. Cellular activity was associated with the inhibition of enzymatic activity of T. cruzi farnesyl pyrophosphate synthase. As bisphosphonate-containing drugs are FDA-approved for the treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases. © 2005 Elsevier Ltd. All rights reserved. |l eng | |
| 536 | |a Detalles de la financiación: Fundación Antorchas | ||
| 536 | |a Detalles de la financiación: Foundation for the National Institutes of Health, GM-65307 | ||
| 536 | |a Detalles de la financiación: Universidad de Buenos Aires, X-252 | ||
| 536 | |a Detalles de la financiación: This work was supported by grants from Fundación Antorchas, and the Universidad de Buenos Aires (X-252) to J.B.R., and the U.S. National Institutes of Health (GM-65307) to R.D. | ||
| 593 | |a Departamento de Química Orgánica, Facultad de Ciencias Exactas Y Naturales, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina | ||
| 593 | |a Center for Global and Emerging Diseases, Department of Cellular Biology, University of Georgia, Athens, GA 30602, United States | ||
| 690 | 1 | 0 | |a BISPHOSPHONATES |
| 690 | 1 | 0 | |a CHAGAS' DISEASE |
| 690 | 1 | 0 | |a FARNESYL PYROPHOSPHATE SYNTHASE |
| 690 | 1 | 0 | |a TRYPANOSOMA CRUZI |
| 690 | 1 | 0 | |a BISPHOSPHONIC ACID DERIVATIVE |
| 690 | 1 | 0 | |a FATTY ACID |
| 690 | 1 | 0 | |a GERANYLTRANSFERASE |
| 690 | 1 | 0 | |a PROTOZOAL PROTEIN |
| 690 | 1 | 0 | |a ANTIPROTOZOAL ACTIVITY |
| 690 | 1 | 0 | |a ARTICLE |
| 690 | 1 | 0 | |a CELL PROLIFERATION |
| 690 | 1 | 0 | |a CHAGAS DISEASE |
| 690 | 1 | 0 | |a DRUG SYNTHESIS |
| 690 | 1 | 0 | |a DRUG TARGETING |
| 690 | 1 | 0 | |a ENZYME INHIBITION |
| 690 | 1 | 0 | |a IC 50 |
| 690 | 1 | 0 | |a NONHUMAN |
| 690 | 1 | 0 | |a TRYPANOSOMA CRUZI |
| 690 | 1 | 0 | |a ANIMALS |
| 690 | 1 | 0 | |a ANTIPROTOZOAL AGENTS |
| 690 | 1 | 0 | |a DIPHOSPHONATES |
| 690 | 1 | 0 | |a DRUG DELIVERY SYSTEMS |
| 690 | 1 | 0 | |a FATTY ACIDS |
| 690 | 1 | 0 | |a INHIBITORY CONCENTRATION 50 |
| 690 | 1 | 0 | |a PYROPHOSPHATASES |
| 690 | 1 | 0 | |a STRUCTURE-ACTIVITY RELATIONSHIP |
| 690 | 1 | 0 | |a TRYPANOSOMA CRUZI |
| 690 | 1 | 0 | |a TRYPANOSOMA CRUZI |
| 700 | 1 | |a Ravaschino, E.L. | |
| 700 | 1 | |a Docampo, R. | |
| 700 | 1 | |a Rodriguez, J.B. | |
| 773 | 0 | |d 2005 |g v. 15 |h pp. 4685-4690 |k n. 21 |p Bioorg. Med. Chem. Lett. |x 0960894X |w (AR-BaUEN)CENRE-3990 |t Bioorganic and Medicinal Chemistry Letters | |
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| 856 | 4 | 0 | |u https://hdl.handle.net/20.500.12110/paper_0960894X_v15_n21_p4685_Szajnman |y Handle |
| 856 | 4 | 0 | |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v15_n21_p4685_Szajnman |y Registro en la Biblioteca Digital |
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