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Design, synthesis and antimalarial evaluation of novel thiazole derivatives
dc.contributor.author | Bueno, José María | |
dc.contributor.author | Carda, Miguel | |
dc.contributor.author | Crespo, Benigno | |
dc.contributor.author | Cuñat, Ana Carmen | |
dc.contributor.author | De Cozar, Cristina | |
dc.contributor.author | León, María Luisa | |
dc.contributor.author | Marco, J. Alberto | |
dc.contributor.author | Roda, Nuria | |
dc.contributor.author | Sanz-Cervera, Juan F. | |
dc.date.accessioned | 2016-11-07T18:44:08Z | |
dc.date.available | 2016-11-07T18:44:08Z | |
dc.date.issued | 2016 | |
dc.identifier.citation | BUENO, José María, et al. Design, synthesis and antimalarial evaluation of novel thiazole derivatives. Bioorganic & Medicinal Chemistry Letters, 2016, vol. 26, no 16, p. 3938-3944. | ca_CA |
dc.identifier.issn | 0960-894X | |
dc.identifier.uri | http://hdl.handle.net/10234/164132 | |
dc.description.abstract | As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain. The results indicate that modifications of the N-aryl amide group linked to the thiazole ring are the most significant in terms of in vitro antimalarial activity, leading to compounds with high antimalarial potency and low cytotoxicity in HepG2 cell lines. Furthermore, the observed SAR implies that non-bulky, electron-withdrawing groups are preferred at ortho position on the phenyl ring, whereas small atoms such as H or F are preferred at para position. Finally, replacement of the phenyl ring by a pyridine affords a compound with similar potency, but with potentially better physicochemical properties which could constitute a new line of research for further studies. | ca_CA |
dc.description.sponsorShip | M.C., A.C.C., J.A.M., N.R. and J.F.S.-C. thank the Ministerio de Ciencia e Innovación of Spain (research grant CTQ2011-27560) and the Consellería d’Educació, Investigació, Cultura i Esport de la Generalitat Valenciana (research grant PROMETEO/2013/027) for financial support. | ca_CA |
dc.format.extent | 7 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | Elsevier | ca_CA |
dc.relation.isPartOf | Bioorganic & Medicinal Chemistry Letters, 2016, vol. 26, núm. 16 | ca_CA |
dc.rights | © 2016 Elsevier Ltd. All rights reserved. | ca_CA |
dc.rights.uri | http://rightsstatements.org/vocab/InC/1.0/ | * |
dc.subject | Malaria | ca_CA |
dc.subject | Antimalarials | ca_CA |
dc.subject | Synthesis | ca_CA |
dc.subject | Thiazoles | ca_CA |
dc.subject | Structure–activity relationship | ca_CA |
dc.title | Design, synthesis and antimalarial evaluation of novel thiazole derivatives | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | http://dx.doi.org/10.1016/j.bmcl.2016.07.010 | |
dc.rights.accessRights | info:eu-repo/semantics/restrictedAccess | ca_CA |
dc.relation.publisherVersion | http://bs8lz6ys5q.search.serialssolutions.com/?ctx_ver=Z39.88-2004&ctx_enc=info%3Aofi%2Fenc%3AUTF-8&rfr_id=info%3Asid%2Fsummon.serialssolutions.com&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.atitle=Design%2C+synthesis+and+antimalarial+evaluation+of+novel+thiazole+derivatives&rft.jtitle=BIOORGANIC+%26+MEDICINAL+CHEMISTRY+LETTERS&rft.au=Bueno%2C+JM&rft.au=Carda%2C+M&rft.au=Crespo%2C+B&rft.au=Cunat%2C+AC&rft.date=2016-08-15&rft.pub=PERGAMON-ELSEVIER+SCIENCE+LTD&rft.issn=0960-894X&rft.eissn=1464-3405&rft.volume=26&rft.issue=16&rft.spage=3938&rft.epage=3944&rft_id=info:doi/10.1016%2Fj.bmcl.2016.07.010&rft.externalDBID=n%2Fa&rft.externalDocID=000380574400019¶mdict=es-ES | ca_CA |
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