@article{PAR00014698, title = {{N}ovel 2-phenyl-5-[({E})-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[({E})-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting {NS}5 polymerase}, author = {{B}enmansour, {F}. and {E}ydoux, {C}. and {Q}uerat, {G}. and de {L}amballerie, {X}avier and {C}anard, {B}. and {A}lvarez, {K}. and {G}uillemot, {J}. {C}. and {B}arral, {K}.}, editor = {}, language = {{ENG}}, abstract = {{U}sing a functional high-throughput screening ({HTS}) and subsequent {SAR} studies, we have discovered a novel series of non-nucleoside dengue viral polymerase inhibitors. {W}e report the elaboration of {SAR} around hit compound 1 as well as the synthesis and antiviral evaluation of 3-phenyl-5-[({E})-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole and 5-phenyl-2-[2-(2-thienyl)ethenyl]-1,3,4-oxadiazole analogues derived from a rapid and easily accessible chemical pathway. {A} large number of compounds prepared by this method were shown to possess in vitro activity against the polymerase of dengue virus. {T}he most potent inhibitors were tested against {D}engue virus clinical isolates on infected cells model and exhibit submicromolar activity on the four dengue virus serotypes.}, keywords = {2-phenyl-5-[({E})-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole ; 3-phenyl-5-[({E})-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole ; {D}engue ; virus ; {NS}5 {R}d{R}p inhibitors ; {A}ntiviral activity}, booktitle = {}, journal = {{E}uropean {J}ournal of {M}edicinal {C}hemistry}, volume = {109}, numero = {}, pages = {146--156}, ISSN = {0223-5234}, year = {2016}, DOI = {10.1016/j.ejmech.2015.12.046}, URL = {https://www.documentation.ird.fr/hor/{PAR}00014698}, }