@article{fdi:010065400, title = {{S}ynthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines}, author = {{M}archand, {P}. and {B}azin, {M}. {A}. and {P}agniez, {F}. and {R}iviere, {G}. and {B}odero, {L}. and {M}arhadour, {S}. and {N}ourrisson, {M}. {R}. and {P}icot, {C}. and {R}uchaud, {S}. and {B}ach, {S}. and {B}aratte, {B}. and {S}auvain, {M}ichel and {P}areja, {D}. {C}. and {V}aisberg, {A}. {J}. and {L}e {P}ape, {P}.}, editor = {}, language = {{ENG}}, abstract = {{A} series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the {C}-8 position, was synthesized and evaluated for their antileishmanial activities. {T}wo derivatives exhibited very good activity against the promastigote and the amastigote forms of {L}eishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3{T}3 mouse fibroblast cells. {T}hrough {L}m{CK}1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed.}, keywords = {{A}ntileishmanial activity ; {I}midazo[1,2-a]pyrazines ; {D}irect arylation ; {C}asein kinase 1}, booktitle = {}, journal = {{E}uropean {J}ournal of {M}edicinal {C}hemistry}, volume = {103}, numero = {}, pages = {381--395}, ISSN = {0223-5234}, year = {2015}, DOI = {10.1016/j.ejmech.2015.09.002}, URL = {https://www.documentation.ird.fr/hor/fdi:010065400}, }