{"id":82038,"date":"2026-08-22T02:30:18","date_gmt":"2026-08-21T17:30:18","guid":{"rendered":"https:\/\/thekoreantoday.com\/dongjak\/2026\/08\/22\/libs-met-au-point-une-technique-dedition-moleculaire-permettant-de-reconcevoir-librement-meme-les-medicaments-complexes\/"},"modified":"2026-08-22T02:30:21","modified_gmt":"2026-08-21T17:30:21","slug":"libs-met-au-point-une-technique-dedition-moleculaire-permettant-de-reconcevoir-librement-meme-les-medicaments-complexes","status":"publish","type":"post","link":"https:\/\/thekoreantoday.com\/dongjak\/2026\/08\/22\/libs-met-au-point-une-technique-dedition-moleculaire-permettant-de-reconcevoir-librement-meme-les-medicaments-complexes\/","title":{"rendered":"L’IBS met au point une technique d’\u00e9dition mol\u00e9culaire permettant de reconcevoir librement m\u00eame les m\u00e9dicaments complexes"},"content":{"rendered":"

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Une nouvelle m\u00e9thode de synth\u00e8se permettant de modifier ais\u00e9ment la structure des compos\u00e9s pyridiniques, les plus largement utilis\u00e9s dans les m\u00e9dicaments, a \u00e9t\u00e9 mise au point par une \u00e9quipe de chercheurs cor\u00e9ens. En ne changeant que la position de l’atome d’azote tout en conservant intacte l’ossature complexe du m\u00e9dicament achev\u00e9, cette approche ouvre, selon les experts, la voie \u00e0 une exploration rapide de divers candidats-m\u00e9dicaments.<\/p>\n

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  [\ucf54\ub9ac\uc548\ud22c\ub370\uc774] Sch\u00e9ma conceptuel de l’isom\u00e9risation de position par r\u00e9arrangement de l’azote dans la pyridine © \uc7a5\ud615\uc784 \uae30\uc790<\/span><\/p>\n<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

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Le minist\u00e8re des Sciences et des TIC (vice-Premier ministre et ministre des Sciences et des TIC, Bae Kyung-hoon) a annonc\u00e9 que l’\u00e9quipe de recherche dirig\u00e9e par Hong Seung-woo, directeur par int\u00e9rim du Centre de recherche sur les r\u00e9actions catalytiques d’activation mol\u00e9culaire de l’Institut des sciences fondamentales (IBS, dirig\u00e9 par Jang Seok-bok) et professeur au d\u00e9partement de chimie du KAIST, a d\u00e9velopp\u00e9 une m\u00e9thode de synth\u00e8se dite de transposition de l’atome d’azote (N-atom transposition), qui permet de d\u00e9placer l’azote du cycle pyridinique vers la position souhait\u00e9e. Cette recherche a \u00e9t\u00e9 men\u00e9e dans le cadre du programme de soutien aux centres de recherche en sciences fondamentales de l’IBS du minist\u00e8re des Sciences et des TIC, et a \u00e9t\u00e9 publi\u00e9e le 18 ao\u00fbt \u00e0 0 h (heure de Cor\u00e9e) dans la prestigieuse revue Nature.<\/p>\n

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La pyridine est une structure cyclique hexagonale compos\u00e9e de cinq atomes de carbone et d’un atome d’azote, qui sert d’ossature de base \u00e0 de nombreux m\u00e9dicaments et substances chimiques. M\u00eame lorsque les m\u00eames substituants y sont fix\u00e9s, les propri\u00e9t\u00e9s physico-chimiques \u2014 solubilit\u00e9, absorption, perm\u00e9abilit\u00e9, liaison \u2014 ainsi que l’efficacit\u00e9 th\u00e9rapeutique varient consid\u00e9rablement selon la position relative de l’azote et des substituants. C’est pourquoi, dans le processus de d\u00e9veloppement de nouveaux m\u00e9dicaments, il est indispensable de produire plusieurs isom\u00e8res de position dont seul l’emplacement de l’azote diff\u00e8re l\u00e9g\u00e8rement, afin d’en comparer les fonctions.<\/p>\n

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Jusqu’\u00e0 pr\u00e9sent, les substituants fix\u00e9s sur le cycle pyridinique \u00e9taient consid\u00e9r\u00e9s comme des \u00e9l\u00e9ments fig\u00e9s, difficiles \u00e0 d\u00e9placer. Pour obtenir un isom\u00e8re dans la configuration voulue, il fallait concevoir d\u00e8s le d\u00e9part, pour chacun d’eux, une substance de d\u00e9part et une voie de synth\u00e8se sp\u00e9cifiques. Des tentatives avaient bien \u00e9t\u00e9 faites pour ne d\u00e9placer que les substituants sur une mol\u00e9cule achev\u00e9e, mais comme les conditions de r\u00e9action variaient selon le type de substituant, leur application \u00e9tait en pratique impossible pour les mol\u00e9cules complexes portant plusieurs substituants.<\/p>\n

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Au lieu de d\u00e9placer les substituants un \u00e0 un, l’\u00e9quipe a r\u00e9solu le probl\u00e8me par une id\u00e9e \u00e0 contre-courant : changer la position de l’azote, qui sert de point de r\u00e9f\u00e9rence. En laissant les substituants en place et en modifiant la position de l’azote, elle a fait varier d’un seul coup les relations de position de plusieurs substituants par rapport \u00e0 l’azote. Pour ce faire, les chercheurs ont con\u00e7u un proc\u00e9d\u00e9 consistant \u00e0 introduire dans le cycle un nouvel azote provenant d’une source ext\u00e9rieure, puis \u00e0 \u00e9liminer l’azote initial. Au cours de ce processus, le cycle initial \u00e0 six atomes s’est temporairement \u00e9largi en un cycle \u00e0 sept atomes avant de se r\u00e9arranger, donnant naissance \u00e0 une nouvelle pyridine dont la position de l’azote avait chang\u00e9. Des exp\u00e9riences de tra\u00e7age isotopique ont confirm\u00e9 que l’azote nouvellement introduit reste dans le cycle tandis que l’azote initial est \u00e9vacu\u00e9 sous forme d’azote gazeux (N2).<\/p>\n

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Cette nouvelle m\u00e9thode de synth\u00e8se s’est appliqu\u00e9e largement, des structures simples ne comportant qu’un seul substituant aux structures complexes en comportant deux ou plus, en passant par celles dot\u00e9es de plusieurs substituants aux propri\u00e9t\u00e9s distinctes. Apr\u00e8s optimisation des conditions de r\u00e9action, le rendement de synth\u00e8se des isom\u00e8res a atteint 88 %, et m\u00eame lors d’exp\u00e9riences o\u00f9 la quantit\u00e9 de r\u00e9actifs a \u00e9t\u00e9 fortement augment\u00e9e jusqu’\u00e0 10 millimoles, un rendement \u00e9lev\u00e9 de 74 % a \u00e9t\u00e9 maintenu, d\u00e9montrant ainsi le potentiel de production \u00e0 grande \u00e9chelle et d’application pratique.<\/p>\n

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En particulier, l’\u00e9quipe a appliqu\u00e9 cette technique \u00e0 des m\u00e9dicaments r\u00e9ellement commercialis\u00e9s \u2014 l’anticanc\u00e9reux vismod\u00e9gib, l’ac\u00e9tate d’abirat\u00e9rone et l’anti-inflammatoire antalgique \u00e9toricoxib \u2014 et a cr\u00e9\u00e9 de nouvelles mol\u00e9cules candidates dont seule la position de l’azote diff\u00e8re, tout en conservant intacte l’ossature complexe du m\u00e9dicament. Les chercheurs ont en outre d\u00e9couvert que, m\u00eame \u00e0 partir d’une m\u00eame substance de d\u00e9part, la proportion des isom\u00e8res de position varie selon le solvant utilis\u00e9. L’analyse par chimie computationnelle a montr\u00e9 que cela tient au fait que la hauteur de la barri\u00e8re \u00e9nerg\u00e9tique \u2014 l’\u00e9nergie minimale n\u00e9cessaire \u00e0 la r\u00e9action chimique \u2014 change selon le solvant, prouvant que le seul r\u00e9glage des conditions de solvant permet de synth\u00e9tiser s\u00e9lectivement l’isom\u00e8re souhait\u00e9.<\/p>\n

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Ce r\u00e9sultat retient l’attention en ce qu’il pourrait transformer la mani\u00e8re m\u00eame dont on obtient les substances candidates sur le terrain du d\u00e9veloppement de nouveaux m\u00e9dicaments. En effet, il devient possible, en s’affranchissant de la m\u00e9thode qui consistait \u00e0 pr\u00e9parer diff\u00e9rentes substances de d\u00e9part et \u00e0 les synth\u00e9tiser s\u00e9par\u00e9ment depuis le d\u00e9but, d’explorer directement divers isom\u00e8res de position \u00e0 partir d’une seule mol\u00e9cule d\u00e9j\u00e0 constitu\u00e9e. Comme on peut examiner de fa\u00e7on syst\u00e9matique l’influence de fines variations de structure sur les propri\u00e9t\u00e9s et l’efficacit\u00e9 d’un m\u00e9dicament, les chances de d\u00e9couvrir rapidement des m\u00e9dicaments plus s\u00fbrs et plus efficaces s’en trouvent d’autant accrues.<\/p>\n

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Hong Seung-woo, directeur par int\u00e9rim de l’IBS, a d\u00e9clar\u00e9 : ‘Cette recherche est n\u00e9e d’un changement de perspective consistant \u00e0 s’\u00e9carter des m\u00e9thodes existantes pour modifier la position m\u00eame des atomes au sein de l’ossature centrale’, ajoutant : ‘En \u00e9ditant directement, au niveau atomique, l’ossature centrale d’une mol\u00e9cule achev\u00e9e, elle contribuera \u00e0 explorer sous de multiples angles les variations de propri\u00e9t\u00e9s et d’efficacit\u00e9, et \u00e0 \u00e9largir de fa\u00e7on spectaculaire le champ de d\u00e9couverte des candidats-m\u00e9dicaments.’ Kim Sung-soo, directeur du bureau des politiques de R&D du minist\u00e8re des Sciences et des TIC, a affirm\u00e9 : ‘Cette recherche est un r\u00e9sultat repr\u00e9sentatif qui montre que la cr\u00e9ativit\u00e9 peut ouvrir de nouvelles voies \u00e0 l’innovation en recherche’, et a assur\u00e9 : ‘Nous continuerons de soutenir les chercheurs afin qu’ils puissent oser d\u00e9passer les cadres existants pour cr\u00e9er de nouveaux concepts et explorer des territoires inconnus.’<\/p>\n

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L’\u00e9quipe pr\u00e9voit d’\u00e9tendre la strat\u00e9gie d’\u00e9dition de cycle qu’elle a mise au point \u00e0 divers cycles h\u00e9t\u00e9roaromatiques azot\u00e9s autres que la pyridine. On s’attend ainsi \u00e0 pouvoir constituer rapidement, sans synth\u00e8se totale distincte, les biblioth\u00e8ques d’isom\u00e8res de position n\u00e9cessaires au d\u00e9veloppement de nouveaux m\u00e9dicaments, et \u00e0 acc\u00e9l\u00e9rer les \u00e9tudes sur les relations structure-activit\u00e9 (SAR).<\/p>\n

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\uc9c0\uc5ed \ud64d\ubcf4\ub300\uc0ac \uc2e0\uccad<\/a> <\/span> \uae30\uc790\uc591\uc131\uacfc\uc815 \uc2e0\uccad<\/a> <\/span> \ucf54\ub9ac\uc548\ud22c\ub370\uc774 \uc9c0\ubd80\uc7a5 \uc2e0\uccad<\/a> <\/span> \ucf54\ub9ac\uc548\ud22c\ub370\uc774 \uc778\ucc9c\uac15\ud654\ucf54\ub9ac\uc548\ube0c\ub79c\ub4dc\ub300\uc0c1 \uc2e0\uccad<\/a> \ucd5c\uace0\uacbd\uc601\uc778\ub300\uc0c1 \uc2e0\uccad<\/a> \uc18c\ube44\uc790\ub9cc\uc871\ub3c4\ub300\uc0c1 \uc2e0\uccad<\/a> <\/p>\n

\ud83d\udcf0 \uae30\uc0ac \uc6d0\ubb38 \ubcf4\uae30<\/a><\/p>\n

<\uc800\uc791\uad8c\uc790 \u24d2 \ucf54\ub9ac\uc548\ud22c\ub370\uc774(The Korean Today) \ubb34\ub2e8\uc804\uc7ac \ubc0f \uc7ac\ubc30\ud3ec \uae08\uc9c0><\/p>\n","protected":false},"excerpt":{"rendered":"

  Une nouvelle m\u00e9thode de synth\u00e8se permettant de modifier ais\u00e9ment la structure des compos\u00e9s pyridiniques, les plus largement utilis\u00e9s dans les m\u00e9dicaments, a \u00e9t\u00e9 mise … Read more<\/a><\/p>\n","protected":false},"author":43,"featured_media":-999999,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"fifu_image_url":"https:\/\/www.thekorean.today\/imgdata\/smilestory_kr\/202608\/2026081847475781.png","fifu_image_alt":"","footnotes":""},"categories":[35],"tags":[257],"class_list":["post-82038","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-society","tag-257","resize-featured-image"],"yoast_head":"\nL'IBS met au point une technique d'\u00e9dition mol\u00e9culaire ... - \ucf54\ub9ac\uc548\ud22c\ub370\uc774<\/title>\n<meta name=\"description\" content=\"Une nouvelle m\u00e9thode de synth\u00e8se permettant de modifier ais\u00e9ment la structure des 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