On drug discovery against infectious diseases and academic medicinal chemistry contributions
This perspective is an attempt to document the problems that medicinal chemists are facing in drug discovery. It is also trying to identify relevant/possible, research areas in which academics can have an impact and should thus be the subject of grant calls. Accordingly, it describes how hit discove...
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| Format: | Article |
| Language: | English |
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Beilstein-Institut
2022-09-01
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| Series: | Beilstein Journal of Organic Chemistry |
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| Online Access: | https://doi.org/10.3762/bjoc.18.141 |
| _version_ | 1817980295213744128 |
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| author | Yves L. Janin |
| author_facet | Yves L. Janin |
| author_sort | Yves L. Janin |
| collection | DOAJ |
| description | This perspective is an attempt to document the problems that medicinal chemists are facing in drug discovery. It is also trying to identify relevant/possible, research areas in which academics can have an impact and should thus be the subject of grant calls. Accordingly, it describes how hit discovery happens, how compounds to be screened are selected from available chemicals and the possible reasons for the recurrent paucity of useful/exploitable results reported. This is followed by the successful hit to lead stories leading to recent and original antibacterials which are, or about to be, used in human medicine. Then, illustrated considerations and suggestions are made on the possible inputs of academic medicinal chemists. This starts with the observation that discovering a “good” hit in the course of a screening campaign still rely on a lot of luck – which is within the reach of academics –, that the hit to lead process requires a lot of chemistry and that if public–private partnerships can be important throughout these stages, they are absolute requirements for clinical trials. Concerning suggestions to improve the current hit success rate, one academic input in organic chemistry would be to identify new and pertinent chemical space, design synthetic accesses to reach these and prepare the corresponding chemical libraries. Concerning hit to lead programs on a given target, if no new hits are available, previously reported leads along with new structural data can be pertinent starting points to design, prepare and assay original analogues. In conclusion, this text is an actual plea illustrating that, in many countries, academic research in medicinal chemistry should be more funded, especially in the therapeutic area neglected by the industry. At the least, such funds would provide the intensive to secure series of hopefully relevant chemical entities which appears to often lack when considering the results of academic as well as industrial screening campaigns. |
| first_indexed | 2024-04-13T22:52:32Z |
| format | Article |
| id | doaj.art-a1033dcbdd2443598749efea074ba5dc |
| institution | Directory Open Access Journal |
| issn | 1860-5397 |
| language | English |
| last_indexed | 2024-04-13T22:52:32Z |
| publishDate | 2022-09-01 |
| publisher | Beilstein-Institut |
| record_format | Article |
| series | Beilstein Journal of Organic Chemistry |
| spelling | doaj.art-a1033dcbdd2443598749efea074ba5dc2022-12-22T02:26:08ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972022-09-011811355137810.3762/bjoc.18.1411860-5397-18-141On drug discovery against infectious diseases and academic medicinal chemistry contributionsYves L. Janin0Structure et Instabilité des Génomes (StrInG), Muséum National d'Histoire Naturelle, INSERM, CNRS, Alliance Sorbonne Université, 75005 Paris, France This perspective is an attempt to document the problems that medicinal chemists are facing in drug discovery. It is also trying to identify relevant/possible, research areas in which academics can have an impact and should thus be the subject of grant calls. Accordingly, it describes how hit discovery happens, how compounds to be screened are selected from available chemicals and the possible reasons for the recurrent paucity of useful/exploitable results reported. This is followed by the successful hit to lead stories leading to recent and original antibacterials which are, or about to be, used in human medicine. Then, illustrated considerations and suggestions are made on the possible inputs of academic medicinal chemists. This starts with the observation that discovering a “good” hit in the course of a screening campaign still rely on a lot of luck – which is within the reach of academics –, that the hit to lead process requires a lot of chemistry and that if public–private partnerships can be important throughout these stages, they are absolute requirements for clinical trials. Concerning suggestions to improve the current hit success rate, one academic input in organic chemistry would be to identify new and pertinent chemical space, design synthetic accesses to reach these and prepare the corresponding chemical libraries. Concerning hit to lead programs on a given target, if no new hits are available, previously reported leads along with new structural data can be pertinent starting points to design, prepare and assay original analogues. In conclusion, this text is an actual plea illustrating that, in many countries, academic research in medicinal chemistry should be more funded, especially in the therapeutic area neglected by the industry. At the least, such funds would provide the intensive to secure series of hopefully relevant chemical entities which appears to often lack when considering the results of academic as well as industrial screening campaigns.https://doi.org/10.3762/bjoc.18.141antibacterialsfrequent hittershit to lead chemical librarymedicinal chemistryvirtual docking |
| spellingShingle | Yves L. Janin On drug discovery against infectious diseases and academic medicinal chemistry contributions Beilstein Journal of Organic Chemistry antibacterials frequent hitters hit to lead chemical library medicinal chemistry virtual docking |
| title | On drug discovery against infectious diseases and academic medicinal chemistry contributions |
| title_full | On drug discovery against infectious diseases and academic medicinal chemistry contributions |
| title_fullStr | On drug discovery against infectious diseases and academic medicinal chemistry contributions |
| title_full_unstemmed | On drug discovery against infectious diseases and academic medicinal chemistry contributions |
| title_short | On drug discovery against infectious diseases and academic medicinal chemistry contributions |
| title_sort | on drug discovery against infectious diseases and academic medicinal chemistry contributions |
| topic | antibacterials frequent hitters hit to lead chemical library medicinal chemistry virtual docking |
| url | https://doi.org/10.3762/bjoc.18.141 |
| work_keys_str_mv | AT yvesljanin ondrugdiscoveryagainstinfectiousdiseasesandacademicmedicinalchemistrycontributions |