{"title":"Large‐Scale Synthesis","authors":"K. P. Cole","doi":"10.1002/0471266949.bmc032.pub3","DOIUrl":"https://doi.org/10.1002/0471266949.bmc032.pub3","url":null,"abstract":"","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72920456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
C. Caffrey, D. Steverding, R. S. Ferreira, R. B. Oliveira, A. O’Donoghue, Ludovica Monti, C. Ballatore, K. Bachovchin, Lori Ferrins, M. Pollastri, Kimberley M. Zorn, Daniel H. Foil, A. Clark, M. Mottin, C. Andrade, J. Siqueira-Neto, S. Ekins
{"title":"Drug Discovery and Development for Kinetoplastid Diseases","authors":"C. Caffrey, D. Steverding, R. S. Ferreira, R. B. Oliveira, A. O’Donoghue, Ludovica Monti, C. Ballatore, K. Bachovchin, Lori Ferrins, M. Pollastri, Kimberley M. Zorn, Daniel H. Foil, A. Clark, M. Mottin, C. Andrade, J. Siqueira-Neto, S. Ekins","doi":"10.1002/0471266949.BMC235.PUB2","DOIUrl":"https://doi.org/10.1002/0471266949.BMC235.PUB2","url":null,"abstract":"We review the disease, biology and biochemistry of kinetoplastids, as well as the new drugs and drug candidates that have entered the clinic in the last decade. We also describe examples of the pre-clinical exploration of small molecules against various protein targets, (e.g., cysteine proteases, the proteasome and tubulin), as well as cutting-edge molecular and computational strategies, and technologies being brought to bear to discover and develop new anti-trypanosomal drugs. For comprehensive descriptions of the disease, biology and drug therapies prior to 2011, the reader is encouraged to review the chapter by P.M. Woster that appeared in 2010 in the seventh edition of Burger’s Medicinal Chemistry, Drug Discovery, and Development, with the title Antiprotozoal/Antiparasitic Agents.","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"67 1","pages":"1-79"},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90397279","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"New and Emerging Antiepileptic Drugs","authors":"J. Witkin, L. Golani, Jodi L. Smith","doi":"10.1002/0471266949.bmc099.pub3","DOIUrl":"https://doi.org/10.1002/0471266949.bmc099.pub3","url":null,"abstract":"","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84457676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Drug Discovery Beyond the Rule of Five","authors":"D. DeGoey, Philip B Cox","doi":"10.1002/0471266949.BMC258","DOIUrl":"https://doi.org/10.1002/0471266949.BMC258","url":null,"abstract":"","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"29 4","pages":"1-35"},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72561329","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Health Outcomes Research","authors":"P. McCollam, J. Birt, Theresa Hunter","doi":"10.1002/0471266949.BMC257","DOIUrl":"https://doi.org/10.1002/0471266949.BMC257","url":null,"abstract":"","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83240351","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Ion Channels as Therapeutic Drug Targets","authors":"M. L. García, G. Kaczorowski","doi":"10.1002/0471266949.BMC255","DOIUrl":"https://doi.org/10.1002/0471266949.BMC255","url":null,"abstract":"","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"6 1","pages":"1-28"},"PeriodicalIF":0.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89066324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Medicinal Chemical Biology","authors":"L. Jones","doi":"10.1002/0471266949.bmc256","DOIUrl":"https://doi.org/10.1002/0471266949.bmc256","url":null,"abstract":"activity genetic profiling of resistant mutants that emerged following prolonged incubation of the lead compound with replicon cells A biotinylated derivative was used to affinity isolate NS5A, and streptavidin-mediated enrichment was competed by the presence of the parent compound confirm the specificity of target engagement. This work led to the development of the drug daclatasvir, an NS5A inhibitor for the treatment of HCV To further validate","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79560055","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The Blood–Brain Barrier and CNS Drug Delivery","authors":"W. Banks","doi":"10.1002/0471266949.BMC285","DOIUrl":"https://doi.org/10.1002/0471266949.BMC285","url":null,"abstract":"The blood–brain barriers (BBBs) act as the guardians and as the slaves to the rest of the central nervous system (CNS). By preventing the unrestricted leakage typical of most capillary beds, the vascular BBB then engages in CNS-blood exchanges that are largely regulated in ways not typical in other tissue beds. Thus, the BBBs are not simply barriers, but interfaces that are also endowed with roles that include nutrition, homeostasis, and communication [1]. The barriers adapt to the needs of the CNS, changing with maturation, aging, and in response to environmental challenges. The barriers also adapt or attempt to do so in the face of pathological states and can themselves be the target or the cause of diseases, both peripheral and central. This varied and complex interface provides the basis for a nuanced approach to drug delivery to the CNS. An understanding of the underlying ways in which the BBBs make their livings and serve the CNS provide many different rational approaches to the development of therapeutics that can influence the CNS. As this article will illustrate, these strategies typically involve the delivery of substances from the blood to the brain. But this article will also consider other viable approaches which in some cases do not require the xenobiotic to cross the BBB, such as the blockade of substances that would otherwise cross the BBB (resulting in an antagonist effect), the induction of the release of secondary agents from the abluminal side of barrier tissues, and the modulation of transporter functions. The vascular BBB, in general, and its use in CNS drug delivery in particular is a poorly studied area. Yet, it is much better understood than the other barrier systems, such as the blood-cerebrospinal fluid barrier (BCSFB), the tanycytic barrier, or the blood–retinal barrier. As such, most of this article will emphasize the vascular barrier. However, these other barriers likely follow similar concepts and, with further study, will yield treasure troves of mechanisms and pathways unique to them and useful for the development of therapeutic agents that impact the CNS.","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"92 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80370675","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. Wolkenberg, Abdellatif El Marrouni, A. Converso, D. Tellers, Richard J. O. Barnard, Tracy L. Diamond
{"title":"Current Status of Approaches to Eradicate\u0000 HIV\u0000 Infection","authors":"S. Wolkenberg, Abdellatif El Marrouni, A. Converso, D. Tellers, Richard J. O. Barnard, Tracy L. Diamond","doi":"10.1002/0471266949.bmc281","DOIUrl":"https://doi.org/10.1002/0471266949.bmc281","url":null,"abstract":"proteins that have shown higher levels of T-cell expression in HIV + patients compared to negative controls [181, 182]. In vitro studies show","PeriodicalId":9514,"journal":{"name":"Burger's Medicinal Chemistry and Drug Discovery","volume":"50 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87841901","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}