Recent developments in the practical application of novel carboxylic acid bioisosteres

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dc.check.date2023-01-03
dc.check.infoAccess to this article is restricted until 12 months after publication by request of the publisher.en
dc.contributor.authorHorgan, Conor
dc.contributor.authorO'Sullivan, Timothy P.
dc.contributor.funderIrish Research Councilen
dc.date.accessioned2022-05-25T08:38:57Z
dc.date.available2022-05-25T08:38:57Z
dc.date.issued2022-01-03
dc.date.updated2022-05-25T08:25:21Z
dc.description.abstractBackground: The carboxylic acid moiety is an important functional group which features in the pharmacophore of some 450 drugs. Unfortunately, some carboxylic acid-containing drugs have been withdrawn from market due to unforeseen toxicity issues. Other issues associated with the carboxylate moiety include reduced metabolic stability or limited passive diffusion across biological membranes. Medicinal chemists often turn to bioisosteres to circumvent such obstacles. Objective: The aim of this review is to provide a summary of the various applications of novel carboxylic acid bioisosteres which have appeared in the literature since 2013. Results: We have summarised the most recent developments in carboxylic acid bioisosterism. In particular, we focus on the changes in bioactivity, selectivity or physicochemical properties brought about by these substitutions, as well as the advantages and disadvantages of each isostere. Conclusion: The topics discussed herein highlight the continued interest in carboxylate bioisosteres. The development of novel carboxylic acid substitutes which display improved pharmacological profiles is a testament to the innovation and creativity required to overcome the challenges faced in modern drug design.en
dc.description.sponsorshipIrish Research Council (Government of Ireland Postgraduate Research Scholarship GOIPG/2017/1111)en
dc.description.statusPeer revieweden
dc.description.versionAccepted Versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.citationHorgan, C. and O'Sullivan, T. P. (2022) 'Recent developments in the practical application of novel carboxylic acid bioisosteres', Current Medicinal Chemistry, 29(13). doi: 10.2174/0929867328666210820112126en
dc.identifier.doi10.2174/0929867328666210820112126en
dc.identifier.eissn1875-533X
dc.identifier.issn0929-8673
dc.identifier.issued13en
dc.identifier.journaltitleCurrent Medicinal Chemistryen
dc.identifier.urihttps://hdl.handle.net/10468/13246
dc.identifier.volume29en
dc.language.isoenen
dc.publisherBentham Science Publishersen
dc.rights© 2022, Bentham Science Publishers. This is the accepted version of the following item: Horgan, C. and O'Sullivan, T. P. (2022) 'Recent developments in the practical application of novel carboxylic acid bioisosteres', Current Medicinal Chemistry, 29(13), doi: 10.2174/0929867328666210820112126. The published manuscript is available at EurekaSelect via http://www.eurekaselect.com/10.2174/0929867328666210820112126en
dc.subjectIsosteresen
dc.subjectBioisosterismen
dc.subjectCarboxylic acidsen
dc.subjectDrug designen
dc.subjectAcidityen
dc.subjectLipophilicityen
dc.titleRecent developments in the practical application of novel carboxylic acid bioisosteresen
dc.typeArticle (peer-reviewed)en
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