Thietanes and Derivatives thereof in Medicinal Chemistry

KR Francisco, C Ballatore - Current Topics in Medicinal …, 2022 - ingentaconnect.com
… of the carboxylic acid moiety of 36 with a corresponding oxetan-3-ol (37) or thietan-3-ol (38) …
Preclinical characterization of acyl sulfonimidamides: Potential carboxylic acid bioisosteres

Carboxylic acid bioisosteres in medicinal chemistry: synthesis and properties

K Bredael, S Geurs, D Clarisse… - Journal of …, 2022 - Wiley Online Library
… the systematic assessment of carboxylic acid bioisosteres of the … or when the design of
derivatives that do not enter the CNS is … The oxetan-3-ol and thietan-3-ol rings and corresponding …

Recent developments in the practical application of novel carboxylic acid bioisosteres

C Horgan, TP O'Sullivan - Current Medicinal Chemistry, 2022 - ingentaconnect.com
… This review focuses on carboxylic acid bioisosteres that have emerged in the subsequent …
meable than carboxylic acid 114. In fact, the oxetan-3ol and thietan-3-ol derivatives displayed …

Structure property relationships of N-acylsulfonamides and related bioisosteres

KR Francisco, C Varricchio, TJ Paniak… - European journal of …, 2021 - Elsevier
bioisosteres in analog design, an assessment of the relative … possible bioisosteric relationships
of these derivatives have … in earlier SPR studies of carboxylic acid bioisosteres [26,41], …

Oxetanes in drug discovery campaigns

JJ Rojas, JA Bull - Journal of Medicinal Chemistry, 2023 - ACS Publications
… and evaluated to some extent versus carboxylic acids, … include the introduction of the carboxylic
acid, which reduced … at Roche on oxetanes as bioisosteres of gem-dimethyl and carbonyl …

[HTML][HTML] Structure-property relationships of fluorinated carboxylic acid bioisosteres

T Alle, S Joyasawal, K Oukoloff, K Long… - Bioorganic & medicinal …, 2023 - Elsevier
… To circumvent this problem, in this study we evaluate model … phenylpropionic acid
derivatives bearing carboxylic acid … , B2), oxetan-3-ol (Y), thietane-3-ol (X1, X2), or acylurea (J) …

[图书][B] Structure Activity and Structure Property Relationships of Small Molecules as Research Tools and Candidate Therapeutics

KRK Francisco - 2022 - search.proquest.com
… and physicochemical evaluation of a series of N-acylsulfonamides and related bioisosteres.
The … of AII receptor antagonist carboxylic acid 1 and its tetrazole bioisostere, losartan 2. One …

NMR quantification of H-bond donating ability for bioactive functional groups and isosteres

JJ Jennings, M Milic, K Targos, AK Franz - European Journal of Medicinal …, 2020 - Elsevier
… to medicinal chemistry were evaluated including carboxylic acids, … Additionally, 31 P NMR
binding data for carboxylic acid … This method has been used to evaluate the H-bond donating …

The role of organic small molecules in pain management

SA Cuesta, L Meneses - Molecules, 2021 - mdpi.com
… Some studies suggest that carboxylic acid is key for binding, but it is also linked to gastrotoxicity.
In this sense, oxetan-3-ol and thietan-3-ol appear to be interesting bioisosteres in COX …

Second generation inhibitors of HIV-1 maturation

A Regueiro-Ren, IB Dicker… - ACS Medicinal …, 2019 - ACS Publications
… to a carboxylic acid, was not burdened with an overt negative charge. This reflects a bioisosteric
… A comprehensive evaluation of the PK profile of 21 in preclinical species is compiled in …