Francisco, Karol R. published the artcileStructure property relationships of N-acylsulfonamides and related bioisosteres, Application of (S)-2-Methylpropane-2-sulfinamide, the main research area is acylsulfonamide structure property relationship bioisostere; Bioisostere; Isosteric replacement; N-Acylsulfonamide isostere; Oxetane; Physicochemical properties; Structure property relationship (SPR); Thietane.
The N-acylsulfonamide functional group is a feature of the pharmacophore of several biol. active mols., including marketed drugs. Although this acidic moiety presents multiple points of attachments that could be exploited to introduce structural diversification, depending on the circumstances, the replacement of the functional group itself with a suitable surrogate, or bioisostere, may be desirable. A number of N-acylsulfonamide bioisosteres have been developed over the years that provide opportunities to modulate both structure and physicochem. properties of this important structural motif. To enable an assessment of the relative impact on physicochem. properties that these replacements may have compared to the N-acylsulfonamide group, we conducted a structure-property relationship study based on matched mol. pairs, in which the N-acylsulfonamide moiety of common template reference structures is replaced with a series of bioisosteres. The data presented, which include an assessment of relative changes in acidity, permeability, lipophilicity and intrinsic solubility, provides a basis for informed decisions when deploying N-acylsulfonamides, or surrogates thereof, in analog design.
European Journal of Medicinal Chemistry published new progress about Biological permeation (artificial membrane permeability assay). 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Application of (S)-2-Methylpropane-2-sulfinamide.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics