Webb8 aug. 2012 · In addition, some strategies for drug discovery based on the bioisostere concept are introduced. Many bioisosteres, which are recognized by corresponding … Webb25 okt. 2024 · Tetrazoles have been widely studied for their biological properties. An efficient route for large-scale synthesis of 1,5-disubstituted tetrazoles (1,5-DTs) is presented. The strategy exploits a reductive approach to synthetize a cyclic chiral imine substrate which is then converted into the target product through an Ugi-azide three …

Simple strategy towards amide bioisosteres Nature Chemistry

Webb6 nov. 2024 · As such, bioisosteres contribute to the field of medicinal chemistry, in terms of improving potency, enhancing selectivity, altering physicochemical properties, … Webb10 nov. 2016 · BIOISOSTERSM 1. BIOISOTERISM:A useful strategy for drug design 1 2. In medicinal chemistry, bioisosteres are chemical substituents or groups with similar … cra new sin number mb

Drug design principles - Stereoelectronics

Webb15 sep. 2024 · Therefore, isosteric replacement of the amide group has been widely adopted as a fundamental tactical approach in medicinal chemistry for the design of new drugs.1 The success of this strategy in identifying new biologically active molecules in distinct therapeutic areas has gained a significant growth. Webb8 maj 2024 · This analysis of the spatial and electronic differences between the amide and 1,2,3-triazole will inform medicinal chemists as they consider using the triazole as an amide bioisostere. Conflict of interest The authors declare no conflict of interest. Citing Literature Supporting Information Volume 15, Issue 18 September 16, 2024 Pages 1720-1730 WebbIf you're trying to find bioisosteres for -NH 3+, I can think up a few possibilities. The first that comes to mind is to fluoronate it to -NF 3+, which would preserve the cationic quaternary... cra new smyrna beach