WebIn summary, we investigated whether a thiophene ring can become a bioisostere for a benzene ring for fungicidal activity against plant pathogens in vivo and in vitro. We also evaluated the inhibitory activity at the action site. Two of the thiophene regioisomers could act as bioisosteres for the benzene ring, whereas one isomer could not. WebFeb 1, 2005 · In this paper, we will discuss bioisosterism as a strategy of molecular modification, showing its importance in building a new series of congeners compounds designed as candidate of new drugs,...
BoBER: web interface to the base of bioisosterically exchangeable ...
WebThiophene, like furan is more reactive towards electrophiles than benzene. Because of its relatively high aromatic character, substitution products predominate over addition … WebJan 10, 2024 · Thiophene bioisosteres of potent GluN2B receptor negative allosteric modulators were prepared and evaluated pharmacologically. The five-step synthesis of … mydailydose.com
Current Medicinal Chemistry, 23-49 23 Bioisosterism: A Useful …
WebThienopyrimidines (TP), comprising a thiophene ring fused with pyrimidine, are famous bioisosteres to purines, an essential part of the human metabolome. WebJan 15, 2024 · Thiophene bioisosteres of potent GluN2B receptor negative allosteric modulators were prepared and evaluated pharmacologically. The five-step synthesis of 4,5,7,8-tetrahydro [7]annuleno [b]thiophen-6-one (10) was considerably improved by carboxylation of thiophene-3-carboxylic acid (8) in the first reaction step. The trifluoromethyl oxetane has been evaluated as a tert‐butyl isostere DOI. It was demonstrated that the trifluoromethyl oxetane‐containing had decreased lipophilicity, improved lipophilic efficiency (LipE) and metabolic stability relative to the corresponding tert‐butyl analogue. They were prepared from the … See more Perhaps the most conservative is the replacement of hydrogen by deuterium, whilst the change does have a minor impact on the physicochemical properties the change is usually … See more Some molecules contain a stereocentre that epimerises in vitro and/or in vivo, in these cases replacement of the of the acidic proton with … See more The replacement of carbon by silicon is a relatively recent exploration and whilst this does appear to be a relatively benign conversion it may be the introduction of silicon is to offer … See more In an similar replacement of one or more hydrogens by Fluorine has been used to modulate metabolism or off-target activity. Fluorine can be used to modulate the pka of a basic nitrogen, … See more office online server aws