In situ Click chemistry. Mgr. Juraj Dobia š KOCH, PRIF UK . What is Click Chemistry ?. joining molecules by an „ ideal chemical reaction “ fast, irreversible reaction, simple conditions starting materials are readily available, stable (biocompatible )
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KOCH, PRIF UK
joining molecules by an „ideal chemical reaction“
2002, Fokin, SharplessMelda
MMP7 selective, low mcM inhibitors
Org. Lett. 8 2006 3821-24.
TDS reduces the number of inactive compounds
Compensate the lack of precision in the predictive ability of in Silico chemistry
In situ AA Click chemistry is completely biocompatible, uses irreversible reaction to unite reagents inside the protein´s binding pocket
Target will pick best fitting ligandsfrom diverse sets of chemical building blocks
Significant portion of the activation barrier is entropic(pieces have to approach each other in precisely the right orientation), pre-assembly of building blocks on the target active site can accelerate cycloaddition.
DDT 9 2004 348.
2013 PNAS 110 15892-97