Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides.

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Wei L, Wu Y, Wilkinson DE, Chen Y, Soni R, Scott C, Ross DT, Guo H, Howorth P, Valentine H, Liang S, Spicer D, Fuller M, Steiner J, Hamilton GS

Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides.

Bioorg Med Chem Lett. 2002 May 20;12(10):1429-33.

PubMed ID

11992791 [ View in PubMed

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Abstract

In parallel with our work on solution-phase parallel synthesis of ligands for the rotamase enzyme FKBP12, we herein report a methodology for the solid-phase synthesis of two classes of inhibitor, N-sulfonyl and N-carbamoylprolyl and pipecolyl amides along with their in vitro/in vivo biological results.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Gpi-1046	Peptidyl-prolyl cis-trans isomerase FKBP1A	Ki (nM)	0.01	N/A	N/A	Details