Synthesis and biological evaluation of non-peptidic cyclophilin ligands.

Autor: Wu YQ; Department of Research, Guilford Pharmaceuticals, Inc., 6611 Tributary Street, Baltimore, Maryland 21224, USA. wuy@guilfordpharm.com, Belyakov S, Choi C, Limburg D, Thomas IV BE, Vaal M, Wei L, Wilkinson DE, Holmes A, Fuller M, McCormick J, Connolly M, Moeller T, Steiner J, Hamilton GS
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2003 Mar 27; Vol. 46 (7), pp. 1112-5.
DOI: 10.1021/jm020409u
Abstrakt: Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through "virtual screening" and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.
Databáze: MEDLINE