Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.

Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor. Research Abstract Details 

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Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor. Abstract Text:

Michael C Myers,Parag P Shah,Scott L Diamond,Donna M Huryn,Amos B Smith,Michael C Myers,Parag P Shah,Scott L Diamond,Donna M Huryn,Amos B Smith,

Library samples containing 2,5-disubstituted oxadiazoles were identified as potent hits in a high throughput screen (HTS) of the NIH Molecular Libraries Small Molecule Repository (MLSMR) directed at discovering inhibitors of cathepsin L. However, when synthesized in pure form, the putative actives were found to be devoid of biological activity. Analyses by LC-MS of original library samples indicated the presence of a number of impurities, in addition to the oxadiazoles. Synthesis and bioassay of the probable impurities led to the identification of a thiocarbazate that likely originated via ring opening of the oxadiazole. Previously unknown, thiocarbazates (-)-11 and (-)-12 were independently synthesized as single enantiomers and found to inhibit cathepsin L in the low nanomolar range.

Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor. Publishing Authors By Initials

MC Myers,PP Shah,SL Diamond,DM Huryn,AB Smith,MC Myers,PP Shah,SL Diamond,DM Huryn,AB Smith,

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Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 210-4

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 1

MONTH: 11

YEAR: 2007

Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.

AFFILIATION: Penn Center for Molecular Discovery, University of Pennsylvania, 1024 Vagelos Research Laboratories, Philadelphia, PA 19104-6383, USA.

Country: England

AGENCY: United States NHGRI

GRANT: 5U54HG003915-03

ACRONYM: HG

MEDLINETA: Bioorg Med Chem Lett

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