PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold.

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Research Abstract Details 

Research Abstract Table of Contents

Jump to the:

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Abstract Text:

We have synthesized and evaluated a series of triaryl sulfonamide-based PTP1B inhibitors in which a difluoro-methylenephosphonate group of a potent lead has been replaced by potential bioisosteric replacements. Several mono- or di-charged compounds (8a, 8b, and 15a) were shown exhibit inhibitory activity in the low micromolar range, demonstrating the feasibility of using this approach in identifying non-phosphonate pTyr mimetics in a small molecular scaffold. These results also provide a useful indication of the relative effectiveness of these pTyr mimetics.

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Publishing Authors By Initials

For similar abstracts research abstracts see: abstracts research

PUBMED ID PMID:

MEDLINE DATE:

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 2719-24

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 6

MONTH: 03

YEAR: 2008

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9107377

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Keywords Mesh Terms:

KEYWORDS:

MESH TERMS:

Chemical & Substance for Abstract: PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold. Information

Substance Name:

Registry Number:

Grant and Affiliation Information for PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold.

AFFILIATION: Affymax, Inc., 4001 Miranda Avenue, Palo Alto, CA 94304, USA. chris_holmes@affymax.com

Country: England

AGENCY:

GRANT:

ACRONYM:

MEDLINETA: Bioorg Med Chem Lett

REFSOURCE:

DATABASENAME:

ACCESSION NUMBER:

Number Hits: 0

PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold Related Publications

• Blindness control in Canada.
• Characterization of brainstem peptide YY (PYY) neurons.
• Development of a laboratory model gas analyzer using emission techniques. MRL-TR-68-130.
• Dimensional analyses of taxonic data.
• Early acute aseptic iritis after cataract extraction.
• Educating the public to prevent dental disease.
• Effect of chronic alcohol use on smooth pursuit eye movements.
• Excess weight gain during the early postnatal period is associated with permanent reprogramming of brown adipose tissue adaptive thermogenesis.
• Listening to the silence: doing better at responding to disasters.
• Melanocortinergic activation by melanotan II inhibits feeding and increases uncoupling protein 1 messenger ribonucleic acid in the developing rat.
• Mercury and drought along the lower Carson River, Nevada: II. Snowy egret and black-crowned night-heron reproduction on Lahontan Reservoir, 1997-2006.
• Modeling residential lawn fertilization practices: integrating high resolution remote sensing with socioeconomic data.
• Neuroscience. Organizing the source of memory.
• New diagnostic techniques for the evaluation of orbital trauma.
• Noise; will it damage your hearing?
• PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold.
• Patterning the dorsal telencephalon: a role for sonic hedgehog?
• Predicting Sex Offender Recidivism. I. Correcting for Item Overselection and Accuracy Overestimation in Scale Development. II. Sampling Error-Induced Attenuation of Predictive Validity Over Base Rate Information.
• Quantitative determination of dihydrostreptomycin by periodate oxidation.
• Self-sacrifice in radical S-adenosylmethionine proteins.
• Some catalyzed gas-phase reactions of aromatic hydrocarbons; the methylation of naphthalene by means of dimethyl ether.
• Strongyloidiasis in Allied ex-prisoners of war in south-east Asia.
• The derivatives of the Wnt3a lineage in the central nervous system.
• The effects of exercise and nicotine replacement therapy on smoking rates in women.
• The importance of sinusitis in allergic manifestations.
• The noise hazard.
• Total synthesis of (-)-salviasperanol.
• Turning neurons into a nervous system.
• Will noise damage one's hearing?
• [Factors concerning disease and health as seen by a physician]