Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement.

08:00 EDT 7th August 2017 | BioPortfolio

Summary of "Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement."

The success of fluorinated molecules in drug design has led medicinal chemists to search for new fluorine-containing substituents. A major recently developed group is the pentafluorosulfanyl group. This group is stable under physiological conditions and displays unique physical and chemical properties. Currently, few synthetic methods exist that install the SF5 group, yet efforts to integrate this group into lead optimization continue unabated. Typically, the SF5 group has been used as a replacement for a trifluoromethyl, a tert-butyl, a halogen, or a nitro group. In this review, the use of the SF5 group as a bioisosteric replacement for each of these three functionalities will be compared and contrasted across different groups of biologically active molecules. The organization and presentation of these data are instructive to medicinal chemists considering to design synthetic strategies to access SF5 substituted molecules.


Journal Details

This article was published in the following journal.

Name: ChemMedChem
ISSN: 1860-7187


DeepDyve research library

PubMed Articles [13563 Associated PubMed Articles listed on BioPortfolio]

Adenosine analogs bearing phosphate isosteres as human MDO1 ligands.

The human O-acetyl-ADP-ribose deacetylase MDO1 is a mono-ADP-ribosylhydrolase involved in the reversal of post-translational modifications. Until now MDO1 has been poorly characterized, partly since n...

Carboxylate analogues of aryl-urea-substituted fatty acids that target the mitochondrion in MDA-MB-231 breast cancer cells to promote cell death.

Targeting of the tumor cell mitochondrion is a viable approach for the development of anti-cancer agents because the organelle differs from that in normal cells. We recently developed a novel aryl-ure...

Synthesis and biological evaluation of some N-(3-(1H-tetrazol-5-yl) phenyl)acetamide derivatives as novel non-carboxylic PTP1B inhibitors designed through bioisosteric modulation.

Described herein is the synthesis and biological evaluation of a series of non-carboxylic inhibitors of Protein Tyrosine Phosphatase 1B designed using bioisosteric replacement strategy. Six N-(3-(1H-t...

Application of vascular replacement technique with allogenic blood vessel in radical resection for pancreatic carcinoma: a report of 33 cases.

To analyze the application of vascular replacement technique with allogenic blood vessel in radical resection for pancreatic carcinoma.The clinical data of 33 patients with vascular invasion of pancre...

Estrogen replacement enhances insulin-induced AS160 activation and improves insulin sensitivity in ovariectomized rats.

Menopause predisposes women to impaired glucose metabolism, but the role of estrogen remains unclear. In this study, we examined the effects of chronic estrogen replacement on whole-body insulin sensi...

Clinical Trials [7662 Associated Clinical Trials listed on BioPortfolio]

Short- Versus Long-duration Tourniquet Use During Total Knee Replacement (TKR)

To establish whether a short duration of tourniquet application (from cement fixation to cement setting)is associated with better patient functional outcomes compared to a long duration of...

To Determine the Effects of Deodorant, Antiperspirant and Washing on the Pharmacokinetics of 2% Testosterone MD Lotion

Testosterone replacement treatment is the most effective way of treating hypogonadism in men. Acrux has a propriety testosterone replacement product, Testosterone MD-Lotion and this ...

Benchmarking the iOS Balance Application Against the Berg Balance Test

This study aims to benchmark the performance of an iOS application against the Berg Balance Scale (BBS), which is the most commonly used assessment tool by clinicians for measuring balance...

The Clinical Observation on Taping After Total Knee Replacement

The investigators will conduct a single-blind, randomized controlled trial of 100 patients with total knee replacement. Patients will be randomly assigned into a control group and an inter...

Effect of a Meal Replacement on Weight Loss Obesity Patients With Metabolic Syndrome

The purpose of this study is to determine whether meal replacement, SlimWell ®, is effective in the treatment of obesity patients with metabolic syndrome.

Medical and Biotech [MESH] Definitions

Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)

A group of conditions due to overexposure to or overexertion in excess environmental temperature. It includes heat cramps, which are non-emergent and treated by salt replacement; HEAT EXHAUSTION, which is more serious, treated with fluid and salt replacement; and HEAT STROKE, a condition most commonly affecting extremes of age, especially the elderly, accompanied by convulsions, delusions, or coma and treated with cooling the body and replacement of fluids and salts. (From Segen, Dictionary of Modern Medicine, 1992)

Therapeutic replacement or supplementation of defective or missing enzymes to alleviate the effects of the enzyme deficiency (e.g., GLUCOSYLCERAMIDASE replacement for GAUCHER DISEASE).

Partial or total replacement of a joint.

Replacement of the hip joint.

Quick Search


DeepDyve research library

Relevant Topic

Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Searches Linking to this Article