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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.
This article was published in the following journal.
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...
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...
Perioperative blood management is essential to minimize allogeneic blood transfusion in total knee replacement. The effect of preoperative administration of erythropoietin, intraoperative cell saver, ...
Experiencing loss of appetite after cardiac surgery is often noted during daily care and has been described by several studies. However, no information is available on either energy needs or spontaneo...
To explore the effect of ulinastatin on perioperative glycocalyx and lung function in patients undergoing mitral valve replacement surgery. Methods: Fourty patients, undergoing mitral valve replace...
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...
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 ...
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 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...
The purpose of this study is to determine whether meal replacement, SlimWell ®, is effective in the treatment of obesity patients with metabolic syndrome.
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.
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...