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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.
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...
Highly electron-withdrawing pentafluorosulfanyl groups were probed as substituents in an organometallic catalyst. In Ni(II) salicylaldiminato complexes as an example case, these highly electron-withdr...
The interrupted noneverting mattress suture technique is typically used in conventional surgical aortic valve replacement. The continuous suture technique, although faster, has been associated with a ...
The electronic properties and relatively small size of fluorine endow it with considerable versatility as a bioisostere and it has found application as a substitute for lone pairs of electrons, the hy...
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...
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...