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The proof of the pudding: A proof-of-concept study using γ-secretase inhibitors as a model has shown that sulfonimidamides act as bioisosteres for sulfonamides. Detailed in vitro and in vivo profiling reveal that the sulfonimidamide motif imparts desirable properties such as decreased lipophilicity and plasma protein binding, accompanied by increased solubility. Our data support a wider use of this unique functional group in the design of new pharmacologically active agents.
Medicinal Chemistry, iScience, CNSP iMed, AstraZeneca R&D Södertälje, Västra Mälarehamnen 9, 151 85 Södertälje (Sweden).
This article was published in the following journal.
Sulfonamide antibiotics have been frequently detected in the aquatic environment and are of emerging concern due to their adverse bio-effect and potential of inducing antibiotic resistance. This study...
An intermolecular alkylation of sulfonamides with trichloroacetimidates is reported. This transformation does not require an exogenous acid, base, or transition metal catalyst, instead the addition oc...
A series of N(1)-substituted aromatic sulfonamides was obtained by applying a selective sulfonamide nitration synthetic strategy leading to Ar-SO2NHNO2 derivatives which were investigated as carbonic ...
A novel modification of piperlongumine is designed, bearing a cyclic sulphonamide (sultam) and its synthesis is described. For the first time herein we report the synthesis and biological evaluation o...
We have developed a simple and convenient method for the cross-coupling of arylboronic acids and their derivatives with DAST-type reagents under mild and metal-free conditions to directly afford sulfi...
Subjects are healthy adult volunteers either at high risk for HIV infection or already known to be seropositive, who will donate blood for in vitro tests of T-cell function and in vitro re...
To compare the safety and efficacy of aerosolized pentamidine and dapsone in the prevention of Pneumocystis carinii pneumonia (PCP) in high-risk HIV-infected patients who are intolerant to...
Oxytocin is normally administered following delivery in pregnant patients to reduce postpartum bleeding by increasing uterine tone. It is unclear whether the use of intravenous oxytocin al...
Continuous albuterol has become the standard of care for patients in status asthmaticus. We have previously performed an in-vitro study comparing 4 different brands of continuous nebulizer...
Methods of infertility treatment may involve in vitro fertilization or IVF. Though effective, IVF is complex and expensive. Methods using no gonadotropin hormone stimulation of the ovaries...
Biologically functional sequences of DNA chemically synthesized in vitro.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Synthetic transcripts of a specific DNA molecule or fragment, made by an in vitro transcription system. This cRNA can be labeled with radioactive uracil and then used as a probe. (King & Stansfield, A Dictionary of Genetics, 4th ed)
Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.
Studies designed to assess the efficacy of programs. They may include the evaluation of cost-effectiveness, the extent to which objectives are met, or impact.
Blood is a specialized bodily fluid that delivers necessary substances to the body's cells (in animals) – such as nutrients and oxygen – and transports waste products away from those same cells. In vertebrates, it is composed of blo...