At 2.5 mol % loadings using reaction temperatures between 30-55 °C, ortho-functionalized diaryl diselenides are highly effective organocatalytic oxidants for aerobic redox dehydrative amidic and peptidic bond formation using triethyl phosphite as a simple terminal reductant. This simple-to-perform organocatalytic reaction relies on the ability of selenols to react directly with dioxygen in air without recourse to metal catalysts. It represents an important step toward the development of a general, economical, and benign catalytic redox dehydration protocol.

01 Jun 2016·Journal of the American Chemical SocietyQ1 · CHEMISTRY

Benzoisothiazolone Organo/Copper-Cocatalyzed Redox Dehydrative Construction of Amides and Peptides from Carboxylic Acids using (EtO)₃P as the Reductant and O₂ in Air as the Terminal Oxidant

Q1 · CHEMISTRY

Article

Author: Lindale, Matthew G. ; Liebeskind, Lanny S. ; Gangireddy, Pavankumar

Carboxylic acids and amine/amino acid reactants can be converted to amides and peptides at neutral pH within 5-36 h at 50 °C using catalytic quantities of a redox-active benzoisothiazolone and a copper complex. These catalytic "oxidation-reduction condensation" reactions are carried out open to dry air using O2 as the terminal oxidant and a slight excess of triethyl phosphite as the reductant. Triethyl phosphate is the easily removed byproduct. These simple-to-run catalytic reactions provide practical and economical procedures for the acylative construction of C-N bonds.

01 Sep 2010·Current Medicinal ChemistryQ2 · MEDICINE

Thromboxane Synthase Inhibitors and Thromboxane A2 Receptor Antagonists: A Quantitative Structure Activity Relationships (QSARs) Analysis

Q2 · MEDICINE

Review

Author: Kontogiorgis, C. ; Hadjipavlou-Litina, D.

Thromboxane A(2) (TxA(2)), a bioactive metabolite of the Arachidonic acid (AA), is a potent mediator of platelet aggregation, vasoconstriction and bronchoconstriction. It plays an important role in major human diseases, such as myocardial infraction, unstable angina, pregnancy-induced hypertension and preeclampsia, thrombosis and thrombotic disorders, pulmonary hypertension, asthma, septic shock, atherosclerosis, lupus nephritis, and Raynaud's phenomenon. Thus, TxA(2) is a therapeutic target for many research groups. A number of TXA(2) receptor antagonists as well as thromboxane synthase inhibitors have been developed. In this research we review and evaluate new quantitative structure activity relationships of thromboxane synthase inhibitors and thromboxane receptor antagonists, using the C-QSAR program of Biobyte. Lipophicity, as Clog P is a significant physicochemical parameter for this biological response. CMR/MR molar refractivity as well as sterimol parameters seemed to be important as well Molecular Volume. Electronic effects with the exception of σ Hammett's constant are not found to govern the biological activity. The derived equations will be very helpful for the design of new potent molecules.

100 Deals associated with CGS-22652

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Indication	Highest Phase	Country/Location	Organization	Date
Myocardial Ischemia	Phase 1	-	Novartis Pharma AG	-
Myocardial Ischemia	Phase 1	United States	-	-
Myocardial Ischemia	Phase 1	Switzerland	Novartis AG	-
Thrombosis	Phase 1	-	Novartis Pharma AG	-
Thrombosis	Phase 1	United States	-	-
Thrombosis	Phase 1	Switzerland	Novartis AG	-

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