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The development of selective steroidal mineralocorticoid receptor antagonists with improved pharmacological profiles over existing marketed drugs is an attractive goal. Such compounds offer potential for the treatment of hypertension, heart failure and renal disease. With this aim, new spirolactones were prepared exploring substitutions at carbons 6, 7, 9?11, 15?16 and 21. Spirolactones 11 a and 20 were identified with promising biological profiles. Both compounds restored Na+/K+ ratios to physiological levels in an in vivo model.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Macrocyclic natural products have been recognized and utilized as new platforms for designing drugs in pharmaceutical research because the constrained three-dimensional shapes and the large surface areas of these complex structures enable selective binding to conventionally undruggable targets. Since natural products are not necessarily ideal for medicinal use, structural optimization is required to obtain superior drug candidates. However, the modifications to macrocyclic natural products that will afford the best pharmacological characteristics cannot be known a priori. Therefore, this optimization procedure requires the exploration of a vast array of natural product analogues to identify new compounds with more desirable properties. To fully explore the chemical space around complex macrocyclic natural products, the construction of a large number of analogues is required. In this review, we provide an overview of the efficient synthetic construction of the analogues of macrocyclic natural products and the evaluation of their biological activities. The examples of the comprehensive structure-activity relationship (SAR) studies depicted herein led to the discoveries of biologically useful analogues. These studies illustrate the importance of designing building blocks and coupling strategies to synthesize a variety of natural product based analogues.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Tetra-n-butylammonium per-ruthenate (Bun4N)(RuO4) and tetra-n-propylammonium per-ruthenate (Prn4N)(RuO4), with N-methylmorpholine N-oxide, function as mild catalitic oxidants for the high yield conversion of alcohols to aldehydes and ketones and are competitive with more conventional reagents.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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In this paper, we report the first total synthesis of (+)-coprophilin, an anticoccidial agent, by constructing the chiral linear precursor via a Mukaiyama-Evans aldol reaction and a stereoselective intramolecular Diels-Alder reaction. The proposed method can be used to provide large amounts of (+)-coprophilin, which exhibits a 3,4,5,6,7-pentasubstituted Delta 1,2 -octalin core structure.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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The synthetic applications of substituted allylamines for the preparation of diverse aza-heterocyclic systems employing nucleophilic reactions, lactamizations, cycloadditions, free radical reactions, cross-couplings and reductive cyclizations are reviewed.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Pyrrole spiroketal alkaloids (PSAs) are a class of novel natural products that have been recently disclosed. Acortatarin A and acortatarin B, two potent antioxidative spiroalkaloids with a naturally rare morpholine moiety, are important members of this class. These spiroalkaloids are isolated from Acorus tatarinowii, Brassica campestris, Capparis spinose, bread crust, Xylaria nigripes and medicine Shensong Yangxin and could inhibit significantly the reactive oxygen species (ROS) production in high-glucose-induced mesangial cells in a time- and dose-dependent manner. Hence, these natural products are promising starting points for the formation of new therapeutics to medicate cardiovascular diseases, cancer, diabetic complications, and other diseases in which ROS are implicated. The impressive structure combined with an interesting pharmacological activity prompted synthetic chemists to construct an asymmetric synthetic strategy that could be used to access structural derivatives in addition to the larger quantities of natural products required for further biological investigations. This review summarizes the current state of the literature regarding with the synthesis of acortatarin A and B and its other family members viz. shensongine A, B and C, and pollenopyrroside A. The present review discusses the pros and cons of synthetic methodologies, which would be beneficial for further developments in the synthetic methodologies. Hopefully, this struggle pushes the reader’s mind to consider new perspectives, think differently and forge new connections.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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The present invention is directed to 2-hydroxymethyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Compounds of Formula 1 STR1 where Y is a bivalent radical having Formula 2 or Formula 3 where o is an integer from 1 to 4 STR2 where the remaining symbols have the meaning described in the specification are selective agonists of RXR retinoid receptors.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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The redox and ligand exchange reactions of oxido-ruthenium complexes are central to the function of the Sharpless and Griffith-Ley one-step alcohol oxidation protocols. However, their mechanisms have not been elucidated. Cyclic voltammetry and UV-vis spectroelectrochemical analysis of [RuO4]- has provided new insight into the key ruthenium oxidation states involved in catalysis. Furthermore, the oxidation states sensitive to the presence of the N-oxide co-oxidant N-methylmorpholine N-oxide (NMO), and its role in catalysis, have been determined.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Compounds of formula (I) STR1where R 1 is hydrogen; R 2 is nitro, cyano or halo(lower)alkyl; R 3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R 4 is a group CR 6 R 7 R 8 wherein R 6 and R 7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R 8 is hydrogen; its prodrug and a salt thereof.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI