J. Appl. Cryst.の発刊に際して

https://pubs.rsc.org/en/content/articlepdf/2019/NP/C8NP00092A

Marine natural products.

The biaryl structural motif is a predominant feature in many pharmaceutically relevant and biologically active compounds. As a result, for over a century 1 organic chemists have sought to develop new and more efficient aryl -aryl bond-forming methods. Although there exist a variety of routes for the construction of aryl -aryl bonds, arguably the most common method is through the use of transition-metalmediated reactions. 2-4 While earlier reports focused on the use of stoichiometric quantities of a transition metal to carry out the desired transformation, modern methods of transitionmetal-catalyzed aryl -aryl coupling have focused on the development of high-yielding reactions achieved with excellent selectivity and high functional group tolerance under mild reaction conditions. Typically, these reactions involve either the coupling of an aryl halide or pseudohalide with an organometallic reagent (Scheme 1), or the homocoupling of two aryl halides or two organometallic reagents. Although a number of improvements have developed the former process into an industrially very useful and attractive method for the construction of aryl -aryl bonds, the need still exists for more efficient routes whereby the same outcome is accomplished, but with reduced waste and in fewer steps. In particular, the obligation to use coupling partners that are both activated is wasteful since it necessitates the installation and then subsequent disposal of stoichiometric activating agents. Furthermore, preparation of preactivated aryl substrates often requires several steps, which in itself can be a time-consuming and economically inefficient process.

http://aether.cmi.ua.ac.be/artikels/Artikels%20Gitte/Artikels/Reviews/Heck-Type-lautens.pdf

Aryl-aryl bond formation by transition-metal-catalyzed direct arylation.

Click Chemistry for Drug Development and Diverse Chemical–Biology Applications

Isatins As Privileged Molecules in Design and Synthesis of Spiro-Fused Cyclic Frameworks

Three Isomeric Diterpenes from Vellozia flavicans.

The pharmacist Theodoro Peckolt was one of the most important figures in the history of the chemistry of natural Brazilian products. Like other nineteenth-century pharmacists in Brazil, he developed formulations and sold them at his pharmacy in Rio de Janeiro, and these enjoyed great prestige in the eyes both of the public and the medical community. The article discusses the relation between the illness originally called "opilacao" (ancylostomiasis, or hookworm) and nineteenth-century treatment. It focuses especially on Peckolt Pharmacy's "Doliarina and iron powder," a formulation extracted from the Ficus gomelleira rubber plant. One of the article's goals is to use modern methods to analyze Ficus gomelleira and identify the chemical composition of the drug.

/pdf/doliarina-and-iron-powder-an-important-medicine-at-peckolt-zulmu2l91p.pdf

["Doliarina and iron powder": an important medicine at Peckolt Pharmacy].

Chagas disease is a neglected tropical disease that affects more than 10 million people worldwide and threatens other 25 million who live in areas of risk. In this work, it is described how inhibitors of the enzyme 14α-demethylase (CYP51) were explored based in the piggyback approach, which is a strategy used to find new applications for known drugs or leads, in this case, against Trypanosoma cruzi. It is shown how the azole class acts in the inhibition of this target, which is a key in the process of ergosterol biosynthesis, a major sterol of the parasite. Their synthetic routes are described in detail and the relationship between the chemical structure of these molecules and the biological activity are correlated.

/pdf/potent-inhibitors-of-the-enzyme-sterol-14a-demethylase-14c47pftj3.pdf

Potent Inhibitors of the Enzyme Sterol 14α-demethylase AgainstTrypanosoma cruzi

Pyrrolizidine or azabicyclo[3.3.0]-octane (Figure 1) and its derivatives are a very common azabicycle motif within natural products (pyrrolizidine alkaloids, PAs) possessing a bridge head nitrogen ...

Angelo C. Pinto

Papers

Three Isomeric Diterpenes from Vellozia flavicans.

["Doliarina and iron powder": an important medicine at Peckolt Pharmacy].

Potent Inhibitors of the Enzyme Sterol 14α-demethylase AgainstTrypanosoma cruzi

Synthetic Strategies Towards the Azabicyclo[3.3.0]‐octane Core of Natural Pyrrolizidine Alkaloids. An Overview

A synthesis of 5‐oxo‐1,2,3,4‐tetrahydro[1,4]azepino‐[6,7,1 ‐kl]phenothiazine