Merck's Annual Report of Recent Advances in Pharmaceutical Chemistry and Therapeutics

Title Varies: 1898-1900, Annual Report; 1906- Report on the Advancements of Pharmaceutical Chemistry and Therapeutics; 1909-14, E. Merck's Annual Report of Recent Advances In Pharmaceutical Chemistry and Therapeutics

Inorganic general, medical and pharmaceutical chemistry, theoretical and practical; a text-book and laboratory manual, containing theoretical, descriptive, and technological chemistry;

Mode of access: Internet.

Medicinal chemistry : chemistry, biochemistry, therapeutic and pharmacological action of natural and synthetic drugs.

Errata slip inserted in v. 1.

Essentials of pathological chemistry, including description of the chemical methods employed in medical diagnosis,

Mode of access: Internet.

Eighth International congress of applied chemistry, Washington and New York, September 4 to 13, 1912.

"Members": v. 28, p. 365-463.

Seventh International Congress of Applied Chemistry, London, May 27th to June 2d, 1909.

Edited by Sir William Ramsay, William Macnab, and others.

Photelometric clinical chemistry,

Bibliography at end of each chapter.

Quantitative clinical chemistry

Mode of access: Internet.

A manual of qualitative analysis and of clinical medical chemistry, for physicians and students

Mode of access: Internet.

Caracterização de polimorfismo em fármacos por ressonância magnética nuclear no estado sólido

This review aims to present some features about solid state NMR and its application in the field of pharmaceutical chemistry, for the characterization of polymorphism of pharmaceutical molecules.

Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines

We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio.

Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines

We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio.

Multigram synthesis and in vivo efficacy studies of a novel multitarget anti-Alzheimer's compound

We describe the multigram synthesis and in vivo efficacy studies of a donepezil‒huprine hybrid that has been found to display a promising in vitro multitarget profile of interest for the treatment of Alzheimer's disease (AD). Its synthesis features as the key step a novel multigram preparative chromatographic resolution of intermediate racemic huprine Y by chiral HPLC. Administration of this compound to transgenic CL4176 and CL2006 Caenorhabditis elegans strains expressing human Aβ42, here used as simplified animal models of AD, led to a significant protection from the toxicity induced by Aβ42. However, this protective effect was not accompanied, in CL2006 worms, by a reduction of amyloid deposits. Oral administration for 3 months to transgenic APPSL mice, a well-established animal model of AD, improved short-term memory, but did not alter brain levels of Aβ peptides nor cortical and hippocampal amyloid plaque load. Despite the clear protective and cognitive effects of AVCRI104P4, the lack of Aβ lowering effect in vivo might be related to its lower in vitro potency toward Aβ aggregation and formation as compared with its higher anticholinesterase activities. Further lead optimization in this series should thus focus on improving the anti-amyloid/anticholinesterase activity ratio.

Argilas como catalisadores verdes na esterificação do colesterol: caracterização espectroscópica e identificação de polimorfos por métodos de análise térmica. Uma proposta laboratorial interdisciplinar para o 1º ciclo universitário

A laboratory experiment that enables the professor to introduce the problematic of sustainable development in pharmaceutical chemistry to undergraduate students is proposed, using a simple synthetic procedure. Cholesteryl acetate is prepared by the esterification of cholesterol using Montmorillonite K10 as heterogeneous catalyst. Cholesterol and cholesteryl acetate are characterized by spectroscopic (¹H RMN, 13C RMN, FTIR) and thermal analysis techniques. The thermal methods are used to introduce the concepts of polymorphism and the nature of mesophases.

Contextualizando reações ácido-base de acordo com a teoria protônica de Brönsted-Lowry usando comprimidos de propranolol e nimesulida

This paper reports the use of alternative materials for teaching experimental chemistry. In this context, nimesulide and propranolol tablets were used to teach chemical concepts about acid-base reactions according to Brönsted-Lowry protonic Theory. Important topics of Organic, Analytical and Pharmaceutical Chemistry were discussed, such as purification by acid-base extraction, solubility of organic compounds in aqueous solutions, buffers, the dissociation constant (pKa), potentiometric titration and ionization of drugs in biological fluids. The purification of propranolol and nimesulide from tablets produced yields of 75% and 90%, respectively. The experimental values of pKa for both drugs were in agreement with those from the literature.