Appunti di Chimica Analitica con esercitazioni numeriche per il corso di laurea in Farmacia

Questo libro deriva dall’elaborazione delle lezioni dell’insegnamento, svolto dall’autore, di Chimica analitica con esercitazioni numeriche e di laboratorio. Nella prima parte sono descritte nozioni di base per la Chimica analitica, tra cui le espressioni della concentrazione di soluzioni e la valutazione statistica di dati. Segue la trattazione degli equilibri chimici e delle applicazioni nell’analisi quantitativa classica. Un gran numero di esercizi svolti arricchisce la parte teorica. Gli esempi e i riferimenti al settore dei medicinali rendono il testo adatto in particolare agli studenti dei corsi di laurea in discipline farmaceutiche

Synthesis and biological evaluation of pyrazoles and pyrazole-containing polycyclic derivatives as new ligands of central and peripheral benzodiazepine receptors

A series of new pyrazole-condensed 6,5,5 tricyclic compounds were synthesized and tested to evaluate their binding affinities at both central (CBR) and peripheral (PBR) benzodiazepine receptors. Some 1-aryl-5-phenylpyrazole derivatives were also prepared and tested for comparison with their corresponding rigid tricyclic analogs.Among the newly synthesized 1-aryl-1,4-dihydro-indeno[1,2-c]pyrazoles bearing both an ethoxycarbonyl group at position 3 and a carbonyl function at the position 4, compound 4b emerged as a new potent (IC50 = 26.4 nM) and selective CBR ligand. The 4-oxo-1-aryl-1,4-dihydro-indeno[1,2-c]pyrazole diethylamide derivative 14a was instead identified as a relatively potent (IC50 = 124 nM) but highly selective PBR ligand

Synthesis and antibacterial activity of pyridazino[4,3-b]indole-4-carboxylic acids carrying different substituents at N-2

The synthesis and the in vitro evaluation of antibacterial activity of new pyridazino[4,3-b]indole-4-carboxylic acids 2-4, 6 against some selected representative of Gram-positive and Gram-negative bacteria are reported. The role of the lipophilicity in the modulation of the antibacterial activity of the tested compounds is discussed. All the synthesized compounds appear quite weak against Gram-positive bacteria, whereas have no significant activity against Gram-negative bacteria. Only derivative 2g possesses an interesting activity against Gram-positive bacteria. © 2002 Elsevier Science S.A. All rights reserved

Synthesis and biological evaluation of arylhydrazone derivatives of indoles and indolin-2-ones as b-amyloid aggregation inhibitors

An increasing number of diseases have being recognized in which misfolded proteins accumulate intracellularly or extracellularly, particularly in diseases of chronic neurodegeneration such as Alzheimer’s disease (AD), Parkinson’s disease (PD), Huntington’s disease, and prion diseases1. AD is characterized, in part, by the aggregation of amyloid β protein (Aβ) into fibrillar amyloid plaques in selected areas of brain2. Morphological and biochemical characterization of the plaques indicated beta-amyloid proteins Aβ1-40 and Aβ1-42 as their main constituents. Aβ fibrils contain β-sheets structure orientated in parallel and anti-parallel directions, giving rise to a specific arrangement of side chains in self- assemblies, termed cross-strand ladders

Synthesis and antibacterial activity of 2-aryl-2, 5-dihydro-3(3H)-oxo-pyridazino[4,3-b]indole-4-carboxylic acids

The in vitro antibacterial and antifungal activities of a series of pyridazinoindolonic acids II against some selected representative of Gram-positive, Gram-negative bacteria and fungi have been investigated. Some interesting observations among the structural features necessary for high antibacterial activity are presented and discussed