1,720,982 research outputs found
Laboratorio di Preparazione Estrattiva e Sintetica dei Farmaci
No full textQuesto testo si propone di fornire le conoscenze per eseguire praticamente la sintesi di un prodotto (v. Figura) o la sua estrazione da materiale vegetale. Per realizzare questi processi occorre familiarizzarsi con varie metodiche generali, che andranno poi applicate ai singoli casi in base a ragionamenti appropriati. Il testo è stato calibrato in modo da soddisfare le esigenze di un Corso di Laboratorio di Preparazione Estrattiva e Sintetica dei Farmaci per il Corso di Laurea in Chimica e Tecnologia Farmaceutiche, in cui la parte pratica è svolta contemporaneamente alla parte teorica, e le conoscenze pratiche (“di laboratorio”) dello studente sono limitate.
Esistono banche dati (ad esempio SciFinder) che possono indirizzare a pubblicazioni che contengono la via di sintesi di un composto noto, oppure possono suggerire una strategia di sintesi di composti non noti, ma sono solo il giudizio e l’esperienza individuali che hanno l’ultima parola, specialmente quando si tratta di sintetizzare o estrarre un prodotto ignoto (il caso più comune per chi fa ricerca).
Vari parametri (scala, disponibilità e prezzo dei prodotti di partenza, difficoltà di esecuzione della sintesi e rese attese) sono in grado di influenzare le strategie sintetiche e verranno quindi presi in considerazione per la scelta della via di sintesi. Il presente libro si occupa inizialmente, sia da un punto di vista teorico che pratico, di tecniche generali; quindi si passa alla descrizione ed esecuzione in laboratorio di sintesi di composti di interesse farmaceutico.
In particolare, verranno illustrati casi in cui l’ordine di aggiunta dei reattivi, la stechiometria o la presenza di altri composti (iniziatori, ecc.) possono modificare l’andamento di una reazione. Accanto alla procedura “classica” di sintesi, in cui si fa avvenire la reazione tra i composti A e B in un contenitore (pallone, reattore) per ottenere il prodotto C (sintesi in serie), verranno illustrate strategie innovative (Flow Chemistry) in cui la reazione viene condotta in tubi sottili, dove i reagenti fluiscono in continuo (v. Figura).
Per finire, verranno riportate tecniche di sintesi in parallelo (generazione di librerie di composti) in soluzione o in fase solida, e reazioni di bioconiugazione
Designing Approaches to Multitarget Drugs
No full textPlexxikon adopted a fragment-based drug discovery strategy for the design of multitarget drugs that represents an evolution of the procedure followed for the discovery of a family of selective phosphodiesterase (PDE) inhibitors. The fragment-based drug design was successfully applied for the discovery of multitarget protein-protein interaction inhibitors. Moreover, protein-protein interactions do not have natural small molecule partners, not allowing the design of compounds on the basis of the structure of a small natural substrate or ligand. The modern phenotypic screening has been successfully applied for the discovery of antinociceptive multitarget compounds and for RET inhibitors; this kind of approach can be used fruitfully also for drug repurposing. A survey of the literature showed that the most common strategy followed for the design of multitarget drugs is that based on the use of pharmacophores or structure-activity relationship (SAR) around a lead
New perspectives on the development of antiobesity drugs
No full textAfter many years of research, obesity is still a disease with an unmet medical need. Very few compounds have been approved, acting mainly on neuromediators; researches, in recent years, pointed toward compounds potentially safer than first-generation antiobesity drugs, able to interact with one or more (multitarget therapy) receptors for substances produced by the gut, adipose tissue and other targets outside CNS. Other holistic approaches, such as those involving gut microbiota and plant extracts, appeared recently in the literature, and undoubtedly will contribute to the discovery of a valuable therapy for this disease. This review deals with the positive results and the pitfalls obtained following these approaches, with a view on their clinical trial studies
Ten years of medicinal chemistry (2005-2014) in the journal of medicinal chemistry: Country of contributors, topics, and public-private partnerships miniperspective
No full textThis review analyzes the articles that have appeared during the past 10 years in the Journal of Medicinal Chemistry, the leading journal in the field of medicinal chemistry, to provide a picture of the changing trends in this research area. Our analysis involved the country of the corresponding author, assuming that he/she was the leader of the research group, the interaction between private and public sectors, and the research topics. This analysis provides information on the contributions to the journal of authors from each country and highlights the differences between the public and private sectors regarding the research topics pursued. Moreover, changes in the number of articles that describe work on hits, leads, or clinical candidates during these years have been correlated with the affiliation of the contributors (public or private). An analysis of top-cited articles that have appeared in the journal has also been included. The data will provide the basis for understanding the evolution that is taking place in medicinal chemistry
Naphthofuranone derivatives as specific inhibitors of thymidylate synthases
No full textSynthetic compounds of 1, 2 -naphthalein molecules (I) having specific inhibitory properties of the enzymatic activity of thymidylate synthases of bacterial species, their preparation, their pharmaceutical composition and use in the treatment and prophylaxis of infectious pathologies are disclosed
NAPHTHOFURANONE DERIVATIVES AS SPECIFIC INHIBITORS OF THYMIDYLATE SYNTHASES
No full textSynthetic compounds of 1, 2 -naphthalein molecules (I) having specific inhibitory properties of the enzymatic activity of thymidylate synthases of bacterial species, their preparation, their pharmaceutical composition and use in the treatment and prophylaxis of infectious pathologies are disclose
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
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