Gigliola Sulis speaks to Ann Goldstein: writing locally, translating globally

The conversation focuses on attitudes and trends in the US publishing market toward translated fiction. The strategies used by Goldstein as a translator of geo-centred and multilingual Italian novels are analysed, with reference to her translations of Pier Paolo Pasolini, Primo Levi, Elena Ferrante, Milena Agus, and Amara Lakhous

Synthesis of the tritium labeled SCH 58261, a new non-xanthine A(2A) adenosine receptor antagonist

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Current developments of A(2a) adenosine receptor antagonists

adenosine regulates a wide range of physiological functions through specific cell membrane receptors. On the basis of pharmacological studies and molecular cloning, four distinct adenosine receptors have been identified and classified as A1, A2a, A2b and A3. These adenosine receptors are members of the G-protein-coupled receptor family. An intense medicinal chemistry effort made over the last 20 years has led to a variety of selective adenosine receptor agonists an antagonists. While all the agonists thus far identified are related to the adenosine structure, the antagonists available belong to different chemical classes. The prototypic antagonists are xanthine derivatives evolved from the natural compounds, caffeine and theophylline. Tipically, they are 8-substituted-1,2,3-trialkylxanthine and are A1 selective antagonists. More recently, 8-styrylxanthines have been found to be selective for A2a receptors. other non-xanthine heterocycles are potent A2a antagonists and possess different degree of selectivity. Selective antagonists are not available yet for A2b and A3 receptors. Given the recent developments of A2a selective antagonists, we have reviewed their chemical structures and biological properties in the attempts to get insight into the emerging class of new interesting compounds. The development of some of the A2a antagonists will provide better understanding of the role of A2a receptors in physiological and pathological states. The compounds appear also to have the potential to be useful for the treatment of cerebral ischemia or neurodegenerative disorders, such as Parkinson's disease

1,2,3-triazolo[5,4-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: A new class of A(2A) adenosine receptor antagonists

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2-Aralkynyl and 2-Heteroalkynyl derivatives of Adenosine-5'-N-ethyluronamide as selective A2a adenosine receptor agonists

A series of new 2-aralkynyl and 2-heteroaralkynyl derivatives of NECA were synthesized and studied in binding and functional assays to assess their potency for the A2, compared to A1 adenosine receptors. Compounds bearing an aromatic or heteroaromatic ring, conjugated to the triple bond, showed generally weaker activity at the A2, receptor and lower selectivity (A2 vs AI) than the alkylalkynyl derivatives previously reported. However, the (4-formylpheny1)-ethynyl derivative 17 showed affinity in the low nanomolar range and high selectivity (about 160-fold) for the Aza receptor. The presence of heteroatoms improved vasorelaxant activity, the 2-thiazolylethynyl derivative 30 being the most potent in the series. Introduction of methylene groups between the triple bond and the phenyl ring favored the A2, binding affinity, and the 5-phenyl-1-pentynyl derivative 24 was found to be highly potent and selective (about 180-fold) at A2, receptors. With regard to antiplatelet activity, the presence of aromatic or heteroaromatic rings decreased potency in comparison with that of NECA and of N-ethyl-1’- deoxy-1’-(6-amino-2-hexynyl-9H-purin-9-yl)-b-D-ribofuranuronamide (HENECA). Introduction of a methylene group was effective in increasing antiaggregatory potency only when this group is linked to a heteroatom (31-35). From these data and those previously reported, the structure-activity relationships derived for the 2-alkynyl-substituted ribose uronamides would indicate that potentiation of A2a receptor affinity could be obtained by aromatic rings not conjugated with the triple bond or by heteroaromatic groups. As for A2a receptors on platelets, the presence of aromatic rings, either conjugated or unconjugated to the triple bond, is detrimental for the antiaggregatory activity. However, the introduction of polar groups a to the triple bond strongly increases the potency when steric hindrance is avoided. Some of the compounds included in this series retain interesting vasodilating properties and merit further investigation for their potential in the treatment of cardiovascular disorders

Letture per il corso di editoria

Una selezione di testi non sempre facilmente rintracciabili ma molto utili a segnare un itinerario che porta alla modernit\ue0 dell\u2019editoria, dal primo editore Manuzio, studiato da Carlo Dionisotti, alla trasformazione dei supporti analizzata da Roger Chartier, passando per i testi di Donald McKenzie e Robert Darnton. Una breve sezione \ue8 dedicata alle scelte editoriali, con la spiegazione di paratesto di Genette e il caso di editing di Vittorini; non mancano infine le voci di grandi editori come Valentino Bompiani e Giangiacomo Feltrinelli. Antologia ad uso didattico con sintetici cappelli introduttivi

Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A(2A) adenosine receptor antagonists

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