Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines

Nitrogen-containing heterocycles represent a major source of pharmacological probes and drug candidates. To extend their molecular diversity and their potential biological activities, it is of importance to design and synthesize new N-heterocyclic scaffolds. Therefore, aza-diketopiperazines (aza-DKPs), the aza analogues of well-known 2,5-diketopiperazines (DKPs), emerged as a promising new scaffold. Although the first synthesis of an aza-DKP dates from 1951, significant developments have been made during the last decade. This feature article summarizes the different synthetic strategies to access and functionalise aza-DKPs. Their biological properties and potential applications in medicinal chemistry and drug discovery are discussed as well

INHIBITORII PROLIFERĂRII BACTERIEI BACILLUS CEREUS ÎN BAZA COMPUŞILOR COORDINATIVI AI CUPRULUI(II) CARE CONŢIN 4-FENILTIOSEMICARBAZONA 2-FORMILPIRIDINEI ŞI SULFANILAMIDE

Uiniversitatea de Stat de Medicină şi Farmacie “N. Testemiţanu”, Catedra Microbiologie, Virusologie şi Imunologie; Universitatea de Stat din Moldova, Catedra Chimie anorganică.Rezumat Studiul dat se referă la obţinerea unui grup de compuşi coordinativi noi de cupru (II) care conţin 4-feniltiosemicarbazona 2-formilpiridinei şi sulfanilamide şi care manifestă activitate antibacteriană pronunţată faţă de bacteriile din genul Bacillus cereus. Proprietăţile stabilite ale compuşilor nominalizaţi asupra altor tipuri de bacterii gram-pozitive şi gramnegative prezintă oportunitate de utilizare în practica medicală din punctul de vedere al extinderii arsenalului de remedii antimicrobiene, iar complecşii respectivi pot fi utilizaţi şi în cazul altor tulpini de microorganisme rezistente la medicamentele tradiţionale. This paper describes a new group of copper (II) coordinative compounds, containing 4-phenyl thiosemi-carbazone 2-formylpyridine and sulfanilamides with a pronounced antibacterial activity against bacteria of the genus Bacillus cereus and other gram-positive and gram-negative microorganisms, which represents new directions in the development of antibacterial products. Были получены новые координационные соединения меди (II) содержащие 4- фенилтиoсемикарбазон 2-формилпиридина и сульфаниламиды с выраженной антибактериальной активностью по отношению к бактериям рода Bacillus сеreus, а также к другим грамположительным и грамотрицательным микроорганизмам. Выявленные антимикробные свойства позволяют рекомендовать соответствующие комплексы меди (II) с 4- фенилтисемикарбазоном 2-формилпиридина и сульфаниламидами для применения в медицинской практике против резистентных штаммов микроорганизмов

Supplementary data for the article: Ristić, P.; Todorović, T. R.; Blagojević, V.; Klisurić, O. R.; Marjanović, I.; Holló, B. B.; Vulić, P.; Gulea, M.; Donnard, M.; Monge, M.; Rodríguez-Castillo, M.; López-de-Luzuriaga, J. M.; Filipović, N. R. 1D and 2D Silver-Based Coordination Polymers with Thiomorpholine-4-Carbonitrile and Aromatic Polyoxoacids as Coligands: Structure, Photocatalysis, Photoluminescence, and TD-DFT Study. Crystal Growth & Design 2020, 20 (7), 4461–4478. https://doi.org/10.1021/acs.cgd.0c00287

Supplementary material for: [https://pubs.acs.org/doi/10.1021/acs.cgd.0c00287#]Related to published version: [https://cherry.chem.bg.ac.rs/handle/123456789/4200]Related to accepted version: [https://cherry.chem.bg.ac.rs/handle/123456789/4203

[Mo2O2S2]2+ and [Mo2O4]2+ -based coordination chemistry: from synthesis to biological applications

International audienc

[Mo2O2S2]2+ and [Mo2O4]2+ -based coordination chemistry: from synthesis to biological applications

International audienc

Synthesis of Sulfur-Containing Exo -Bicyclic Dienes and Their Diels-Alder Reactions to Access Thiacycle-Fused Polycyclic Systems

International audienceThe stereocontrolled synthesis of unprecedented sulfur-containing exo-bicyclic 1,3-dienes is reported through a palladium-catalyzed reductive cyclization of sulfur-linked 2-bromoenynes. The fused bicyclic structure provides a better stability to the thiacyclic diene compared to the simple 3,4-dimethylenetetrahydrothiophene. Their reactivity toward several dienophiles has been investigated, and various original thiacycle-fused polycyclic systems have been obtained with high or total diastereoselectivity. Moreover, they are the first exo-bicyclic dienes used in Diels–Alder reactions. The relative configurations of four cycloadducts have been unambiguously assigned by X-ray crystallographic analysis. Mechanistic details of the cycloadditions have been examined by computational means