345294-39-5Relevant academic research and scientific papers
Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis
Guardia, Ana,Baiget, Jessica,Cacho, Mónica,Pérez, Arancha,Ortega-Guerra, Montserrat,Nxumalo, Winston,Khanye, Setshaba D.,Rullas, Joaquín,Ortega, Fátima,Jiménez, Elena,Pérez-Herrán, Esther,Fraile-Gabaldón, María Teresa,Esquivias, Jorge,Fernández, Raquel,Porras-De Francisco, Esther,Encinas, Lourdes,Alonso, Marta,Giordano, Ilaria,Rivero, Cristina,Miguel-Siles, Juan,Osende, Javier G.,Badiola, Katrina A.,Rutledge, Peter J.,Todd, Matthew H.,Remui?án, Modesto,Alemparte, Carlos
, p. 11327 - 11340 (2019/01/08)
Society urgently needs new, effective medicines for the treatment of tuberculosis. To kick-start the required hit-to-lead campaigns, the libraries of pharmaceutical companies have recently been evaluated for starting points. The GlaxoSmithKline (GSK) library yielded many high-quality hits, and the associated data were placed in the public domain to stimulate engagement by the wider community. One such series, the spiro compounds, are described here. The compounds were explored by a combination of traditional in-house research and open source methods. The series benefits from a particularly simple structure and a short associated synthetic chemistry route. Many members of the series displayed striking potency and low toxicity, and highly promising in vivo activity in a mouse model was confirmed with one of the analogues. Ultimately the series was discontinued due to concerns over safety, but the associated data remain public domain, empowering others to resume the series if the perceived deficiencies can be overcome.
SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENES
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Page/Page column 25, (2010/06/11)
The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
Novel spiropiperidines as highly potent and subtype selective σ-receptor ligands. Part 1
Maier, Christoph A.,Wünsch, Bernhard
, p. 438 - 448 (2007/10/03)
A series of spiro[[2]benzopyran-1,4′-piperidines] and spiro[[2]benzofuran-1,4′-piperidines] of general structure 10 is prepared, and the affinity for σ1- and σ2-receptors is investigated by means of radioligand binding assays. The sy
