908084-16-2Relevant articles and documents
Synthesis and Structure?Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases
Silva, Daniel G.,Junker, Anna,de Melo, Shaiani M. G.,Fumagalli, Fernando,Gillespie, J. Robert,Molasky, Nora,Buckner, Frederick S.,Matheeussen, An,Caljon, Guy,Maes, Louis,Emery, Flavio S.
, p. 966 - 975 (2021)
Neglected tropical diseases remain among the most critical public health concerns in Africa and South America. The drug treatments for these diseases are limited, which invariably leads to fatal cases. Hence, there is an urgent need for new antitrypanosomal drugs. To address this issue, a large number of diverse heterocyclic compounds were prepared. Straightforward synthetic approaches tolerated pre-functionalized structures, giving rise to a structurally diverse set of analogs. We report on a set of 57 heterocyclic compounds with selective activity potential against kinetoplastid parasites. In general, 29 and 19 compounds of the total set could be defined as active against Trypanosoma cruzi and T. brucei brucei, respectively (antitrypanosomal activities 10 μM). The present work discusses the structure?activity relationships of new fused-ring scaffolds based on imidazopyridine/pyrimidine and furopyridine cores. This library of compounds shows significant potential for anti-trypanosomiases drug discovery.
Identification of Three Novel Radiotracers for Imaging Aggregated Tau in Alzheimer's Disease with Positron Emission Tomography
Gobbi, Luca C.,Knust, Henner,K?rner, Matthias,Honer, Michael,Czech, Christian,Belli, Sara,Muri, Dieter,Edelmann, Martin R.,Hartung, Thomas,Erbsmehl, Isabella,Grall-Ulsemer, Sandra,Koblet, Andreas,Rueher, Marianne,Steiner, Sandra,Ravert, Hayden T.,Mathews, William B.,Holt, Daniel P.,Kuwabara, Hiroto,Valentine, Heather,Dannals, Robert F.,Wong, Dean F.,Borroni, Edilio
, p. 7350 - 7370 (2017/09/22)
Aggregates of tau and beta amyloid (Aβ) plaques constitute the histopathological hallmarks of Alzheimer's disease and are prominent targets for novel therapeutics as well as for biomarkers for diagnostic in vivo imaging. In recent years much attention has been devoted to the discovery and development of new PET tracers to image tau aggregates in the living human brain. Access to a selective PET tracer to image and quantify tau aggregates represents a unique tool to support the development of any novel therapeutic agent targeting pathological forms of tau. The objective of the study described herein was to identify such a novel radiotracer. As a result of this work, we discovered three novel PET tracers (2-(4-[11C]methoxyphenyl)imidazo[1,2-a]pyridin-7-amine 7 ([11C]RO6924963), N-[11C]methyl-2-(3-methylphenyl)imidazo[1,2-a]pyrimidin-7-amine 8 ([11C]RO6931643), and [18F]2-(6-fluoropyridin-3-yl)pyrrolo[2,3-b:4,5-c′]dipyridine 9 ([18F]RO6958948)) with high affinity for tau neurofibrillary tangles, excellent selectivity against Aβ plaques, and appropriate pharmacokinetic and metabolic properties in mice and non-human primates.
IMIDAZOPYRIDINE OR IMIDAZOPYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10A INHIBITORS
-
Page/Page column 71-72, (2011/04/24)
The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically accept
