1314908-30-9Relevant academic research and scientific papers
IMIDAZOPYRIDAZINE AND IMIDAZOTHIADIAZOLE COMPOUNDS
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Page/Page column 148-149, (2016/09/26)
The present invention provides imidazopyridazine compounds or imidazothiadiazole compounds of Formula I having the structure: (I) wherein X1, X2, X3, X4, X5, Y, W, R1, R2, R
A divergent SAR study allows optimization of a potent 5-HT2c inhibitor to a promising antimalarial scaffold
Calderon, Felix,Vidal-Mas, Jaume,Burrows, Jeremy,De La Rosa, Juan Carlos,Jimenez-Diaz, Maria Belen,Mulet, Teresa,Prats, Sara,Solana, Jorge,Witty, Michael,Gamo, Francisco Javier,Fernandez, Esther
supporting information; experimental part, p. 373 - 377 (2012/06/30)
From the 13-533 chemical structures published by GlaxoSmithKline in 2010, we identified 47 quality starting points for lead optimization. One of the most promising hits was the TCMDC-139046, a molecule presenting an indoline core, which is well-known for its anxiolytic properties by interacting with serotonin antagonist receptors 5-HT2. The inhibition of this target will complicate the clinical development of these compounds as antimalarials. Herein, we present the antimalarial profile of this series and our efforts to avoid interaction with this receptor, while maintaining a good antiparasitic potency. By using a double-divergent structure-activity relationship analysis, we have obtained a novel lead compound harboring an indoline core.
A novel series of thromboxane A2 synthetase inhibitors with free radical scavenging and anti-peroxidative activities
Kamiya,Shirahase,Nakamura,Kanda,Matsui,Yoshimi,Kasai,Takahashi,Kurahashi
, p. 563 - 571 (2007/10/03)
A novel series of indoline derivatives with imidazole and carboxyl moieties were synthesized and evaluated for their thromboxane A2 (TXA2) synthetase inhibiting, radical scavenging and anti-peroxidative activities. Among the compounds synthesized, 3.{5-substituted-3-[2-(imidazol-1-yl)ethyl]indolin-1-yl}propionic acids showed free radical scavenging activity and inhibitory effects on lipid-peroxidation of rat brain homogenate and on arachidonate-induced TXA2-dependent aggregation of rabbit platelets. The anti-platelet and anti-peroxidative activities were related to the lipophilicity of the 5-substituent. The 5-hexyloxy derivative (13) showed about 35-fold higher inhibitory activity on TXA2 synthesis than that of ozagrel and about 100-fold higher activity on lipid peroxidation than that of α-tocopherol. Compound 13 showed in vivo anti-thrombotic effect in mice and ex vivo anti-peroxidative activity in rats.
