170230-17-8Relevant articles and documents
POTENT AND SELCTIVE COMPOUNDS AS SEROTONIN 1B RECEPTOR MODULATORS
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Page/Page column 37, (2022/04/16)
The present invention relates to new compounds of formula (I): as modulators of serotonin receptor 1B (5-HTR1B) also known as 5-hydroxytryptamine receptor 1B (5-HT1B). The compounds are of potential utility in the treatment of diseases and conditions mediated by serotonin receptor type 1B (5-HTR1B), such as cancer, including blood cancer and solid tumors, respiratory diseases and hepatic disorders.
Synthesis, antimalarial activity, and structure-activity relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones
Cross, R. Matthew,Namelikonda, Niranjan K.,Mutka, Tina S.,Luong, Lisa,Kyle, Dennis E.,Manetsch, Roman
, p. 8321 - 8327 (2012/02/04)
ICI 56,780 (5) displayed causal prophylactic and blood schizonticidal activity (ED50 = 0.05 mg/kg) in rodent malaria models but produced rapid acquisition of parasitological resistance in P. berghei infected mice. Herein we describe the synthesis of analogues of 5 with EC50 as low as 0.15 nM against multidrug resistant P. falciparum. Optimal activity with low cross-resistance indexes (RI) to atovaquone was achieved by introducing ortho-substituted aryl moieties at the 3-position of the 7-(2-phenoxyethoxy)- 4(1H)-quinolone core. (Figure presented