2017
DOI: 10.1016/j.bmc.2017.06.003
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Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition

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Cited by 11 publications
(13 citation statements)
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“…49 In addition, a hERG inhibitory effect was observed on somatostatin and its derivatives as well. 50 The detailed prediction results for 1,824 approved drugs by deephERG are provided in Supporting Information, Table S6. We next turned to focus on the deephERG-predicted cardiotoxicity risk on approved anticancer agents (colored in red in Figure 6).…”
Section: Resultsmentioning
confidence: 99%
“…49 In addition, a hERG inhibitory effect was observed on somatostatin and its derivatives as well. 50 The detailed prediction results for 1,824 approved drugs by deephERG are provided in Supporting Information, Table S6. We next turned to focus on the deephERG-predicted cardiotoxicity risk on approved anticancer agents (colored in red in Figure 6).…”
Section: Resultsmentioning
confidence: 99%
“…The total quantity of SP of stomach can be measured in the mucous membrane, especially in pylorus the muscular coat with the largest amount of SP ( Pernow, 1951 ). Somatostatin (SS) is growth hormone–inhibiting hormone and a peptide hormone regulating the endocrine system, and affecting neurotransmission by interacting with G protein-coupled SS receptors and inhibiting hormone release ( Yamasaki et al, 2017 ). Somatostatin inhibits insulin and glucagon secretion.…”
Section: Methodsmentioning
confidence: 99%
“…Compounds with simple substituents such as bromo, nitro, nitroso, amino and dimethylamino (7-11) showed no cytotoxicity. Acylamides (12)(13)(14) seemed to have equipotent cytotoxicity compared to the natural product 1 while aminoacetamides (15)(16)(17)(18) showed lower cytotoxicity except substituted by 4-methylpiperazine (17). Similar rule appeared in (20)(21)(22)(23)(24), that is the mannich base of 4-methylpiperazine (23) exhibited the highest cytotoxic effect which is much higher than the natural compound 1.…”
Section: Cytotoxicity and Sar Analysismentioning
confidence: 99%
“…Purication by silica gel chromatography afforded 14 as a white powder (81%). Mp 118-120 C. 1 N-(5-Allyl-2-hydroxy-3-(2-methylbenzofuran-5-yl)phenyl)-2-(piperidin-1-yl)acetamide (15). A solution of 14 (0.5 mmol), piperidine (1.5 mmol) and triethylamine (1.0 mmol) in THF (5 mL) was stirred at room temperature for 8 h. Then the mixture was concentrated under reduced pressure and puried by silica gel chromatography to afford 15 as a brown powder (48%).…”
Section: H Nmr Andmentioning
confidence: 99%