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Identification and electrophysiological evaluation of 2-methylbenzamide derivatives as Nav1.1 modulators.
Crestey F, Frederiksen K, Jensen HS, Dekermendjian K, Larsen PH, Bastlund JF, Lu D, Liu H, Yang CR, Grunnet M, Svenstrup N. Crestey F, et al. ACS Chem Neurosci. 2015 Aug 19;6(8):1302-8. doi: 10.1021/acschemneuro.5b00147. Epub 2015 Jul 8. ACS Chem Neurosci. 2015. PMID: 26114759
Here, we report for the first time the synthesis and the electrophysiological evaluation of 16 ligands based on a 2-methylbenzamide scaffold that have been identified as Nav1.1 modulators. Among these compounds, N,N'-(1,3-phenylene)bis(2-methylbenzamide
Here, we report for the first time the synthesis and the electrophysiological evaluation of 16 ligands based on a 2-methylbenzamid
Discovery of Novel Isoxazoline Compounds that Incorporate a para-Diamide Moiety as Potential Insecticidal Agents against Fall Armyworm (Spodoptera frugiperda).
Jiang B, Li F, Feng D, Wei W, Luo Y, He S, Dong Y, Hu D. Jiang B, et al. J Agric Food Chem. 2023 Apr 12;71(14):5516-5524. doi: 10.1021/acs.jafc.3c00351. Epub 2023 Mar 31. J Agric Food Chem. 2023. PMID: 37000156
Based on the three-dimensional quantitative structure-activity relationship of those compounds, the compound G22 (N-(4-acetamidophenyl)-4-(5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-2-methylbenzamide) was developed. A bioassay showed that G …
Based on the three-dimensional quantitative structure-activity relationship of those compounds, the compound G22 (N-(4-acetamidophenyl)-4-(5 …
Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists.
Tokumaru K, Ito Y, Nomura I, Nakahata T, Shimizu Y, Kurimoto E, Aoyama K, Aso K. Tokumaru K, et al. Bioorg Med Chem. 2017 Jun 15;25(12):3098-3115. doi: 10.1016/j.bmc.2017.03.064. Epub 2017 Apr 1. Bioorg Med Chem. 2017. PMID: 28433511
During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (4u; half maximal effective concentration (EC(50))=75nM, maximal res …
During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl) …
Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.
Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW. Laufer R, et al. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3562-6. doi: 10.1016/j.bmcl.2016.06.021. Epub 2016 Jun 9. Bioorg Med Chem Lett. 2016. PMID: 27335255
The SAR indicates a strong dependence of activity on the presence of the N-cyclopropyl-2-methylbenzamide moiety delineating the geometry for 1 type kinase inhibitor. ...
The SAR indicates a strong dependence of activity on the presence of the N-cyclopropyl-2-methylbenzamide moiety delineating th …
LC, LC-MS/TOF and MS(n) studies for the identification and characterization of degradation products of nelfinavir mesylate.
Tiwari RN, Bonde CG. Tiwari RN, et al. J Pharm Biomed Anal. 2011 Jun 1;55(3):435-45. doi: 10.1016/j.jpba.2011.02.020. Epub 2011 Feb 24. J Pharm Biomed Anal. 2011. PMID: 21392920
The degradation products were identified as 3-hydroxy-N-((2R,3R)-3-hydroxy-1-(phenylthio)butan-2-yl)-2-methylbenzamide and (3S,4aS,8aS)-N-tert-butyl-2-((2R,3R)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(phenylsulfinyl)butyl)decahydroisoquinoline-3-carboxamide....
The degradation products were identified as 3-hydroxy-N-((2R,3R)-3-hydroxy-1-(phenylthio)butan-2-yl)-2-methylbenzamide and (3S …
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Kim H, Kim M, Lee J, Yu H, Hah JM. Kim H, et al. Bioorg Med Chem. 2011 Nov 15;19(22):6760-7. doi: 10.1016/j.bmc.2011.09.042. Epub 2011 Oct 1. Bioorg Med Chem. 2011. PMID: 22014755
Among them, N-(3-(1-benzyl-7-oxo-1,6,7,8-tetrahydropyrazolo[3,4-b][1,4]diazepin-5-yl)phenyl)-4-chloro-3-(trifluoro methyl)benzamide-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl) phenyl) ureido)-2-methylbenzamide (7b) exhibited potent …
Among them, N-(3-(1-benzyl-7-oxo-1,6,7,8-tetrahydropyrazolo[3,4-b][1,4]diazepin-5-yl)phenyl)-4-chloro-3-(trifluoro methyl)benzamide-amino-1- …
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.
Kim MH, Kim M, Yu H, Kim H, Yoo KH, Sim T, Hah JM. Kim MH, et al. Bioorg Med Chem. 2011 Mar 15;19(6):1915-23. doi: 10.1016/j.bmc.2011.01.067. Epub 2011 Feb 3. Bioorg Med Chem. 2011. PMID: 21353571
Among them, N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl)phenyl) ureido)-2-methylbenzamide 7c exhibited potent activities (GI(50)=0.27 muM). ...
Among them, N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl)phenyl) ureido)-2-methylbenzamide
FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia.
Nishiyama K, Suzuki H, Harasawa T, Suzuki N, Kurimoto E, Kawai T, Maruyama M, Komatsu H, Sakuma K, Shimizu Y, Shimojo M. Nishiyama K, et al. J Pharmacol Exp Ther. 2017 Nov;363(2):253-264. doi: 10.1124/jpet.117.242925. Epub 2017 Aug 29. J Pharmacol Exp Ther. 2017. PMID: 28851764
In the current study, we investigated the in vitro and in vivo pharmacologic activities of a novel GPR52 agonist, 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (FTBMT). FTBMT functioned as a selective GPR52 agonist in vi …
In the current study, we investigated the in vitro and in vivo pharmacologic activities of a novel GPR52 agonist, 4-(3-(3-fluoro-5-(trifluor …
Synthesis of new carbon-11 labeled naphthalene-sulfonamides for PET imaging of human CCR8.
Wang M, Cooley B, Gao M, Miller KD, Sledge GW, Hutchins GD, Zheng QH. Wang M, et al. Appl Radiat Isot. 2008 Oct;66(10):1406-13. doi: 10.1016/j.apradiso.2008.03.010. Epub 2008 Mar 20. Appl Radiat Isot. 2008. PMID: 18455923
Carbon-11 labeled naphthalene-sulfonamides, N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphthalene-1-yl)benzamide ([(11)C]5a), N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphthalene-1-yl)-2-methylbenzamide ([(11)C]5b), N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphtha …
Carbon-11 labeled naphthalene-sulfonamides, N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphthalene-1-yl)benzamide ([(11)C]5a), N-(4-(N-(4-[(1 …
11 results