3652-31-1Relevant academic research and scientific papers
Synthesis, antifungal activity, 3d-qsar, and molecular docking study of novel menthol-derived 1,2,4-triazole-thioether compounds
Duan, Wen-Gui,Huang, Mei,Li, Bao-Yu,Lin, Gui-Shan
, (2021/11/30)
A series of novel menthol derivatives containing 1,2,4-triazole-thioether moiety were designed, synthesized, characterized structurally, and evaluated biologically to explore more potent natural product-based antifungal agents. The bioassay results reveal
Design, synthesis and antibacterial evaluation of 1-[(1R,2S)-2-Fluorocyclopropyl] Ciprofloxacin-(4-Methyl-3-Aryl)-1,2,4-Triazole-5(4H)-Thione Hybrids
Geng, Yun-He,Wei, Zeng-Quan,Xu, Zhi,Na, Lu-Xin,Zhang, Shu,Guo, Hui-Yuan,Liu, Ming-Liang,Feng, Lian-Shun,You, Xue-Fu
, p. 101 - 107 (2019/08/01)
Fourteen novel 1-[(1R,2S)-2-Fluorocyclopropyl]ciprofloxac in-(4-methyl-3-aryl)-1,2,4-triazole-5(4H)-thione hybrids 6a-n were designed, synthesized and assessed for their in vitro antibacterial activities against representative Gram-positive and Gram-negat
DOPAMINE D3 RECEPTOR ANTAGONISTS HAVING A MORPHOLINE MOIETY
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Paragraph 0234-0235, (2018/11/21)
The disclosure provides compounds of formula (I) or pharmaceutically acceptable salts thereof: The disclosure also provides processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them, and their use
DOPAMINE D3 RECEPTOR ANTAGONISTS HAVING A BICYCLO MOIETY
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Paragraph 0547; 0548, (2017/02/28)
The disclosure provides compounds having formula (I), wherein the substituents are as defined herein. The compounds are useful for modulating the dopamine D3 receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.
DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
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Page/Page column 113; 115, (2016/05/19)
The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists
Micheli, Fabrizio,Cremonesi, Susanna,Semeraro, Teresa,Tarsi, Luca,Tomelleri, Silvia,Cavanni, Paolo,Oliosi, Beatrice,Perdon, Elisabetta,Sava, Anna,Zonzini, Laura,Feriani, Aldo,Braggio, Simone,Heidbreder, Christian
, p. 1329 - 1332 (2016/02/23)
A new series of morpholine derivatives has been identified as selective DA D3 receptor antagonists; their in vitro profile and pharmacokinetic data are provided.
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists
Micheli, Fabrizio,Bernardelli, Andrea,Bianchi, Federica,Braggio, Simone,Castelletti, Laura,Cavallini, Palmina,Cavanni, Paolo,Cremonesi, Susanna,Cin, Michele Dal,Feriani, Aldo,Oliosi, Beatrice,Semeraro, Teresa,Tarsi, Luca,Tomelleri, Silvia,Wong, Andrea,Visentini, Filippo,Zonzini, Laura,Heidbreder, Christian
, p. 1619 - 1636 (2016/04/05)
A novel series of 1,2,4-triazolyl octahydropyrrolo[2,3-b]pyrroles showing high affinity and selectivity at the DA D3 receptor is reported here. Compounds endowed with high selectivity over the hERG channel were identified and their pharmacokinetic properties thoroughly analyzed. A few derivatives with appropriate developability characteristics were selected for further studies and progression along the screening cascade. In particular, derivative 60a, (DA D3 pKi = 8.4, DA D2 pKi = 6.0 and hERG fpKi = 5.2) showed a balanced profile and further refinements are in progress around this molecule.
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists
Micheli, Fabrizio,Bacchi, Alessia,Braggio, Simone,Castelletti, Laura,Cavallini, Palmina,Cavanni, Paolo,Cremonesi, Susanna,Dal Cin, Michele,Feriani, Aldo,Gehanne, Sylvie,Kajbaf, Mahmud,Marchió, Luciano,Nola, Selena,Oliosi, Beatrice,Pellacani, Annalisa,Perdonà, Elisabetta,Sava, Anna,Semeraro, Teresa,Tarsi, Luca,Tomelleri, Silvia,Wong, Andrea,Visentini, Filippo,Zonzini, Laura,Heidbreder, Christian
, p. 8549 - 8576 (2016/10/03)
A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of these compounds also have high selectivity over the hERG channel and were characterized with respect to their pharmacokinetic properties both in vitro and in vivo during lead identification and early lead optimization phases. A few derivatives with overall favorable developability characteristics were selected for further late lead optimization studies.
PROCESSES FOR THE MANUFACTURE OF 3-{4-METHYL-5- [ (IR) -1- (2- (3-METHYLPHENYL) -2H-TETRAZOL-5-YL) -ETHOXY] -4H- [1,2, 4] TRIAZOL-3-YL} -PYRIDINE, 4-METHYL-3-METHYLTHIO-5- (3- PYRIDYL)-L,2,4-TRIAZOLE, AND (IR) -1- [2- (3-METHYLPHENYL) -2H- TETRAZOL-5-YL]
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Page/Page column 15-16, (2010/08/05)
The present invention provides a process for the manufacture of the compound 3-{4-methyl-5-[(1R)-1-(2-(3-methylphenyl-2H-tetrazol-5-yl)-ethoxy]-4H-[1,2,4]triazol-3-yl}-pyridine of formula 14 wherein a) the compound 3-(5-methanesulfonyl-4-methyl-4H-1,2,4-t
TETRAZOLE COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONITS
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Page/Page column 92-93, (2010/02/13)
The present invention relates to new compounds of formula I, wherein P, Q, X1, X2, X3, X4, R1, R2, m and p, are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds, and to the use of said compounds in therapy.
