- Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease
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In the course of a programme aimed at identifying Nurr1/NOT agonists for potential treatment of Parkinson's disease, a few hits from high throughput screening were identified and characterized. A combined optimization pointed to a very narrow and stringen
- Lesuisse, Dominique,Malanda, André,Peyronel, Jean-Fran?ois,Evanno, Yannick,Lardenois, Patrick,De-Peretti, Danielle,Abécassis, Pierre-Yves,Barnéoud, Pascal,Brunel, Pascale,Burgevin, Marie-Claude,Cegarra, Céline,Auger, Florian,Dommergue, Amélie,Lafon, Corinne,Even, Luc,Tsi, Joanna,Luc, Thy Phuong Hieu,Almario, Antonio,Olivier, Anne,Castel, Marie-No?lle,Taupin, Véronique,Rooney, Thomas,Vigé, Xavier
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p. 929 - 932
(2019/02/19)
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- BENZYL-, (PYRIDIN-3-YL)METHYL- OR (PYRIDIN-4-YL)METHYL-SUBSTITUTED OXADIAZOLOPYRIDINE DERIVATIVES AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS
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The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
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Page/Page column 79; 81; 95
(2019/08/26)
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- Synthesis, molecular docking and anti-mycobacterial evaluation of new imidazo[1,2-a]pyridine-2-carboxamide derivatives
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New anti-tubercular agents, imidazo[1,2-a]pyridine-2-carboxamide derivatives (5a-q) have been designed and synthesized. The structural considerations of the designed molecules were further supported by the docking study with a long-chain enoyl-acyl carrier protein reductase (InhA). The chemical structures of the new compounds were characterized by IR, 1H NMR, 13C NMR, HRMS and elemental analysis. In addition, single crystal X-ray diffraction has also been recorded for compound 5f. Compounds were evaluated in vitro against Mycobacterium tuberculosis H37Rv, and cytotoxicity against HEK-293T cell line. Amongst the tested compounds 5j, 5l and 5q were emerged as good anti-tubercular agents with low cytotoxicity. The structure-anti TB activity relationship of these derivatives was explained by molecular docking.
- Jose, Gilish,Kumara, T.H. Suresha,Nagendrappa, Gopalpur,Sowmya,Sriram, Dharmarajan,Yogeeswari, Perumal,Sridevi, Jonnalagadda Padma,Row, Tayur N. Guru,Hosamani, Amar A.,Sujan Ganapathy,Chandrika,Narendra
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p. 616 - 627
(2014/12/11)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-COA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 44-45
(2010/07/04)
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- NOVEL COMPOUNDS AS PHARMACEUTICAL AGENTS
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The current invention relates to compounds of the formula:(Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.
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- Bis-cationic heteroaromatics as macrofilaricides: Synthesis of Bis- amidine and bis-guanylhydrazone derivatives of substituted imidazol[1,2- a]pyridines
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A series of guanylhydrazone, amidine, and hydrazone derivatives of 2- phenylimidazo[1,2-a]-pyridine have been prepared and evaluated for macrofilarial activity against Acanthocheilonema viteae and Brugia pahangi in jirds. Compounds with 4',6-bis-substitut
- Sundberg, Richard J.,Biswas, Sujay,Murthi, Krishna Kumar,Rowe, Donna,McCall, John W.,Dzimianski, Michael T.
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p. 4317 - 4328
(2007/10/03)
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