126541-82-0Relevant academic research and scientific papers
INACTIVATORS OF TOXOPLASMA GONDII ORNITHINE AMINOTRANSFERASE FOR TREATING TOXOPLASMOSIS AND MALARIA
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, (2018/04/20)
Disclosed are methods, compounds, and compositions for treating infection by an Apicomplexan parasite that include administering a compound that selectively inactivates ornithine aminotransferase of the Apicomplexan parasite. Specifically, the methods, co
TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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, (2016/10/31)
The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis
Heimburg, Tino,Chakrabarti, Alokta,Lancelot, Julien,Marek, Martin,Melesina, Jelena,Hauser, Alexander-Thomas,Shaik, Tajith B.,Duclaud, Sylvie,Robaa, Dina,Erdmann, Frank,Schmidt, Matthias,Romier, Christophe,Pierce, Raymond J.,Jung, Manfred,Sippl, Wolfgang
supporting information, p. 2423 - 2435 (2016/04/10)
Schistosomiasis is a major neglected parasitic disease that affects more than 265 million people worldwide and for which the control strategy consists of mass treatment with the only available drug, praziquantel. In this study, a series of new benzohydroxamates were prepared as potent inhibitors of Schistosoma mansoni histone deacetylase 8 (smHDAC8). Crystallographic analysis provided insights into the inhibition mode of smHDAC8 activity by these 3-amidobenzohydroxamates. The newly designed inhibitors were evaluated in screens for enzyme inhibitory activity against schistosome and human HDACs. Twenty-seven compounds were found to be active in the nanomolar range, and some of them showed selectivity toward smHDAC8 over the major human HDACs (1 and 6). The active benzohydroxamates were additionally screened for lethality against the schistosome larval stage using a fluorescence-based assay. Four of these showed significant dose-dependent killing of the schistosome larvae and markedly impaired egg laying of adult worm pairs maintained in culture.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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, (2015/12/08)
The present invention is directed to substituted five membered heteroaryl benzamide compounds compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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, (2015/12/30)
The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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, (2016/03/04)
The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula(I) which are tropomyosin-related kinase(Trk)family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF)receptor TrkA.
Demethyl(trifluoromethyl)actinomycins
Giencke, Astrid,Lackner, Helmut
, p. 569 - 579 (2007/10/02)
The synthesis of new 4-(trifluoromethyl)benzoic acid derivatives 2-10 and their coupling with amino acids and peptides 12, 13, 15 is described.They serve as precursors for the synthesis of the hitherto unknown demethyl(trifluoromethyl)actinocin dimethyl esters 11, demethyl-trifluoromethyl-actinocinyl peptides 14, 16, 18 and the demethyl-trifluoromethyl-actinomycins 17.Although spacially comparable with the methyl residues, the 4- and 6-trifluoromethyl groups have unexpected strong influences on the antibiotic and cytostatic properties of the actinomycins.The CH3/CF3 exchange makes it possible to bring NMR-analytically useful hetero nuclei into the centre of the actinomycin/DNA complex (Figure 1).
