32813-52-8Relevant academic research and scientific papers
BENZIMIDAZOLE AND IMADAZOPYRIDINE CARBOXIMIDAMIDE COMPOUNDS
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Paragraph 1508, (2016/12/01)
The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
Regioselective covalent modification of hemoglobin in search of antisickling agents
Park, Soobong,Hayes, Brittany L.,Marankan, Fatima,Mulhearn, Debbie C.,Wanna, Linda,Mesecar, Andrew D.,Santarsiero, Bernard D.,Johnson, Michael E.,Venton, Duane L.
, p. 936 - 953 (2007/10/03)
Although the molecular defect in sickle hemoglobin that produces sickle cell disease has been known for decades, there is still no effective drug treatment that acts on hemoglobin itself. In this work, a series of diversely substituted isothiocyanates (R-NCS) were examined for their regioselective reaction with hemoglobin in an attempt to alter the solubility properties of sickle hemoglobin. Electrospray mass spectrometry, molecular modeling, X-ray crystallography, and conventional protein chemistry were used to study this regioselectivity and the resulting increase in solubility of the modified hemoglobin. Depending on the attached R-group, the isothiocyanates were found to react either with the Cysβ93 or the N-terminal amine of the α-chain. One of the most effective compounds in the series, 2-(N,N-dimethylamino)ethyl isothiocyanate, selectively reacts with the thiol of Cysβ93 which, in conjunction with the cationic group, was seen to perturb the local hemoglobin structure. This modified HbS shows an approximately 30% increase in solubility for the fully deoxygenated state, along with a significant increase in oxygen affinity. This compound and a related analogue appear to readily traverse the erythrocyte membrane. A discussion of the relation of these structural changes to inhibition of gelation is presented. The dual activities of increasing HbS oxygen affinity and directly inhibiting deoxy HbS polymerization, in conjunction with facile membrane traversal, suggest that these cationic isothiocyanates show substantial promise as lead compounds for development of therapeutic agents for sickle cell disease.
Synthesis of new alkylaminoalkyl thiosemicarbazones of 3-acetylindole and their effect on DNA synthesis and cell proliferation
Siatra-Papastaikoudi,Tsotinis,Raptopoulou,Sambani,Thomou
, p. 107 - 114 (2007/10/02)
The preparation of a number of thiobemicarbazones of 3-acetylindole is described. These compounds were evaluated in vitro for their effect on proliferation and cell-division delays in cultured human peripheral blood lymphocytes, and their effect on DNA synthesit in T-cell leukemia Molt-4 cells.
Heterocyclic and aromatic thiosemicarbazones useful in the treatment of filariasis
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, (2008/06/13)
This invention is directed to heterocyclic and aromatic thiosemicarbazonesseful in the treatment of filariasis and in an animal, including humans.
2-acetylpyridine thiosemicarbazone compositions as anitviral agents
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, (2008/06/13)
This invention relates to various compositions, comprising a 2-acetylprid thiosemicarbazone and a diol, which are useful in the treatment of viral infections.
Transition metal complexes of the selenium analogs of 2-acetyl- and 2-propionylpyridine thiosemicarbazones useful for treating malarial infections and leukemia
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, (2008/06/13)
This invention relates to novel transition metal complexes of 2-acetyl- and-propionylpyridine thiosemicarbazones, their selenium analogs. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures u
2-acetyl- and 2-propionylpyridine selenosemicarbazones
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, (2008/06/13)
This invention relates to novel 2-acetyl- and 2-propionylpyridine selenosemicarbazones. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the selenosemicarbazones.
2-acetylpyridine thiosemicarbazones as antiviral agents
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, (2008/06/13)
This invention relates to the use of various 2-acetylpyridine thiosemicarbazones which are substituted on the 4-nitrogen atom in the treatment of viral infections. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones.
2-Acetyl-and 2-propionylpyridine thiosemicarbazones
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, (2008/06/13)
This invention relates to various 2-acetyl- and 2-propionylpyridine thioscarbazones which are substituted on the 4-nitrogen atom. These compounds are useful in the treatment of gonorrhea and, in addition, many are useful either in the treatment of malari
Anticoccidial activity of dithiosemicarbazones
Winkelmann,Wagner,Wirth
, p. 950 - 967 (2007/10/05)
Dithiosemicarbazones (di-TSC) with one or two basic substituents were found to be highly active against a variety of Eimeria species (coccidia) in chicks after both prophylactic and therapeutic application. As to the structure-activity relation, it could be shown that the necessary prerequisites of activity were a di-TSC structure in which at least one radical of the TSC part of the molecule carried a basic function, and the C=S group in TSC being freely enolizable, i.e., both nitrogen atoms next to the C=S group carrying another hydrogen atom. If the C=S groups were replaced by C=O or C=NH to form either disemicarbazones or diguanylhydrazones, the compounds obtained were ineffective. The limitation of action to di-TSC with basic substituents of a small volume suggested that the basic radical was of great importance for the absorption of the compound by the mucosa and penetration into the coccidia. The activity against coccidia was clearly attributable to the whole molecule, since the parts resulting from degradation (possibly by hydrolysis), e.g., α,β-dicarbonyl compounds and their derivatives, such as dihydrazones or thiosemicarbazides with basic substituents, or isothiocyanates with basic substituents, were completely ineffective.
