Category: 51987-99-6

Wang, Xiaoran published the artcileAquaporin 4 differentially modulates osmotic effects on vasopressin neurons in rat supraoptic nucleus, Name: N-(1,3,4-Thiadiazol-2-yl)nicotinamide, the publication is Acta Physiologica (2021), 232(3), e13672, database is CAplus and MEDLINE.

Aim : Glial fibrillary acidic protein (GFAP) molecularly associates with aquaporin 4 (AQP4) in astrocytic plasticity. Here, we further examined how AQP4 modulates osmotic effects on vasopressin (VP) neurons in rat supraoptic nucleus (SON) through interactions with GFAP in astrocytes. Methods : Brain slices from adult male rats were kept under osmotic stimulation. Western blot, co-immunoprecipitation, immunohistochem. and patch-clamp recordings were used for anal. of expressions and interactions between GFAP and AQP4, astrocyte-specific proteins in the SON, as well as their influence on VP neuronal activity. Data were analyzed using SPSS software. Results : Hyposmotic challenge (HOC) of acute SON slices caused an early (within 5 min) and transient increase in the colocalization of AQP4 with GFAP filaments. This effect was prominent at astrocytic processes surrounding VP neuron somata and was accompanied by inhibition of VP neuronal activity. Similar HOC effect was seen in the SON isolated from rats subjected to in vivo HOC, wherein a transiently increased mol. association between GFAP and AQP4 was detected using co-immunoprecipitation The late stage rebound excitation (10 min) of VP neurons in brain slices subjected to HOC and the associated astrocytic GFAP’s ‘return to normal’ were both hampered by 2-(nicotinamide)-1,3,4-thiadiazole, a specific AQP4 channel blocker that itself did not influence VP neuronal activity. Moreover, this agent prevented hyperosmotic stress-evoked excitation of VP neurons and associated reduction in GFAP filaments. Conclusion : These findings indicate that osmotically driven increase in VP neuronal activity requires the activation of AQP4, which determines a retraction of GFAP filaments.

Acta Physiologica published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C5H7F3O3, Name: N-(1,3,4-Thiadiazol-2-yl)nicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wang, Duo-Zhi published the artcileBis[μ-N-(1,3,4-thiadiazol-2-yl)pyridine-3-carboxamide-κ²N¹,N³]disilver(I) bis(perchlorate), Quality Control of 51987-99-6, the publication is Acta Crystallographica, Section E: Structure Reports Online (2007), 63(5), m1294-m1296, database is CAplus.

In the title compound, [Ag₂(C₈H₆N₄OS)₂](ClO₄)₂, each Ag^I center in the centrosym. dinuclear complex cation is coordinated by one pyridine N and a thiadiazole N atom of two inversion-related N-(1,3,4-thiadiazol-2-yl)pyridine-3-carboxamide ligands in an almost linear geometry [Ag-N = 2.187(3) and 2.172(3) Å, and N-Ag-N = 171.8(1)°]. Weak Ag···Ag and Ag-perchlorate interactions, together with π-π stacking interactions, link the complex cations along the a axis to form a ribbon. Crystallog. data are given.

Acta Crystallographica, Section E: Structure Reports Online published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C10H14N2O, Quality Control of 51987-99-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Huber, Vincent J. published the artcileIdentification of Aquaporin 4 inhibitors using in vitro and in silico methods, Formula: C8H6N4OS, the publication is Bioorganic & Medicinal Chemistry (2009), 17(1), 411-417, database is CAplus and MEDLINE.

The in vitro inhibitory effects and in silico docking energies of 18 compounds with respect to Aquaporin 4 (AQP4) were investigated. More than half of the compounds tested showed inhibitory activity in the in vitro functional assay and included the 5-HT_1B/1D agonists sumatriptan, and rizatriptan. Moreover, the observed inhibitory activity of the compounds used in this study at 20 μM showed a strong correlation with their in silico docking energies, r ² = 0.64, which was consistent with that found in previous studies. The AQP4 inhibitory IC₅₀ values of three compounds, 2-(nicotinamido)-1,3,4-thiadiazole, sumatriptan and rizatriptan, were subsequently found to be 3, 11, and 2 μM, resp.

Bioorganic & Medicinal Chemistry published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C8H6N4OS, Formula: C8H6N4OS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Burnett, Marianne E. published the artcileStructural characterization of the aquaporin inhibitor 2-nicotinamido-1,3,4-thiadiazole, Synthetic Route of 51987-99-6, the publication is Acta Crystallographica, Section C: Structural Chemistry (2015), 71(12), 1074-1079, database is CAplus and MEDLINE.

Nicotinamides are a class of compounds with a wide variety of applications, from use as antimicrobial agents to inhibitors of biol. processes. These compounds are also cofactors, which are necessary components of metabolic processes. Structural modification gives rise to the activities observed Similarly, 1,3,4-thiadiazoles have been shown to possess antioxidant, antimicrobial, or anti-inflammatory biol. activity. To take advantage of each of the inherent characteristics of the two aforementioned functional groups, 2-nicotinamido-1,3,4-thiadiazole, C₈H₆N₄OS, was synthesized. Since defining chem. connectivity is paramount in understanding biol. activity, in this report, the structural characterization of 2-nicotinamido-1,3,4-thiadiazole has been carried out using X-ray crystallog. methods. The NMR-derived assignments were made possible by utilizing one- (1D) and two-dimensional (2D) NMR techniques. In addition, UV-Visible and IR spectroscopies, and elemental anal. were used to fully characterize the product synthesized by the one-step reaction between nicotinoyl chloride hydrochloride and 2-amino-1,3,4-thiadiazole. Computational parameters related to blood-brain barrier permeability are also presented.

Acta Crystallographica, Section C: Structural Chemistry published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C8H6N4OS, Synthetic Route of 51987-99-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Takatori, Kichitaro published the artcileSyntheses of amides derived from heterocyclic acids and heterocyclic amines and their antitumor activities, Application In Synthesis of 51987-99-6, the publication is Yakugaku Zasshi (1976), 96(4), 471-4, database is CAplus and MEDLINE.

Pyridineacetamides I, II (R = 3-, 4-pyridyl) and 12 thiadiazoles (III, R = 3-,4-pyridyl, 2-thienyl, 2-furyl; R1 = H, CHMe2, CH2CHMe2) were prepared from the phenyl esters of heterocyclic acids and heterocyclic amines preparation procedure not given in the original. III (R = 4-pyridyl, R1 = H, CHMe2, CH2CHMe2; R = 3-pyridyl, R1 = CHMe2, R = 2-thienyl, R1 = CHMe2CH2CHMe2; R = 2-furyl, R1 = CHMe2, CH2CHMe2) had slight antitumor activity against Ehrlich ascites carcinoma and crocker sarcoma-180 in mice.

Yakugaku Zasshi published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C42H63O3P, Application In Synthesis of 51987-99-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics