Category: 35375-74-7

Catarzi, Daniela; Colotta, Vittoria; Varano, Flavia; Calabri, Francesca Romana; Filacchioni, Guido; Galli, Alessandro; Costagli, Chiara; Carla, Vincenzo published the artcile< Synthesis and Biological Evaluation of Analogues of 7-Chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic Acid (TQX-173) as Novel Selective AMPA Receptor Antagonists>, Quality Control of 35375-74-7, the main research area is TQX 173 preparation AMPA receptor antagonist; carboxypyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; pyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; triazolyl pyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; imidazolyl pyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; amino pyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; kainate aminopyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; neuroprotective aminopyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; anticonvulsant aminopyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist; cytoprotective aminopyrrolyl triazoloquinoxalinecarboxylate TQX 173 preparation AMPA receptor antagonist.

In recent papers (Catarzi, D.; et al. J. Med. Chem. 2000, 43, 3824-3826; 2001, 44, 3157-3165) the authors reported chem. and biol. studies on 4,5-dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates (TQXs) bearing different nitrogen-containing heterocycles at position-8. In particular, from these studies it emerged that both the 7-chloro-4,5-dihydro-4-oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid TQX-173 and its corresponding Et ester were the most active and selective compounds of this series. In pursuing the investigation on the structure-activity relationships of these TQX derivatives, different electron-withdrawing groups (CF3, NO2) were introduced at position 7 on the TQX ring system, replacing the 7-chloro substituent of TQX-173 and of other selected 8-heteroaryltriazoloquinoxaline-2-carboxylates previously described. All the newly synthesized compounds were biol. evaluated for their binding at the Gly/NMDA, AMPA, and KA high-affinity receptors. Gly/NMDA binding assays were performed to assess the selectivity of the reported compounds toward the AMPA receptor. Compounds endowed with micromolar binding affinity for the KA high-affinity binding site were also evaluated for their binding at the KA low-affinity receptor. Some selected compounds were also tested for their functional antagonist activity at the AMPA and NMDA receptor-ion channel complex. The results obtained in this study have pointed out that 4,5-dihydro-7-nitro-4-oxo-8-(3-carboxypyrrol-1-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid and its corresponding Et ester are the most potent and selective AMPA receptor antagonists reported to date among the TQX series.

Journal of Medicinal Chemistry published new progress about AMPA receptors Role: BCP (Biochemical Process), BIOL (Biological Study), PROC (Process) (AMPA receptor antagonists). 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, Quality Control of 35375-74-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Plashkina, N. A.; Troitskaya, V. I.; Pushkareva, Z. V.; Ryapasova, T. P. published the artcile< Studies on riboflavine analogs. VIII. 7-(Trifluoromethyl)-8-chloroisoalloxazines>, Synthetic Route of 35375-74-7, the main research area is isoalloxazine chlorotrifluoromethyl; cyclocondensation alloxan ribityltoluidine; galactyltoluidine cyclocondensation; sorbityltoluidine cyclocondensation; rhamnityltoluidine cyclocondensation.

Chlorotoluidines I (R = H, Me, CH2CH2OH, ribityl, galactyl, sorbityl, rhamnityl), prepared in 72-95% yields by amination of the corresponding dichlorotoluene with RNH2, were reduced by Raney Ni and cyclized with alloxan to give 63-85% isoalloxazines II.

Khimiya Geterotsiklicheskikh Soedinenii published new progress about Condensation reaction. 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, Synthetic Route of 35375-74-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gable, Jonathan E.; Lee, Gregory M.; Acker, Timothy M.; Hulce, Kaitlin R.; Gonzalez, Eric R.; Schweigler, Patrick; Melkko, Samu; Farady, Christopher J.; Craik, Charles S. published the artcile< Fragment-Based Protein-Protein Interaction Antagonists of a Viral Dimeric Protease>, HPLC of Formula: 35375-74-7, the main research area is fragment based screening inhibitor binding dimer interface KSHV protease; NMR spectroscopy; dimer disruption; fragment-based screening; human herpesviruses; proteases.

Fragment-based drug discovery has shown promise as an approach for challenging targets such as protein-protein interfaces. We developed and applied an activity-based fragment screen against dimeric Kaposi’s sarcoma-associated herpesvirus protease (KSHV Pr) using an optimized fluorogenic substrate. Dose-response determination was performed as a confirmation screen, and NMR spectroscopy was used to map fragment inhibitor binding to KSHV Pr. Kinetic assays demonstrated that several initial hits also inhibit human cytomegalovirus protease (HCMV Pr). Binding of these hits to HCMV Pr was also confirmed by NMR spectroscopy. Despite the use of a target-agnostic fragment library, more than 80 % of confirmed hits disrupted dimerization and bound to a previously reported pocket at the dimer interface of KSHV Pr, not to the active site. One class of fragments, an aminothiazole scaffold, was further explored using com. available analogs. These compounds demonstrated greater than 100-fold improvement of inhibition. This study illustrates the power of fragment-based screening for these challenging enzymic targets and provides an example of the potential druggability of pockets at protein-protein interfaces.

ChemMedChem published new progress about Enzyme functional sites, inhibitor-binding. 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, HPLC of Formula: 35375-74-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gilfillan, Lynne; Blair, Adele; Morris, Brian J.; Pratt, Judith A.; Schweiger, Lutz; Pimlott, Sally; Sutherland, Andrew published the artcile< Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor>, Recommanded Product: 5-Chloro-2-nitro-4-(trifluoromethyl)aniline, the main research area is dihydrobenzodiazepinone preparation PET SPECT imaging agent.

A focused library of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones containing sites for 11C-, 18F- and 123I-labeling were prepared and evaluated against membrane expressing human recombinant metabotropic glutamate 2 receptor (mGluR2). The compounds are non-competitive antagonists with nanomolar affinity. HPLC evaluation of the physiochem. properties of these compounds identified two candidates for PET and SPECT imaging of mGluR2.

MedChemComm published new progress about Combinatorial library. 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, Recommanded Product: 5-Chloro-2-nitro-4-(trifluoromethyl)aniline.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics