126799-84-6

Upstream product

• 3958-57-4 1-bromomethyl-3-nitrobenzene 
• 619-25-0 3-Nitrobenzyl alcohol 
• 121-92-6 3-nitrobenzoic acid 
• 99-08-1 1-methyl-3-nitrobenzene 
• 619-23-8 3-Nitrobenzyl chloride 
• 99-61-6 3-nitro-benzaldehyde 

Downstream Products

• 141072-11-9 methyl 1-(3-nitrobenzyl)-1H-1,2,3-triazole-4-carboxylate 
• 141071-98-9 di-tert-butyl 1-(3-nitrobenzyl)-1H-1,2,3-triazole-4,5-dicarboxylate 
• 126800-29-1 ethyl 1-(3-nitrobenzyl)-1H-1,2,3-triazole-4-carboxylate 
• 4403-70-7 m-aminobenzylamine 
• 7409-18-9 3-nitrobenzylamine 
• 99-61-6 3-nitro-benzaldehyde 
• 1569352-18-6 6-bromo-N-(2-(cyclohexylamino)-1-(2-((1-(3-nitrophenyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-2-oxoethyl)-2-oxo-N-(p-tolyl)-2H-chromene-3-carboxamide 
• 1569352-20-0 6-bromo-N-(4-chlorophenyl)-N-(2-(cyclohexylamino)-1-(2-((1-(3-nitrophenyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-2-oxoethyl)-2-oxo-2H-chromene-3-carboxamide 
• 1569352-21-1 6-bromo-N-(2-(cyclohexylamino)-1-(2-((1-(3-nitrophenyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-2-oxoethyl)-N-(4-methoxyphenyl)-2-oxo-2H-chromene-3-carboxamide 
• 1569352-23-3 6-bromo-N-(2-(cyclohexylamino)-1-(5-methoxy-2-((1-(3-nitrophenyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-2-oxoethyl)-2-oxo-N-(p-tolyl)-2H-chromene-3-carboxamide 

Relevant academic research and scientific papers

A Photoregulated Racemase Mimic

The racemase enzymes convert L-amino acids to their D-isomer. The reaction proceeds through a stepwise deprotonation–reprotonation mechanism that is assisted by a pyridoxal phosphate (PLP) coenzyme. This work reports a PLP–photoswitch–imidazole triad where the racemization reaction can be controlled by light by tweaking the distance between the basic residue and the reaction centre.

Synthesis of 1,2,3-triazole benzophenone derivatives and evaluation of in vitro sun protection, antioxidant properties, and antiproliferative activity on HT-144 melanoma cells

Benzophenones display several biological activities, including antioxidant, anticancer, and photoprotective. Furthermore, antioxidants can minimize both ultraviolet absorption and tumor development. In the present investigation, a series of twenty-six 1,2

Design, synthesis, and evaluation of metronidazole-1,2,3-triazole derivatives as potent urease inhibitors

A new series of metronidazole-1,2,3-triazole derivatives 6a–o was synthesized and evaluated as Helicobacter pylori urease inhibitors. All the synthesized compounds were more potent than standard inhibitor thiourea against urease. Among the synthesized compounds, compound 6f (IC50 = 1.975 ± 0.25?μM) with inhibitory activity around 11-fols more than thiourea (IC50 = 22.00 ± 0.14?μM) was the most potent compound. Kinetic study of this compound revealed that compound 6f inhibited urease in an uncompetitive mode. Based on molecular modeling study, compound 6f pointed toward the bi-nickel center and stabilized by H-bond and T-shape π–π hydrophobic interactions with the critical residues His492 and Asp633. Moreover, it anchored to the helix-turn-helix motif in the active site cavity through interaction with His593 and Arg609. Consequently, it proposed that compound 6f through stabilization of active site flap inhibited urease activity.

Thymol as an Interesting Building Block for Promising Fungicides against Fusarium solani

The semisynthesis of 15 new thymol derivatives was achieved through Williamson synthesis and copper-catalyzed azide-alkyne cycloaddition (CuAAC) approaches. The reaction of CuAAC using the "Click Chemistry"strategy, in the presence of an alkynyl thymol de

Synthesis of 1,2,3,triazole modified analogues of hydrochlorothiazide via click chemistry approach and in-vitro α-glucosidase enzyme inhibition studies

The current study was aimed to discover potent inhibitors of α-glucosidase enzyme. A 25 membered library of new 1,2,3-triazole derivatives of hydrochlorothiazide (1) (HCTZ, a diuretic drug also being used for the treatment of high blood pressure) was synt

Design, synthesis, biological evaluation, and docking study of new acridine-9-carboxamide linked to 1,2,3-triazole derivatives as antidiabetic agents targeting α-glucosidase

A new series of acridine-9-carboxamide-1,2,3-triazole derivatives 7a-m were designed, synthesized, and evaluated as novel α-glucosidase inhibitors. Acridine-9-carboxamide-1,2,3-triazole scaffold has been designed by combination of effective moieties from potent α-glucosidase inhibitors. Most of the synthesized compounds were more potent than standard inhibitor acarbose. Among the title compounds, the most potent compounds were compounds 7j, 7k, and 7a with IC50 values of 120.2 ± 1.0, 151.1 ± 1.4, and 157.6 ± 1.6 μM, respectively (IC50 value of acarbose = 750.0 ± 10.0 μM). Docking study of the most potent compounds demonstrated that these compounds formed stable complexes with α-glucosidase active site. Anti-α-amylase assay of compounds 7j, 7k, and 7a was performed and no activity was observed. in vitro cytotoxicity assay of the latter compounds revealed that these compounds were not cytotoxic toward human normal (HDF) and cancer (MCF-7) cell lines. ADME and toxicity prediction of compounds 7j, 7k, and 7a were also performed.

Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries

Cell division cycle 25 (Cdc25) protein phosphatases play key roles in the transition between the cell cycle phases and their association with various cancers has been widely proven, which makes them ideal targets for anti-cancer treatment. Though several Cdc25 inhibitors have been developed, most of them displayed low activity and poor subtype selectivity. Therefore, it is extremely important to discover novel small molecule inhibitors with potent activities and significant selectivity for Cdc25 subtypes, not only served as drugs to treat cancer but also to probe its mechanism in transitions. In this study, miniaturized parallel click chemistry synthesis via CuAAC reaction followed by in situ biological screening were used to discover selective Cdc25 inhibitors. The bioassay results showed that compound M2N12 proved to be the most potent Cdc25 inhibitor, which also act as a highly selective Cdc25C inhibitor and was about 9-fold potent than that of NSC 663284. Moreover, M2N12 showed remarkable anti-growth activity against the KB-VIN cell line, equivalent to that of PXL and NSC 663284. An all-atom molecular dynamics (MD) simulation approach was further employed to probe the significant selectivity of M2N12 for Cdc25C relative to its structural homologs Cdc25A and Cdc25B. Overall, above results make M2N12 a promising lead compound for further investigation and structural modification.

Carcarinic acid-1, 2, 3- based triazole compound as well as preparation method and application thereof (by machine translation)

The method comprises the following steps: firstly 1, 2, 3 - oxidizing and opening the carbon- carbon double bond of the, carcarinic acid into methylene to, obtain carcarinic acid (not shown, in the technical field of, organic 3 - synthesis), Wolf - Kishner - 1, 2, 3 - 1, 2, 3 - 1, 2, 3 - 3 . (by machine translation)

Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry

The over-expression of aminopeptidase N on diverse malignant cells is associated with the tumor angiogenesis and metastasis. In this report, one new series of leucine ureido derivatives containing the triazole moiety was designed, synthesized and evaluated as APN inhibitors. Among them, compound 13v showed the best APN inhibition with an IC50 value of 0.089 ± 0.007 μM, which was two orders of magnitude lower than that of bestatin (IC50 = 9.4 ± 0.5 μM). Compound 13v also showed dose-dependent anti-angiogenesis activities. Even at the lower concentration (10 μM), compound 13v presented similar anti-angiogenesis activity compared with bestatin at 100 μM in both the human umbilical vein endothelial cells (HUVECs) capillary tube formation assay and the rat thoracic aorta rings test. Moreover, compared with bestatin, 13v exhibited comparable, if not better in vivo anti-metastasis activity in a mouse H22 pulmonary metastasis model.

COMPOUNDS AND METHODS FOR REGULATING INSULIN SECRETION

Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods.