Category: Triazoles

HPLC of Formula: 65705-44-4. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine, is researched, Molecular C10H9BrN2S, CAS is 65705-44-4, about Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening. Author is Agrawal, Madhavi; Kharkar, Prashant; Moghe, Sonali; Mahajan, Tushar; Deka, Vaishali; Thakkar, Chandni; Nair, Amrutha; Mehta, Chirag; Bose, Julie; Kulkarni-Almeida, Asha; Bhedi, Dilip; Vishwakarma, Ram A..

With the aim to discover orally active small mols. that stimulate glucose uptake, high throughput screening of a library of 5000 drug-like compounds was conducted in differentiated skeletal muscle cells in presence of insulin. N-Substituted phthalazinone acetamide was identified as a potential glucose uptake modulator. Several novel derivatives were synthesized to establish structure activity relationships. Identified lead thiazolyl-phthalazinone acetamide (7114863; I) increased glucose uptake (EC50 of 0.07±0.02 μM) in differentiated skeletal muscle cells in presence of insulin. Furthermore, I was superior to rosiglitazone under similar exptl. conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Safety of 4-(4-Bromophenyl)-5-methylthiazol-2-amine. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine, is researched, Molecular C10H9BrN2S, CAS is 65705-44-4, about Unique Sulfur-Aromatic Interactions Contribute to the Binding of Potent Imidazothiazole Indoleamine 2,3-Dioxygenase Inhibitors. Author is Peng, Yi-Hui; Liao, Fang-Yu; Tseng, Chen-Tso; Kuppusamy, Ramajayam; Li, An-Siou; Chen, Chi-Han; Fan, Yu-Shiou; Wang, Sing-Yi; Wu, Mine-Hsine; Hsueh, Ching-Cheng; Chang, Jia-Yu; Lee, Lung-Chun; Shih, Chuan; Shia, Kak-Shan; Yeh, Teng-Kuang; Hung, Ming-Shiu; Kuo, Ching-Chuan; Song, Jen-Shin; Wu, Su-Ying; Ueng, Shau-Hua.

Indoleamine 2,3-dioxygenase (IDO1) inhibitors are speculated to be useful in cancer immunotherapy, but a phase III clin. trial of the most advanced IDO1 inhibitor, epacadostat, did not meet its primary endpoint and was abandoned. In previous work we identified the novel IDO1 inhibitor N-(4-chlorophenyl)-2-((5-phenylthiazolo[2,3-c][1,2,4]triazol-3-yl)thio)acetamide 1 through high-throughput screening (HTS). Herein, we report a structure-activity relationship (SAR) study of this compound, which resulted in the potent IDO1 inhibitor 1-(4-cyanophenyl)-3-(3-(cyclopropylethynyl)imidazo[2,1-b]thiazol-5-yl)thiourea 47 (hIDO IC50 = 16.4 nM). X-ray co-crystal structural anal. revealed that the basis for this high potency is a unique sulfur-aromatic interaction network formed by the thiourea moiety of 47 with the F163 and F226. This finding is expected to inspire new approaches towards the discovery of potent IDO1 inhibitors in the future.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

SDS of cas: 3222-47-7. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 6-Methylnicotinic acid, is researched, Molecular C7H7NO2, CAS is 3222-47-7, about Unexpected small molecules as novel SIRT2 suicide inhibitors. Author is Chen, Xiaoxue; Zou, Yefang; Wang, Jie; Cao, Zhuoxian; Liu, Jingzi; Li, Yan; Zhao, Yonglong; He, Bin.

A series of sirtuin inhibitor candidates were assembled based on an intermediate ester (1a) our accidently discovered. After screening and evaluation, several SIRT2 selective inhibitors were identified, which can inhibit all the deacetylation, defatty-acylation and debenzoylation of SIRT2. Among these inhibitors, compound 1e was the best SIRT2 selective inhibitors. The primary study on the inhibitory mechanism indicated that compound 1e may be a suicide inhibitor acting as an irreversible way. Given almost all reported sirtuin inhibitors are non-covalent, sirtuin covalent inhibitors are still need to be developed. These findings will facilitate for further development of SIRT2 selective and suicide inhibitors.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ) is researched.Related Products of 86404-63-9.Ramesh, B.; Narayana, P. Sreeman; Reddy, A. Shiva; Devi, P. Sita published the article 《Spectrodensitometric evaluation and determination of fluconazole and its impurities in pharmaceutical formulations by high performance thin layer chromatography》 about this compound( cas:86404-63-9 ) in Journal of Pharmacy Research. Keywords: fluconazole impurity determination densitometry HPTLC. Let’s learn more about this compound (cas:86404-63-9).

A quant. densitometric HPTLC method was developed and validated for the determination of fluconazole and its structurally related impurities. The separations were accomplished on silica gel 60 F254 plates using a saturated mixture of butanol: water: acetic acid (8:2:1 volume/volume). UV light facilitated the visualization of the active drug substance fluconazole and impurity-e while impurity-b was visible only when exposed to iodine vapors, as dark brown chromatog. zone. Densitometric quantification was performed at λ = 254nm by reflecting scanning and fluconazole (Rr 0.67 ± 0.02) resolved well from the 2 impurities. The standard fluconazole curve is linear (r = > 0.9995) over a concentration range of 1-6 μg/spot. Recovery from tablet formulation was statistically equal to 100%. The limits of detection and quantification were 0.031 and 0.098 μg/spot resp. The precision of the method with respect to concentration is acceptable with a relative standard deviation of 2%. The proposed method is specific for fluconazole in the presence of its structurally related impurities and proved to be a valuable complimentary method for impurity profiling and quality control.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Kawashita, Seiji; Aoyagi, Koichi; Yamanaka, Hiroshi; Hantani, Rie; Naruoka, Shiori; Tanimoto, Atsuo; Hori, Yuji; Toyonaga, Yukiyo; Fukushima, Kyoko; Miyazaki, Susumu; Hantani, Yoshiji published an article about the compound: 5-(Chloromethyl)nicotinonitrile( cas:562074-59-3,SMILESS:N#CC1=CN=CC(CCl)=C1 ).Related Products of 562074-59-3. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:562074-59-3) through the article.

The development of small mol. inhibitors of PD-1/PD-L1 is eagerly anticipated for treatment of cancer. We focused on the symmetry of the ternary complex structure of reported small mol. ligands and hPD-L1 homodimers, and designed partially- or fully-sym. compounds for more potent inhibitors. The design of the new compounds was guided by our hypothesis that the designed sym. compound would induce a flip of sidechain of ATyr56 protein residue to form a new cavity. The designed compound 4 exhibited substantially increased binding affinity to hPD-L1, as well as PD-1/PD-L1 inhibitory activity in physiol. conditions. Compound 4 also showed a dose-dependent increase in IFN-γ secretion levels in a mixed lymphocyte reaction assay. These results not only indicate the feasibility of targeting the PD-1/PD-L1 pathway with small mols., but illustrate the applicability of the symmetry-based ligand design as an attractive methodol. for targeting protein-protein interaction stabilizers.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 86404-63-9, is researched, Molecular C10H7F2N3O, about Studies on synthesis, structure and biological activities of novel triazole compounds containing thioamide, the main research direction is triazole thioamide preparation triazole isothiocyanate aryl ketone; benzoyl triazole ethanethioamide preparation agrochem fungicide.Quality Control of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

Four novel triazole compounds containing thioamide group were designed and synthesized by using triazole, Ph isothiocyanate and aryl Et ketones as starting materials. The desired intermediates were thus derivatives of α-(1H-1,2,4-triazol-1-yl)methyl ketones. Their structures were confirmed by elemental anal., 1H NMR, IR and MS spectra. The crystal structure of 1-[1-[(anilino)thiocarbonyl]-1-(4-fluorobenzoyl)methyl]-1,2,4-triazole [also, i.e., α-(fluorobenzoyl)-N-phenyl-1,2,4-triazole-1-ethanethioamide] has been determined by X-ray diffraction anal. The preliminary bioassays have shown that the title compounds exhibit certain antifungal activity.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives, published in 2010-05-01, which mentions a compound: 86404-63-9, mainly applied to triazolylpropanol piperidinone oxime ether containing derivative preparation antifungal activity; mol docking CACYP51 triazolylpropanol piperidinone oxime ether containing derivative, Related Products of 86404-63-9.

In an attempt to find novel azole antifungal agents with improved activity and broader spectrum, computer modeling was used to design a series of new azoles with piperidin-4-one O-substituted oxime side chains. Mol. docking studies revealed that they formed hydrophobic and hydrogen-bonding interactions with lanosterol 14α-demethylase of Candida albicans (CACYP51). In vitro antifungal assay indicates that most of the synthesized compounds showed good activity against tested fungal pathogens. In comparison with fluconazole, itraconazole and voriconazole, several compounds (such as I, R = H, 3-Cl, 2-F) show more potent antifungal activity and broader spectrum, suggesting that they are promising leads for the development of novel antifungal agents.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Liessi, Nara; Cichero, Elena; Pesce, Emanuela; Arkel, Maria; Salis, Annalisa; Tomati, Valeria; Paccagnella, Matteo; Damonte, Gianluca; Tasso, Bruno; Galietta, Luis J. V.; Pedemonte, Nicoletta; Fossa, Paola; Millo, Enrico published the article 《Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools》. Keywords: thiazole VX809 hybrid cystic fibrosis deletion mutation corrector QSAR; Aminoarylthiazole; CFTR; Corrector; Cystic fibrosis; QSAR; VX809.They researched the compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine( cas:65705-44-4 ).Synthetic Route of C10H9BrN2S. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:65705-44-4) here.

The most common CF mutation, F508del, impairs the processing and gating of CFTR protein. This deletion results in the improper folding of the protein and its degradation before it reaches the plasma membrane of epithelial cells. Present correctors, like VX809 only induce a partial rescue of the mutant protein. Our previous studies reported a class of compounds, called aminoarylthiazoles (AATs), featuring an interesting activity as correctors. Some of them show additive effect with VX-809 (I) indicating a different mechanism of action. In an attempt to construct more interesting mols., it was thought to generate chem. hybrid compounds, blending a portion of VX-809 merged to the thiazole scaffold. This approach was guided by the development of QSAR analyses, which were performed based on the F508del correctors so far disclosed in the literature. This strategy was aimed at exploring the key requirements turning in the corrector ability of the collected derivatives and allowed us to derive a predictive model guiding for the synthesis of novel hybrids as promising correctors. The new mols. were tested in functional and biochem. assays on bronchial CFBE41o-cells expressing F508del-CFTR showing a promising corrector activity.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Bioorganic & Medicinal Chemistry Letters called Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols, Author is Chai, Xiaoyun; Zhang, Jun; Yu, Shichong; Hu, Honggang; Zou, Yan; Zhao, Qingjie; Dan, Zhigang; Zhang, Dazhi; Wu, Qiuye, which mentions a compound: 86404-63-9, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3O, Reference of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

Based on the results of computational docking to the active site of the cytochrome P 450 14α-demethylase (CYP51), a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols, e.g., I, as analogs of fluconazole were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all the title compounds exhibited excellent activities with broad spectrum.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 86404-63-9, is researched, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3OJournal, Inorganica Chimica Acta called Four novel Co(II) and Mn(II) coordination polymers with triazolyl derivate: Syntheses, crystal structures and magnetic properties, Author is Zhang, Lei; Ling, Yun; Hu, Ai-Xi; Yao, Ting-Ting; Li, Jing, the main research direction is manganese cobalt fluorophenyltriazolylethanone azido dicyanamide polymeric preparation antiferromagnetic ferromagnetic; crystal structure manganese cobalt fluorophenyltriazolylethanone azido dicyanamide coordination polymer.COA of Formula: C10H7F2N3O.

Four novel coordination polymers, 1-dimensional chains [M(PTE)2(N3)2]n (M = Mn for 1 and Co for 2), and two-dimensional layers [M(PTE)2(dca)2]n (M = Mn for 3 and Co for 4) (PTE = 1-(2,4-difluorophenyl-2-(1H-1,2,4-triazol-1-yl)ethanone), dca = dicyanamide anion, N(CN)2 -), were synthesized under mild ambient conditions and structurally characterized by single crystal x-ray diffraction. In all four crystal structures, the metal atoms adopt octahedral coordination geometry with six N atoms from two monodentate PTE ligands and four azido (or dca) bridging ligands. The crystal structures of 1 and 2 are isostructural 1-dimensional polymeric chains, alternatively linked by double end-on and double end-to-end azido bridges. However, the bent dca ligands as bidentate μ2-1,5 bridging ligands interlink the octahedral metal units to lead to 2-dimensional (4,4) grid networks in 3 and 4. Temperature-dependent magnetic measurements in 2-300 K were performed for these four polymers, and suggest alternative ferro- and antiferromagnetic couplings for end-on and end-to-end azido bridges in 1, and the dominant ferromagnetic coupling in 2, resp. Both polymers 3 and 4 show weak antiferromagnetic exchanges through the μ2-1,5-dca bridges. The effects of auxiliary coligands on the structure and the nature of these magnetic exchanges are discussed in the light of the crystal structures.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics