Month: February 2022

An article Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5 WOS:000505633400007 published article about BINDING-SITE; SMALL-MOLECULE; POTENT; DRUGS in [Zacarias, Natalia V. Ortiz; van Veldhoven, Jacobus P. D.; den Hollander, Lisa S.; Dogan, Burak; Openy, Joseph; Hsiao, Ya-Yun; Lenselink, Eelke B.; Heitman, Laura H.; IJzerman, Adriaan P.] Leiden Univ, Div Drug Discovery & Safety, Leiden Acad Ctr Drug Res, POB 9502, NL-2300 RA Leiden, Netherlands in 2019.0, Cited 60.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Category: Triazoles

CC chemokine receptors 2 (CCR2) and 5 (CCR5) are involved in many inflammatory diseases; however, most CCR2 and CCR5 clinical candidates have been unsuccessful. (Pre)clinical evidence suggests that dual CCR2/CCR5 inhibition might be more effective in the treatment of such multifactorial diseases. In this regard, the highly conserved intracellular binding site in chemokine receptors provides a new avenue for the design of multitarget ligands. In this study, we synthesized and evaluated the biological activity of a series of triazolopyrimidinone derivatives in CCR2 and CCR5. Radioligand binding assays first showed that they bind to the intracellular site of CCR2, and in combination with functional assays on CCR5, we explored structure-affinity/activity relationships in both receptors. Although most compounds were CCR2-selective, 39 and 43 inhibited beta-arrestin recruitment in CCR5 with high potency. Moreover, these compounds displayed an insurmountable mechanism of inhibition in both receptors, which holds promise for improved efficacy in inflammatory diseases.

Welcome to talk about 61-82-5, If you have any questions, you can contact Zacarias, NVO; van Veldhoven, JPD; den Hollander, LS; Dogan, B; Openy, J; Hsiao, YY; Lenselink, EB; Heitman, LH; IJzerman, AP or send Email.. Category: Triazoles

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

An article Design, synthesis, characterization, and physical property determination of a new ionic liquid: the preparation of triazolo-pyrimidines at room temperature under metal-free conditions WOS:000557222500001 published article about AGENTS; ACID in [Shahnavaz, Zohreh; Khaligh, Nader Ghaffari; Johan, Mohd Rafie] Univ Malaya, Nanotechnol & Catalysis Res Ctr, Inst Postgrad Studies, Kuala Lumpur 50603, Malaysia; [Mihankhah, Taraneh] Iran Univ Sci & Technol, Sch Civil Engn, Dept Water & Environm Engn, Environm Res Lab, Tehran 16765163, Iran in 2020.0, Cited 19.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Name: 1H-1,2,4-Triazol-5-amine

A new ionic liquid is synthesized, and its chemical structure is characterized by FTIR, 1D NMR and 2D NMR, and mass analyses. The thermal behavior and thermal stability of this ionic liquid are investigated. The results approved the formation of 4,4MODIFIER LETTER PRIME-trimethylene-N,NMODIFIER LETTER PRIME-dipiperidinium sulfate instead of 4,4MODIFIER LETTER PRIME-trimethylene-N,NMODIFIER LETTER PRIME-dipiperidinium hydrogen sulfate. Moreover, the synthesis of triazolo-pyrimidine derivatives was successfully conducted in the presence of new ionic liquid at room temperature under metal-free conditions, which demonstrated the catalytic efficiency of this ionic liquid. The workup was carried out without the utilization of high-cost column chromatography. After extraction of desired products, the residual ionic liquid could be recycled and reused in the next runs. New ionic liquid exhibited high catalytic activity even after fifth run with no significant change in the chemical structure.

Welcome to talk about 61-82-5, If you have any questions, you can contact Shahnavaz, Z; Khaligh, NG; Mihankhah, T; Johan, MR or send Email.. Name: 1H-1,2,4-Triazol-5-amine

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Computed Properties of C2H4N4. In 2019.0 J MEMBRANE SCI published article about POLY(ARYLENE ETHER SULFONE)S; QUATERNARY AMMONIUM GROUPS; FUEL-CELL APPLICATIONS; SIDE-CHAINS; CROSS-LINKING; KETONE); BLOCK; CONDUCTIVITY; ELECTROLYTE; CATIONS in [Du, Xinming; Wang, Zhe; Zhang, Hongyu; Liu, Wenchang; Chen, Zhaoyu; Xu, Jingmei] Changchun Univ Technol, Coll Chem Engn, Changchun 130012, Jilin, Peoples R China; [Du, Xinming; Wang, Zhe; Xu, Jingmei] Changchun Univ Technol, Adv Inst Mat Sci, Changchun 130012, Jilin, Peoples R China in 2019.0, Cited 48.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.

A double-network anion exchange membrane (TA/AT-PEK/PVA-x) was prepared by Br-PEK and PVA, 3-amino-1,2,4 triazole forms a cross-linking structure with PVA under the action of 1,4-phthalaldehyde and then triazole can be linked with Br-PEK. The structure of membranes was verified by FT-IR. The composite membrane is uniform and smooth can be seen from the scanning electron microscope (SEM) and exhibit good hydrophilic/hydrophobic micro-phase separation structure proved by Transmission electron micrograph (TEM). The ionic conductivity of TA/AT-PEK/PVA-0.15 is 0.062 S/cm at 80 degrees C. With the addition of PVA within a certain range, the water uptake, swelling ratio hydroxide conductivity and alkaline stability are increase. The membranes are more flexible. After immersing in 4M NaOH solutions for 240 h at 80 degrees C, it remains at least 65% of its initial hydroxide ion conductivity of TA/AT-PEK/PVA-0.3 membrane. With the increasing number of water molecules solvating the hydroxide, its nucleophilicity and basicity were hindered, which enhance alkaline stability of anion exchange membranes.

About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Du, XM; Wang, Z; Zhang, HY; Liu, WC; Chen, ZY; Xu, JM or concate me.. Computed Properties of C2H4N4

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

An article An efficient synthesis of novel heterocyclic systems incorporating coumarin moiety WOS:000495758700001 published article about BIOLOGICAL EVALUATION; DERIVATIVES; DESIGN; FLUORESCENCE; INSIGHT; HYBRIDS in [El-Gohary, Nasser M.; El-Kazak, Azza M.; Ibrahim, Magdy A.] Ain Shams Univ, Fac Educ, Dept Chem, Cairo 11711, Egypt in 2020.0, Cited 33.0. Category: Triazoles. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

Polyfunctional 3-chloro-3-(4-chlorocoumarin-3-yl)prop-2-enal (1) used as a precursor for heterocyclic synthesis. Dichloro-aldehyde 1 was allowed to react with variable nucleophilic reagents, and a diversity of heterocyclic systems linked coumarin moiety at position 3 was synthesized. The reaction of compound 1 with guanidine and cyanoguanidine produced 3-(pyrimidin-4-yl)-4-chlorocoumarins 2 and 3. Treating compound 1 with 3-amino-1,2,4-triazole and 2-aminobenzimidazole yielded triazolo[4,3-a]pyrimidine 4 and pyrimido[1,2-a]benzimidazole 5. The treatment of compound 1 with cyanoacetamide, N-benzyl-2-cyanoacetamide, and 1H-benzimidazolylacetonitrile gave 2(1H)-pyridones 6, 7 and pyrido[1,2-a]benzimidazole 8. The reaction of compound 1 with 5-amino-3-methyl-1H-pyrazole and 6-aminouracil afforded pyrazolo[3,4-b]pyridine 9 and pyrido[2,3-d]pyrimidine 10, respectively. Compound 1 reacted with ethylenediamine, o-phenylenediamine, o-aminophenol, and o-aminothiophenol leading to 5-(imidazolylmethyl)chromeno[4,3-e] [1,4]diazepine (12), 3-(benzodiazepin/benzoxazepin-2-yl)-4-chlorocoumarins 13, 14, and 6-(benzothiazol-2-ylmethyl)chromeno[4,3-b][1,5]benzothiazepine 16, respectively. Structures of the new synthesized products were deduced on the basis of their analytical and spectral data.

Welcome to talk about 61-82-5, If you have any questions, you can contact El-Gohary, NM; El-Kazak, AM; Ibrahim, MA or send Email.. Category: Triazoles

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

An article The Rab5 activator RME-6 is required for amyloid precursor protein endocytosis depending on the YTSI motif WOS:000516383900001 published article about APP; TRANSPORT; SIGNALS; UBIQUITINATION; DEGRADATION; TRAFFICKING; MEMBRANE; INTERNALIZATION; LOCALIZATION; COMPONENTS in [Eggert, Simone; Gruebl, Tomas; Rajender, Ritu; Rupp, Carsten; Sander, Bianca; Heesch, Amelie; Zimmermann, Marius; Kins, Stefan] Tech Univ Kaiserslautern, Dept Human Biol & Human Genet, Erwin Schrodinger Str 13, D-67663 Kaiserslautern, Germany; [Hoepfner, Sebastian] MPI Mol Cell Biol & Genet, Dresden, Germany; [Hoepfner, Sebastian] Bird & Bird LLM, Munich, Germany; [Zentgraf, Hanswalter] DKFZ, Heidelberg, Germany in 2020.0, Cited 75.0. Formula: C2H4N4. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5

Endocytosis of the amyloid precursor protein (APP) is critical for generation of beta-amyloid, aggregating in Alzheimer’s disease. APP endocytosis depending on the intracellular NPTY motif is well investigated, whereas involvement of the YTSI (also termed BaSS) motif remains controversial. Here, we show that APP lacking the YTSI motif (Delta YTSI) displays reduced localization to early endosomes and decreased internalization rates, similar to APP Delta NPTY. Additionally, we show that the YTSI-binding protein, PAT1a interacts with the Rab5 activator RME-6, as shown by several independent assays. Interestingly, knockdown of RME-6 decreased APP endocytosis, whereas overexpression increased the same. Similarly, APP Delta NPTY endocytosis was affected by PAT1a and RME-6 overexpression, whereas APP Delta YTSI internalization remained unchanged. Moreover, we could show that RME-6 mediated increase of APP endocytosis can be diminished upon knocking down PAT1a. Together, our data identify RME-6 as a novel player in APP endocytosis, involving the YTSI-binding protein PAT1a.

Formula: C2H4N4. Welcome to talk about 61-82-5, If you have any questions, you can contact Eggert, S; Gruebl, T; Rajender, R; Rupp, C; Sander, B; Heesch, A; Zimmermann, M; Hoepfner, S; Zentgraf, H; Kins, S or send Email.

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

In 2020.0 J HETEROCYCLIC CHEM published article about ONE-POT SYNTHESIS; ASSISTED SYNTHESIS; REARRANGEMENT; HETEROCYCLES in [Kassem, Asmaa F.; Abbas, Eman M. H.] Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Chem Nat & Microbial Prod Dept, 33 Bohouth St,POB 12622, Giza, Egypt; [Al-Qurashi, Nadia T.] Umm Al Qura Univ, Univ Coll Adam, Dept Basic Sci, Mecca, Almukkarramah, Saudi Arabia; [Farghaly, Thoraya A.] Cairo Univ, Fac Sci, Dept Chem, Giza 1263, Egypt; [Farghaly, Thoraya A.] Umm Al Qura Univ, Fac Appl Sci, Dept Chem, Mecca 21514, Almukkarramah, Saudi Arabia in 2020.0, Cited 28.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. COA of Formula: C2H4N4

With aiding of microwave radiation, new series of fused-thiazolopyrimidines and fused-triazolopyrimidines each with cycloheptane have been synthesized through the reaction of cycloheptane-thione with alpha-haloketones or hydrazonoyl chlorides in short-time intervals as well as high yield. Moreover, reaction of 2,7-bis(2-chlorobenzylidene)cycloheptan-1-one with o-aminothiophenol and heterocyclic amines afforded benzo[b]cyclohepta[e][1,4]thiazepine derivative and cycloheptapyrimidines fused with different azoles, respectively. The structure for all products was discussed and proved based on the results of spectral data and elemental analysis. Evaluation of the antimicrobial activity of selected products indicated that most of derivatives showed their potent activity exceeds the reference antibiotic in some cases.

COA of Formula: C2H4N4. Welcome to talk about 61-82-5, If you have any questions, you can contact Kassem, AF; Abbas, EMH; Al-Qurashi, NT; Farghaly, TA or send Email.

Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics