Month: November 2022

McCrary, Parker D. published the artcileHypergolic ionic liquids to mill, suspend, and ignite boron nanoparticles, HPLC of Formula: 39602-93-2, the main research area is energetic hypergolic ionic liquid milling suspension boron nanoparticle ignition.

Boron nanoparticles prepared by milling in the presence of a hypergolic energetic ionic liquid (EIL) are suspendable in the EIL and the EIL retains hypergolicity leading to the ignition of the boron. This approach allows for incorporation of a variety of nanoscale additives to improve EIL properties, such as energetic d. and heat of combustion, while providing stability and safe handling of the nanomaterials.

Chemical Communications (Cambridge, United Kingdom) published new progress about Combustion enthalpy. 39602-93-2 belongs to class triazoles, name is 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, and the molecular formula is C3H7IN4, HPLC of Formula: 39602-93-2.

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

Xue, Hong published the artcileEnergetic Salts from N-Aminoazoles, Formula: C3H7IN4, the main research area is triazolium amino nitrate perchlorate preparation thermal property thermochem density; tetrazolium amino nitrate perchlorate preparation thermal property thermochem density.

New energetic salts (1-amino-1,2,4-triazolium nitrate and perchlorate, 1-amino-4-methyl-1,2,4-triazolium nitrate and perchlorate, 1,5-diamino-1,2,4-triazolium nitrate and perchlorate, and 2-amino-4,5-dimethyltetrazolium nitrate and perchlorate) were synthesized via the quaternization of the corresponding N-aminoazoles with nitric or perchloric acid or with iodomethane followed by metathesis reaction with silver nitrate or silver perchlorate. The structure of 2-amino-4,5-dimethyltetrazolium nitrate was confirmed by single-crystal X-ray anal. Most of the salts exhibit good thermal stabilities and low m.ps. By using exptl. determined constant volume combustion energies, the standard molar enthalpies of formation were derived on the basis of designed Hess thermochem. cycles.

Inorganic Chemistry published new progress about Combustion enthalpy. 39602-93-2 belongs to class triazoles, name is 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, and the molecular formula is C3H7IN4, Formula: C3H7IN4.

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

Zhang, Hong published the artcileThe synthesis and energetic properties of pyridinium and triazolium N-(nitrobenzoyl)-imides, Quality Control of 39602-93-2, the main research area is pyridinium triazolium nitrobenzoyl imide energetic property.

Syntheses of nitrogen rich, energetic N-(nitro-substituted-benzoylimino)pyridinium and N-(nitrosubstituted-benzoylimino)1,2,4-triazolium imides are reported and their energetic properties calculated/determined in terms of heats of formation (HOF), densities, detonation parameters, heats of decomposition and heats of combustion.

ARKIVOC (Gainesville, FL, United States) published new progress about Combustion enthalpy. 39602-93-2 belongs to class triazoles, name is 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, and the molecular formula is C3H7IN4, Quality Control of 39602-93-2.

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

Iwamura, Ryo published the artcileIdentification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl, SDS of cas: 143426-50-0, the main research area is prostanoid EP2 receptor agonist preparation glaucoma.

EP2 receptor agonists are expected to be effective ocular hypotensive agents; however, it has been suggested that agonism to other EP receptor subtypes may lead to undesirable effects. Through medicinal chem. efforts, we identified a scaffold bearing a (pyridin-2-ylamino)acetic acid moiety as a promising EP2-selective receptor agonist. (6-((4-(Pyrazol-1-yl)benzyl)(pyridin-3-ylsulfonyl)aminomethyl)pyridin-2-ylamino)acetic acid 13ax (omidenepag, OMD) exerted potent and selective activity toward the human EP2 receptor (h-EP2). Low doses of omidenepag iso-Pr (OMDI), a prodrug of 13ax, lowered intraocular pressure (IOP) in ocular normotensive monkeys. OMDI was selected as a clin. candidate for the treatment of glaucoma.

Journal of Medicinal Chemistry published new progress about Antiglaucoma agents. 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, SDS of cas: 143426-50-0.

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

Wagman, Allan S. published the artcileSynthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3, Application of 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is imidazolyl phenylpyrimidinyl pyridylaminoethylamine preparation glycogen synthase kinase inhibitory activity.

In an effort to identify new antidiabetic agents, we have discovered a novel family of (5-imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine analogs which are inhibitors of human glycogen synthase kinase 3 (GSK3). We developed efficient synthetic routes to explore a wide variety of substitution patterns and convergently access a diverse array of analogs. Compound I (CHIR-911, CT-99021, or CHIR-73911) emerged from an exploration of heterocycles at the C-5 position, Ph groups at C-4, and a variety of differently substituted linker and aminopyridine moieties attached at the C-2 position. These compounds exhibited GSK3 IC50s in the low nanomolar range and excellent selectivity. They activate glycogen synthase in insulin receptor-expressing CHO-IR cells and primary rat hepatocytes. Evaluation of lead compounds I and II (CHIR-611 or CT-98014) in rodent models of type 2 diabetes revealed that single oral doses lowered hyperglycemia within 60 min, enhanced insulin-stimulated glucose transport, and improved glucose disposal without increasing insulin levels.

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Application of 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.

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

Esteban-Parra, Gines M. published the artcileAnti-diabetic and anti-parasitic properties of a family of luminescent zinc coordination compounds based on the 7-amino-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine ligand, SDS of cas: 24415-66-5, the main research area is crystal structure antidiabetic antiparasitic activity zinc triazolopyrimidine complex preparation; MO luminescence zinc triazolopyrimidine complex; 7-Amino-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine ligand; Chagas; Diabetes; Lesihmaniasis; Luminescence; Zinc.

We report on the formation of a triazolopyrimidine derivative ligand, 7-amino-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine (7-amtp), and a new family of coordination compounds based on this ligand and zinc as metal ion, synthesized by conventional routes. These materials possess different mononuclear structures, namely [ZnCl2(7-amtp)2] (1), [Zn(7-amtp)2(H2O)4](NO3)2·2(7-amtp)·6H2O (2) and [Zn(7-amtp)2(H2O)4](SO4)·1.5H2O (3) derived from the use of different zinc (II) salts, in such a way that the counterions govern the crystallization to a large extent. These compounds present and show variable luminescent properties based on ligand-centered charge transfers which have been deeply studied by Time Dependent D. Functional Theory (TD-DFT) calculations When these compounds are transferred to solution, preserving complex entities as corroborated by NMR studies, they present interesting anti-diabetic and anti-parasitic capabilities, with a comparatively higher selectivity index than other previously reported triazolopyrimidine-based materials. The results derived from in vivo experiments conducted in mice also confirm their promising activity as anti-diabetic drug being capable of dropping glucose levels after oral administration. Therefore, these new materials may be considered as excellent candidates to be further investigated in the field of luminescent coordination compounds with biomedical applications.

Journal of Inorganic Biochemistry published new progress about Antidiabetic agents. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, SDS of cas: 24415-66-5.

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

Cox, Jason M. published the artcileThe discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors, Application of 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, the main research area is tricyclic pyrrolidine preparation DPP4 inhibitor structure diabetes; Dipeptidyl peptidase IV (DPP-4); Omarigliptin; Sitagliptin; Type 2 diabetes mellitus.

Novel potent and selective 5,6,5- and 5,5,6-tricyclic pyrrolidine dipeptidyl peptidase IV (DPP-4) inhibitors were identified. Structure-activity relationship (SAR) efforts focused on improving the intrinsic DPP-4 inhibition potency, increasing protease selectivity, and demonstrating clean ion channel and cytochrome P 450 profiles while trying to achieve a pharmacokinetic profile suitable for once weekly dosing in humans.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Application of 5-Cyclopropyl-4H-1,2,4-triazol-3-amine.

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

Clough, John M. published the artcileSynthesis and evaluation of hydroxyazolopyrimidines as herbicides; the generation of amitrole in planta, HPLC of Formula: 502546-41-0, the main research area is hydroxyazolopyrimidine amitrole herbicide azolopyrimidine; amitrole; herbicides; metabolism; mode of action.

BACKGROUND : Exploiting novel herbicidal modes of action is an important method to overcome the challenges faced by increasing resistance and regulatory pressure on existing com. herbicides. Recent reports of inhibitors of enzymes in the non-mevalonate pathway of isoprenoid biosynthesis led to the design of a novel class of azolopyrimidines which were assessed for their herbicidal activity. Studies were also undertaken to determine the mode of action responsible for the observed herbicidal activity. RESULTS : In total, 30 novel azolopyrimidines were synthesized and their structures were unambiguously determined by 1H NMR, mass spectroscopy and X-ray crystallog. anal. The herbicidal activity of this new chem. class was assessed against six common weed species, with compounds from this series displaying bleaching symptomol. in post-emergence tests. A structure-activity relationship for the novel compounds was determined, which showed that only those belonging to the hydroxytriazolopyrimidine subclass displayed significant herbicidal activity. Observed similarities between the bleaching symptomol. displayed by these herbicides and amitrole suggested that hydroxytriazolopyrimidines could be acting as elaborate propesticides of amitrole, and this was subsequently demonstrated in plant metabolism studies using Amaranthus retroflexus. It was shown that selected hydroxytriazolopyrimidines that displayed promising herbicidal activity generated amitrole, with peak concentrations of amitrole generally being observed 1 day after application. Addnl., the herbicidal activity of selected compounds was profiled against tobacco plants engineered to overexpress 4-diphosphocytidyl-2C-methyl-D-erythritol synthase (IspD) or lycopene β-cyclase, and the results suggested that, where significant herbicidal activity was observed, inhibition of IspD was not responsible for the activity. Tobacco plants overexpressing lycopene β-cyclase showed tolerance to amitrole and the two most herbicidally active triazolopyrimidines. CONCLUSIONS : Inhibition of IspD leading to herbicidal activity has been ruled out as the mode of action for the hydroxytriazolopyrimidine class of herbicides. Addnl., tobacco plants overexpressing lycopene β-cyclase showed tolerance to amitrole, which indicates that this is the main herbicidal mode of action for amitrole. Results from the metabolic fate study of selected hydroxytriazolopyrimidines suggested that the herbicidal activity displayed by these compounds is due to amitrole production, which was confirmed when tobacco plants overexpressing lycopene β-cyclase also showed tolerance towards two triazolopyrimidines from this study. © 2016 Society of Chem. Industry.

Pest Management Science published new progress about Amaranthus retroflexus. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, HPLC of Formula: 502546-41-0.

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

Wang, Shuai published the artcileDiscovery of [1,2,4]triazolo[1,5-a]pyrimidine derivatives as new bromodomain-containing protein 4 (BRD4) inhibitors, Computed Properties of 24415-66-5, the main research area is epigenetic regulation BRD4 inhibitor AML treatment PARP apoptosis.

Targeting bromodomain-containing protein 4 (BRD4) has been proved to be an effective strategy for cancer therapy. To date, numerous BRD4 inhibitors and degraders have been identified, some of which have advanced into clin. trials. In this work, a focused library of new [1,2,4]triazolo[1,5-a]pyrimidine derivatives were discovered to be able to inhibit BRD4. WS-722 inactivated BRD4 (BD1/BD2), BRD2 (BD1/BD2) and BRD3 (BD1/BD2) broadly with the IC50 values less than 5μmol/L. Besides, WS-722 inhibited growth of THP-1 cells with an IC50 value of 3.86μmol/L. Like (+)-JQ1, WS-722 inhibited BRD4 in a reversible manner and enhanced protein stability. Docking studies showed that WS-722 occupied the central acetyl-lysine (Kac) binding cavity and formed a hydrogen bond with Asn140. In THP-1 cells, WS-722 showed target engagement to BRD4. Cellular effects of WS-722 on THP-1 cells were also examined, showing that WS-722 could block c-MYC expression, induce G0/G1 phase arrest and p21 up-regulation, and promote differentiation of THP-1 cells. BRD4 inhibition by WS-722 resulted in cell apoptosis and up-regulated expression of cleaved caspased-3/7 and PARP in THP-1 cell lines. The [1,2,4]triazolo[1,5-a]pyrimidine is a new template for the development of new BRD4 inhibitors.

Chinese Chemical Letters published new progress about Acute myeloid leukemia. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Computed Properties of 24415-66-5.

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

Engers, Darren W. published the artcileDiscovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability, Computed Properties of 108281-78-3, the main research area is preparation dialkylindazolyl pyrazolopyridin amine derivative Parkinson’s; CYP induction; Parkinson’s disease; Positive allosteric modulator; Structure-activity relationship; mGlu4 PAM.

Previous reports from our laboratory disclosed the structure and activity of a novel 1H-pyrazolo[4,3-b]pyridine-3-amine scaffold (VU8506) which showed excellent potency, selectivity and in vivo efficacy in preclin. rodent models of Parkinson’s disease. Unfortunately, this compound suffered from significant CYP1A2 induction as measured through upstream AhR activation (125-fold) and thus was precluded from further advancement in chronic studies. Herein, we report a new scaffold developed recently which was systematically studied in order to mitigate the CYP1A2 liabilities presented in the earlier scaffolds. We have identified a novel structure that maintains the potency and selectivity of other mGlu4 PAMs, leading to 9i (hmGlu4 EC50 = 43 nM; AhR activation = 2.3-fold).

Bioorganic & Medicinal Chemistry Letters published new progress about Antiparkinsonian agents. 108281-78-3 belongs to class triazoles, name is 6-Bromo-3-methyl-[1,2,4]triazolo[4,3-a]pyridine, and the molecular formula is C7H6BrN3, Computed Properties of 108281-78-3.

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