Month: November 2022

On April 10, 2008, Elzein, Elfatih; Kalla, Rao V.; Li, Xiaofen; Perry, Thao; Gimbel, Art; Zeng, Dewan; Lustig, David; Leung, Kwan; Zablocki, Jeff published an article.COA of Formula: C9H7N3O2 The title of the article was Discovery of a Novel A2B Adenosine Receptor Antagonist as a Clinical Candidate for Chronic Inflammatory Airway Diseases. And the article contained the following:

Recently, the authors have reported a series of new 1,3-sym. (R1 = R3) substituted xanthines which have high affinity and selectivity for the human adenosine A2B receptors (hA2B-AdoR). Unfortunately, this class of compounds had poor pharmacokinetic properties. This prompted us to investigate the effect of differential alkyl substitution at the N-1 and N-3 positions (N1-R ≠ N3-R) on A2B-AdoR affinity and selectivity; the authors had the dual objectives of enhancing affinity and selectivity for the A2B-AdoR, as well as improving oral bioavailability. This effort has led to the discovery of compound (I), that displayed high affinity and selectivity for the hA2B-AdoR (Ki = 22 nM). In addition, compound I showed high functional potency in inhibiting the accumulation of cAMP induced by 5′-N-ethylcarboxamidoadenosine in HEK-A2B-AdoR and NIH3T3 cells with KB values of 6 and 2 nM, resp. In a single ascending-dose phase I clin. study, compound I had no serious adverse events and was well tolerated. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).COA of Formula: C9H7N3O2

The Article related to adenosine receptor antagonist preparation antiinflammatory inflammatory airway disease pharmacokinetics, Pharmacology: Structure-Activity and other aspects.COA of Formula: C9H7N3O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Kamal, Raj; Kumar, Vipan; Kumar, Ravinder; Bhardwaj, Jitender K.; Saraf, Priyanka; Kumari, Priya; Bhardwaj, Vikas published an article in 2017, the title of the article was Design, Synthesis, and Screening of Triazolopyrimidine-Pyrazole Hybrids as Potent Apoptotic Inducers.HPLC of Formula: 36640-53-6 And the article contains the following content:

An efficient synthesis of novel 3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-5,7-dimethyl-[1,2,4]triazolo[4,3-a]-pyrimidines was accomplished by the oxidation of pyrimidinylhydrazones by using organoiodine(III) reagent. All new triazolopyrimidine derivatives bearing the pyrazole scaffold were screened to evaluate them as a reproductive toxicant in the testicular germ cells of goat (Capra hircus). This study aimed at assessing the cytol. and biochem. changes in testicular germ cells after the exposure to triazolopyrimidines in a dose- and time-dependent manner. Histomorphol. anal., fluorescence assays, apoptosis quantification, and terminal deoxynucleotidyl transferase dUTP-mediated nick-end labeling (TUNEL) assays were performed to determine cytol. changes, whereas thiobarbituric acid-reactive substance (TBARS) and ferric reducing antioxidant power (FRAP) assays were carried out to measure the oxidative stress in triazolopyrimidines treated germ cells. The parallel use of these methods enabled us to determine the role of triazolopyrimidines in inducing apoptosis as a consequence of cytogenetic damage and oxidative stress generated in testicular germ cells of goat. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).HPLC of Formula: 36640-53-6

The Article related to screening triazolopyrimidine pyrazole apoptosis inducer, cytotoxic activity, pyrazole, synthesis, triazole, Pharmacology: Structure-Activity and other aspects.HPLC of Formula: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On May 14, 2015, Hatcher, John M.; Zhang, Jinwei; Choi, Hwan Geun; Ito, Genta; Alessi, Dario R.; Gray, Nathanael S. published an article.Synthetic Route of 98138-75-1 The title of the article was Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. And the article contained the following:

Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson’s disease (PD) patients and may represent an attractive therapeutic target. Here the authors report JH-II-127 I, as a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. Compound I substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 μM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Synthetic Route of 98138-75-1

The Article related to pyrrolopyrimidine brain penetrant lrrk inhibitor, lrrk2, parkinson’s disease, leucine-rich repeat kinase 2, pharmacokinetics, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 98138-75-1

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 3, 2018, Naim, Mohd. Javed; Alam, Ozair; Alam, Jahangir Md.; Shaquiquzzaman, Mohammad; Alam, Mumtaz Md.; Naidu, Vegi Ganga Modi published an article.Recommanded Product: 36640-53-6 The title of the article was Synthesis, docking, in vitro and in vivo antidiabetic activity of pyrazole-based 2,4-thiazolidinedione derivatives as PPAR-γ modulators. And the article contained the following:

The design, synthesis, structure-activity relationship, and biol. activity of 2,4-thiazolidinedione derivatives as peroxisome proliferator-activated receptor-γ (PPAR-γ) modulators for antidiabetic activity are reported. Fifteen 2,4-thiazolidinedione derivatives clubbed with pyrazole moiety were docked into the ligand binding domain of PPAR-γ by the Glide XP module of Schrodinger. Eight derivatives (5a (5-((3-(3,4-dichlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thiazolidine-2,4-dione), 5b (5-((1-phenyl-3-(thien-2-yl)-1H-pyrazol-4-yl)methylene)thiazolidine-2,4-dione), 5d, 5f, 5i, 5l, 5n, 5o) having Glide XP scores > -8 as compared to the standard drug, rosiglitazone (Glide XP score = -9.165), showed almost similar interaction with the amino acids such as HIS 449, TYR 473, TYR 327, HIS 323, and SER 289 in the mol. docking studies. These eight derivatives were further screened for PPAR-γ transactivation and in vivo blood glucose lowering activity in the streptozotocin-induced diabetic rat model. Compounds 5o, 5n, 5a, 5i, and 5b showed 52.06, 51.30, 48.65, 43.13, and 40.36% PPAR-γ transactivation as compared to the reference drugs rosiglitazone and pioglitazone with 85.30 and 65.22% transactivation, resp. The data anal. showed significant blood glucose lowering effects (hypoglycemia) of compounds 5o, 5n, and 5a (140.1±4.36, 141.4±6.15, and 150.7±4.15, resp.), along with reference drugs pioglitazone (135.2±4.91) and rosiglitazone (141.1±5.88) as compared to the diabetic control. Furthermore, the most potent compound 5o also elevated the PPAR-γ gene expression by 2.35-fold as compared to rosiglitazone (1.27-fold) and pioglitazone (1.6-fold). It also significantly lowered the AST, ALT, and ALP levels and caused no damage to the liver. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Recommanded Product: 36640-53-6

The Article related to pyrazole thiazolidinedione preparation ppar gamma modulator docking antidiabetic diabetes, ppar-γ, diabetes, molecular docking, thiazolidinedione, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On August 31, 2017, Naim, Mohd. Javed; Alam, Jahangir Md.; Nawaz, Farah; Naidu, V. G. M.; Aaghaz, Shams; Sahu, Meeta; Siddiqui, Nadeem; Alam, Ozair published an article.SDS of cas: 36640-53-6 The title of the article was Synthesis, molecular docking and anti-diabetic evaluation of 2,4-thiazolidinedione based amide derivatives. And the article contained the following:

A series of thiazolidinedione based amide derivatives were designed, synthesized and docked against the PPARγ receptor target. 11 Compounds from the series with good glide scores were selected for in vivo antidiabetic study based on streptozotocin induced diabetic rat model. It was observed that 4 compounds (I, II, III & IV) showed significantly good antidiabetic activity in comparison to rosiglitazone and pioglitazone as reference drugs. Compound I appeared as the most potent derivative in lowering blood glucose level and showed excellent interaction with SER 342, ILE 281, pi-pi interaction with ARG 288 and halogen bond interaction with LYS 367. Further, PPARγ transactivation and gene expression studies of compound I were carried out to investigate the possible mechanism of action through PPARγ modulation. Compound I exhibited 53.65% transactivation and elevated PPARγ gene expression by 2.1 folds. The biochem. parameters (AST, ALT and ALP levels) were found within the range with no noteworthy damage to liver. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).SDS of cas: 36640-53-6

The Article related to thiazolidinedione amide derivative synthesis sar antidiabetic pharmacokinetics toxicity, antidiabetic, molecular docking, pparγ, thiazolidinedione, Pharmacology: Structure-Activity and other aspects.SDS of cas: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 21, 2011, Bretschneider, Thomas; Fuesslein, Martin; Koehler, Adeline; Muehlthau, Friedrich August; Franken, Eva-Maria; Voerst, Arnd published a patent.Computed Properties of 1014631-89-0 The title of the patent was Synthesis of 1-(pyrid-3-yl)-pyrazoles and 1-(pyramid-5-yl)-pyrazoles and use as insecticide and/or acaricide.. And the patent contained the following:

The invention relates to the use of partially known heterocyclic compounds for combating animal pests, including arthropods and in particular insects, and further relates to novel heterocyclic compounds and to methods for synthesis thereof. Also disclosed are the rates of effectiveness of selected compounds, relating to the invention, in killing particular insect and acarid pests on sample crops. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Computed Properties of 1014631-89-0

The Article related to pyridyl pyramidyl pyrazole insecticide acaricide crop protection, Agrochemical Bioregulators: Invertebrate and other aspects.Computed Properties of 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Verma, Anil; Kumar, Vinod; Khare, Rajshree; Singh, Joginder published an article in 2019, the title of the article was Synthesis of some hippuric acid substrate linked novel pyrazoles as antimicrobial agents.Category: pyrazoles-derivatives And the article contains the following content:

Escalating resistance of microorganisms to the currently accessible antimicrobial drugs has forced to synthesize some novel biol. active compounds as efficient alternates via economical substrates. Hence, hippuric acid was used as one of the starting materials to synthesize pyrazole derivatives All the synthesized compounds were characterized by IR, NMR (1H & 13C) and mass spectral data. The antimicrobial potential of synthesized compounds has been explored against four bacterial and two fungal strains. Among the 12 compounds, 3 compounds 8j, 8k and 8l were found to exhibit prominent antimicrobial potential as compared with the standards ciprofloxacin and amphotericin-B. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Category: pyrazoles-derivatives

The Article related to hippuric acid antimicrobial pyrazoles, Placeholder for records without volume info and other aspects.Category: pyrazoles-derivatives

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Sirbu, Doina; Diharce, Julien; Martinic, Ivana; Chopin, Nicolas; Eliseeva, Svetlana V.; Guillaumet, Gerald; Petoud, Stephane; Bonnet, Pascal; Suzenet, Franck published an article in 2019, the title of the article was An original class of small sized molecules as versatile fluorescent probes for cellular imaging.Category: pyrazoles-derivatives And the article contains the following content:

An unusual class, compact in size, of fluorescent probes based on pyridazino-1,3a,6a-triazapentalene scaffolds exhibits promising fluorescent properties (quantum yield values up to 73%, large Stokes shifts, emission wavelengths located in the green-yellow range, excellent solubility) with good photostability suitable for optical imaging applications. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Category: pyrazoles-derivatives

The Article related to fluorescent probe cell imaging, Biochemical Methods: Spectral and Related Methods and other aspects.Category: pyrazoles-derivatives

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 13, 2013, Houze, Jonathan B.; Dransfield, Paul; Pattaropong, Vatee; Du, Xiaohui; Fu, Zice; Lai, Sujen; Park, Jaehyeon; Jiao, Xianyun; Kohn, Todd J.; Aicher, Thomas Daniel; Boyd, Steven Armen; Bencsik, Josef; Condroski, Kevin Ronald; Hinklin, Ronald Jay; Kraser, Christopher F.; Pratt, Scott; Singh, Ajay; Wenglowsky, Steven Mark; Boys, Mark Laurence; Chicarelli, Mark Joseph; Mohr, Peter J.; Cardozo, Mario G. published a patent.Reference of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol The title of the patent was Urea compounds as GKa activators and their preparation. And the patent contained the following:

The invention relates to urea compounds of formula I, to pharmaceutical compositions comprising the compounds, to a process for making the compounds and to the use of the compounds in the treatment of diseases and disorders that would benefit from activation of glucokinase. Compounds of formula I wherein R1 is H, alkyl, alkenyl, haloalkyl, etc.; R2 is H, alkyl and halo; R3 is H, halo, alkoxycarbonyl, etc.; G is C and N; P is H and LR6; L is O, S, CH2 and CH2O; R6 is aryl aralkyl, heterocyclyl, etc.; and with proviso; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their glucokinase activation activity (data given). The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Reference of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

The Article related to pyridinyl urea preparation glucokinase activator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Reference of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Komatsuda, Masaaki; Suto, Ayane; Kondo, Hiroki Jr; Takada, Hiroyuki; Kato, Kenta; Saito, Bunnai; Yamaguchi, Junichiro published an article in 2022, the title of the article was Ring-opening fluorination of bicyclic azaarenes.HPLC of Formula: 143803-93-4 And the article contains the following content:

Authors have discovered a ring-opening fluorination of bicyclic azaarenes. Upon treatment of bicyclic azaarenes such as pyrazolo[1,5-a]pyridines with electrophilic fluorinating agents, fluorination of the aromatic ring is followed by a ring-opening reaction. Although this overall transformation can be classified as an electrophilic fluorination of an aromatic ring, it is a novel type of fluorination that results in construction of tertiary carbon-fluorine bonds. The present protocol can be applied to a range of bicyclic azaarenes, tolerating azines and a variety of functional groups. Addnl., mechanistic studies and enantioselective fluorination have been examined The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).HPLC of Formula: 143803-93-4

The Article related to pyrazolopyridine bicyclic azaarene ring opening fluorination, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 143803-93-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics