Category: 5451-40-1

Formula: C5H2Cl2N4. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Discovery of MK-4688: an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction. Author is Reutershan, Michael H.; Machacek, Michelle R.; Altman, Michael D.; Bogen, Stephane; Cai, Mingmei; Cammarano, Carolyn; Chen, Dapeng; Christopher, Matthew; Cryan, John; Daublain, Pierre; Fradera, Xavier; Geda, Prasanthi; Goldenblatt, Peter; Hill, Armetta D.; Kemper, Raymond A.; Kutilek, Victoria; Li, Chaomin; Martinez, Michelle; McCoy, Mark; Nair, Latha; Pan, Weidong; Thompson, Christopher F.; Scapin, Giovanna; Shizuka, Manami; Spatz, Marianne L.; Steinhuebel, Dietrich; Sun, Binyuan; Voss, Matthew E.; Wang, Xiao; Yang, Liping; Yeh, Tammie C.; Dussault, Isabelle; Marshall, C. Gary; Trotter, B. Wesley.

Identification of low-dose, low-mol.-weight, drug-like inhibitors of protein-protein interactions (PPIs) is a challenging area of research. Despite the challenges, the therapeutic potential of PPI inhibition has driven significant efforts toward this goal. Adding to recent success in this area, we describe herein our efforts to optimize a novel purine carboxylic acid-derived inhibitor of the HDM2-p53 PPI into a series of low-projected dose inhibitors with overall favorable pharmacokinetic and phys. properties. Ultimately, a strategy focused on leveraging known binding hot spots coupled with biostructural information to guide the design of conformationally constrained analogs and a focus on efficiency metrics led to the discovery of MK-4688 (compound 56), a highly potent, selective, and low-mol.-weight inhibitor suitable for clin. investigation.

As far as I know, this compound(5451-40-1)Formula: C5H2Cl2N4 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

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, Catalysts called Synthesis of ribavirin, tecadenoson, and cladribine by enzymatic transglycosylation, Author is Rabuffetti, Marco; Bavaro, Teodora; Semproli, Riccardo; Cattaneo, Giulia; Massone, Michela; Morelli, Carlo F.; Speranza, Giovanna; Ubiali, Daniela, which mentions a compound: 5451-40-1, SMILESS is C2=NC1=C(C(=NC(=N1)Cl)Cl)[NH]2, Molecular C5H2Cl2N4, Related Products of 5451-40-1.

Despite the impressive progress in nucleoside chem. to date, the synthesis of nucleoside analogs is still a challenge. Chemoenzymic synthesis has been proven to overcome most of the constraints of conventional nucleoside chem. A purine nucleoside phosphorylase from Aeromonas hydrophila (AhPNP) has been used herein to catalyze the synthesis of ribavirin, tecadenoson, and cladribine, by a “”one-pot, one-enzyme”” transglycosylation, which is the transfer of the carbohydrate moiety from a nucleoside donor to a heterocyclic base. As the sugar donor, 7-methylguanosine iodide and its 2′-deoxy counterpart were synthesized and incubated either with the “”purine-like”” base or the modified purine of the three selected APIs. Good conversions (49-67%) were achieved in all cases under screening conditions. Following this synthetic scheme, 7-methylguanine arabinoside iodide was also prepared with the purpose to synthesize the antiviral vidarabine by a novel approach. However, in this case, neither the phosphorolysis of the sugar donor, nor the transglycosylation reaction were observed This study was enlarged to two other ribonucleosides structurally related to ribavirin and tecadenoson, namely, acadesine, or AICAR, and 2-chloro-N6-cyclopentyladenosine, or CCPA. Only the formation of CCPA was observed (52%). This study paves the way for the development of a new synthesis of the target APIs at a preparative scale. Furthermore, the screening herein reported contributes to the collection of new data about the specific substrate requirements of AhPNP.

As far as I know, this compound(5451-40-1)Related Products of 5451-40-1 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

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 9-Sulfonyl-9(H)-Purine Derivatives Inhibit HCV Replication Via their Degradation Species, published in 2021-04-30, which mentions a compound: 5451-40-1, mainly applied to sulfonylpurine degradation species hepatitis C virus inhibitor, Application In Synthesis of 2,6-Dichloropurine.

Cell-based screening of a privileged small mol. library led to the discovery of 9-sulfonyl-9(H)-purine as new scaffold for hepatitis C virus (HCV) inhibitors. Structure-activity relationship study with respect to the 2-, 6- and 9-positions in the purine core resulted in the identification of several active compounds with moderate potency against the HCV genotype 1b. Subsequent stability studies demonstrated that HCV inhibitors of this type were unstable in Dulbecco’s modified eagle medium (DMEM) and plasma, as well as glutathione-containing water, and their instability was closely related to their HCV inhibitory activity. A preliminary study of the mechanism of action showed that the sulfonamide bond at the 9-position of purine would be the primary degradation site and the resulting sulfonylation degradation species would mediate the anti-HCV activity of 9-sulfonyl-9(H)-purines. Results of this study demonstrated that 9-sulfonyl-9(H)-purine is an unstable scaffold for HCV inhibitors and further detailed anal. of the degradation species is needed to determine the main active components and direct target for this type of mols.

This literature about this compound(5451-40-1)Application In Synthesis of 2,6-Dichloropurinehas given us a lot of inspiration, and I hope that the research on this compound(2,6-Dichloropurine) can be further advanced. Maybe we can get more compounds in a similar way.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Formula: C5H2Cl2N4. 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: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about NMR studies of new heterocycles tethered to purine moieties with anticancer activity. Author is Fernandez-Saez, Nerea; Campos, Joaquin M.; Camacho, Maria Encarnacion; Carrion, Maria Dora.

The synthesis and biol. evaluation of a novel family of purine derivatives linked to six-membered heterocyclic moieties, which were designed and evaluated as anticancer agents, are described. The structures of these new compounds have been determined by 1H and 13C NMR and mass spectrometry. Some of them have been studied more in detail in order to corroborate their skeleton by using two-dimensional techniques.

In addition to the literature in the link below, there is a lot of literature about this compound(2,6-Dichloropurine)Formula: C5H2Cl2N4, illustrating the importance and wide applicability of this compound(5451-40-1).

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Application In Synthesis of 2,6-Dichloropurine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Study of the N7 Regioselective Glycosylation of 6-Chloropurine and 2,6-Dichloropurine with Tin and Titanium Tetrachloride.

6-Chloropurine and 2,6-dichloropurine were regioselectively glycosylated at position 7 to give the corresponding peracetylated N7-nucleosides, which can be suitable for other purine transformations. In this work, we study the distribution of N7/N9-isomers produced via the Vorbruggen method under different conditions, using an N-trimethylsilylated purine derivative and SnCl4 or TiCl4 as a catalyst. The main effort is devoted to reversing the disadvantageous predominant selectivity of most glycosylation reactions at the N9 position and thus to determining conditions that maximize the regioselectivity of glycosylation toward the desired N7-isomer.

In addition to the literature in the link below, there is a lot of literature about this compound(2,6-Dichloropurine)Application In Synthesis of 2,6-Dichloropurine, illustrating the importance and wide applicability of this compound(5451-40-1).

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Automated Nanomole-Scale Reaction Screening toward Benzoate Bioisosteres: A Photocatalyzed Approach to Highly Elaborated Bicyclo[1.1.1]Pentanes.Name: 2,6-Dichloropurine.

Through the application of high-throughput nanoscale optimization, a mild, photocatalyzed, Minisci-like protocol were developed to access highly functionalized 1,3-disubstituted bicyclopentanes. The benzoate-isosteric compounds were prepared using a readily available organic photocatalyst, mitigating the need for precious metals. The strategy described furnished products in synthetically useful yields and were demonstrated to be executable in parallel medicinal chem. format.

In addition to the literature in the link below, there is a lot of literature about this compound(2,6-Dichloropurine)Name: 2,6-Dichloropurine, illustrating the importance and wide applicability of this compound(5451-40-1).

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Csenki, Janos T.; Meszaros, Adam; Gonda, Zsombor; Novak, Zoltan published the article 《Stereoselective Direct N-Trifluoropropenylation of Heterocycles with a Hypervalent Iodonium Reagent》. Keywords: azole trifluoroisopropenyl iodonium trifluoromethanesulfonate diastereoselective trifluoropropenylation; trifluoropropenyl azole preparation; Michael addition; enamines; iodonium salt; nitrogen heterocycles; trifluoromethyl.They researched the compound: 2,6-Dichloropurine( cas:5451-40-1 ).Name: 2,6-Dichloropurine. 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:5451-40-1) here.

The availability and synthesis of fluorinated enamine derivatives such as N-(3,3,3-trifluoropropenyl)heterocycles are challenging, especially through direct functionalization of the heterocyclic scaffold. Herein, a stereoselective N-trifluoropropenylation method based on the use of a bench-stable trifluoropropenyl iodonium salt was described. This reagent enabled the straightforward trifluoropropenylation of various N-heterocycles under mild reaction conditions, providing trifluoromethyl enamine type moieties with high stereoselectivity and efficiency.

There are many compounds similar to this compound(5451-40-1)Name: 2,6-Dichloropurine. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Formula: C5H2Cl2N4. 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: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Neuroprotective potential of adenosine A1 receptor partial agonists in experimental models of cerebral ischemia. Author is Martire, Alberto; Lambertucci, Catia; Pepponi, Rita; Ferrante, Antonella; Benati, Nicholas; Buccioni, Michela; Dal Ben, Diego; Marucci, Gabriella; Klotz, Karl-Norbert; Volpini, Rosaria; Popoli, Patrizia.

Cerebral ischemia is the second most common cause of death and a major cause of disability worldwide. Available therapies are based only on anticoagulants or recombinant tissue plasminogen activator. Extracellular adenosine increases during ischemia and acts as a neuroprotective endogenous agent mainly by activating adenosine A1 receptors (A1Rs) which control calcium influx, glutamate release, membrane potential, and metabolism Accordingly, in many exptl. paradigms it has been already demonstrated that the stimulation of A1R with full agonists is able to reduce ischemia-related structural and functional brain damage; unfortunately, cardiovascular side effects and desensitization of A1R induced by these compounds have strongly limited their exploitation in stroke therapy so far. Among the newly emerging compounds, A1R partial agonists could be almost free of side effects and equally effective. Therefore, we decided to evaluate the neuroprotective potential of two A1R partial agonists, namely 2′-dCCPA and 3′-dCCPA, in in vitro and ex vivo exptl. models of cerebral ischemia. Within the exptl. paradigm of oxygen-glucose deprivation in vitro in human neuroblastoma (SH-SY5Y) cells both A1R partial agonists increased cell viability. Considering the high level of expression of A1Rs in the hippocampus and the susceptibility of CA1 region to hypoxia, we performed electrophysiol. experiments in this subfield. The application of 7 min of oxygen-glucose deprivation constantly produces an irreversible synaptic failure in all the C57Bl/6 mice hippocampal slices evaluated; both tested compounds allowed a significant recovery of synaptic transmission. These findings demonstrate that A1R and its partial agonists are still of interest for cerebral ischemia therapy. Open Science Badges : This article has received a badge for *Open Materials* because it provided all relevant information to reproduce the study in the manuscript. The complete Open Science Disclosure form for this article can be found at the end of the article. More information about the Open Practices badges can be found at https://cos.io/our-services/open-science-badges/.

There are many compounds similar to this compound(5451-40-1)Formula: C5H2Cl2N4. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Synthetic Route of C5H2Cl2N4. 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: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors. Author is Barbosa da Silva, Elany; Rocha, Debora A.; Fortes, Isadora S.; Yang, Wenqian; Monti, Ludovica; Siqueira-Neto, Jair L.; Caffrey, Conor R.; McKerrow, James; Andrade, Saulo F.; Ferreira, Rafaela S..

The cysteine proteases, cruzain and TbrCATL (rhodesain), are therapeutic targets for Chagas disease and Human African Trypanosomiasis, resp. Among the known inhibitors for these proteases, N4-benzyl-N2-phenylquinazoline-2,4-diamine (1a I [R1 = phenyl; R2 = benzyl] in this study), as a competitive cruzain inhibitor (Ki = 1.4μM) was described. The synthesis and biol. evaluation of 22 analogs I [R1 = Ph, 4-OH-Ph, 2-pyridyl; R2 = benzyl, Ph, 3-Cl-Ph, etc] of I [R1 = phenyl; R2 = benzyl], containing modifications in the quinazoline core, and in the substituents in positions 2 and 4 of this ring was described. The analogs I demonstrate low micromolar inhibition of the target proteases and cidal activity against Trypanosoma cruzi with up to two log selectivity indexes in counterscreens with myoblasts. Fourteen compounds were active against Trypanosoma brucei at low to mid micromolar concentrations During the optimization of I [R1 = phenyl; R2 = benzyl], structure-based design and prediction of physicochem. properties were employed to maintain potency against the enzymes while removing colloidal aggregator characteristics observed for some mols. in this series.

I hope my short article helps more people learn about this compound(2,6-Dichloropurine)Synthetic Route of C5H2Cl2N4. Apart from the compound(5451-40-1), you can read my other articles to know other related compounds.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Prevention and rescue of cardiac dysfunction by methanocarba adenosine monophosphonate derivatives, the main research direction is cardiac dysfunction methanocarba adenosine monophosphonate derivative; Adenine nucleoside phosphonate; Cardiac function; Heart failures; Purinergic receptors.Related Products of 5451-40-1.

Abstract: Accumulating evidence supports a therapeutic role of purinergic signaling in cardiac diseases. Previously, efficacy of systemically infused MRS2339, a charged methanocarba derivative of 2-Cl-adenosine monophosphate, was demonstrated in animal models of heart failure. We now test the hypothesis that an uncharged adenine nucleoside phosphonate, suitable as an oral agent with a hydrolysis-resistant phospho moiety, can prevent the development of cardiac dysfunction in a post-infarction ischemic or pressure overload-induced heart failure model in mice. The diester-masked uncharged phosphonate MRS2978 was efficacious in preventing cardiac dysfunction with improved LV fractional shortening when administered orally at the onset of ischemic or pressure overload-induced heart failure. MRS2925, the charged, unmasked MRS2978 analog, prevented heart dysfunction when infused s.c. but not by oral gavage. When administered orally or systemically, MRS2978 but not MRS2925 could also rescue established cardiac dysfunction in both ischemic and pressure overload heart failure models. The diester-masked phosphate MRS4074 was highly efficacious at preventing the development of dysfunction as well as in rescuing pressure overload-induced and ischemic heart failure. MRS2978 was orally bioavailable (57-75%) giving rise to MRS2925 as a minor metabolite in vivo, tested in rats. The data are consistent with a novel therapeutic role of adenine nucleoside phosphonates in systolic heart failure.

I hope my short article helps more people learn about this compound(2,6-Dichloropurine)Related Products of 5451-40-1. Apart from the compound(5451-40-1), you can read my other articles to know other related compounds.

Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem