Category: imidazoles-derivatives

On April 20, 2022, Bai, Jie; Wang, Jie; Feng, Yecheng; Yao, Yongfang; Zhao, Xubo published an article.Electric Literature of 5036-48-6 The title of the article was Stability-tunable core-crosslinked polymeric micelles based on an imidazole-bearing block polymer for pH-responsive drug delivery. And the article contained the following:

Polymeric micelles from block copolymers have gained increasing attention in cancer drug delivery. However, the fabrication of polymeric micelles that are stable in biol. fluids and unstable at tumor sites remains a principal challenge. To achieve the tunable stability for the polymeric micelles, Zn coordination-induced core-crosslinked polymeric micelles have been proposed and confirmed. Herein, a block copolymer bearing imidazole pendants is synthesized which is capable of self-assembling into polymeric micelles in water. After core-crosslinking, it can be found that the critical micelle concentration (CMC) of the core-crosslinked polymeric micelles is significantly lower than that of non-crosslinked polymeric micelles. Particularly, the drug-loaded core-crosslinked polymeric micelles are fragile and easily affected by the slightly acidic environments, which makes it possible to turn the polymeric micelles back to hydrophilic polymers and therefore disassemble micelles to unload cargoes. The drug-loaded core-crosslinked polymeric micelles display adequate toxicity as a result of their low IC50 value of 3.713 �0.166 渭g/mL. Collectively, Zn coordination-induced core-crosslinked polymeric micelles offer a design idea for practicable drug delivery system in cancer therapy. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Electric Literature of 5036-48-6

The Article related to imidazole block polymer micelle drug delivery systems, Placeholder for records without volume info and other aspects.Electric Literature of 5036-48-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Woodcock, Clayton B.; Horton, John R.; Zhou, Jujun; Bedford, Mark T.; Blumenthal, Robert M.; Zhang, Xing; Cheng, Xiaodong published an article in 2020, the title of the article was Biochemical and structural basis for YTH domain of human YTHDC1 binding to methylated adenine in DNA.Name: N-Methyl-7H-purin-6-amine And the article contains the following content:

The recently characterized mammalian writer (methyltransferase) and eraser (demethylase) of the DNA N6-methyladenine (N6mA) Me mark act on single-stranded (ss) and transiently-unpaired DNA. As YTH domain-containing proteins bind N6mA-containing RNA in mammalian cells, we investigated whether mammalian YTH domains are also Me mark readers of N6mA DNA. Here, we show that the YTH domain of YTHDC1 (known to localize in the nucleus) binds ssDNA containing N6mA, with a 10 nM dissociation constant This binding is stronger by a factor of 5 than in an RNA context, tested under the same conditions. However, the YTH domains of YTHDF2 and YTHDF1 (predominantly cytoplasmic) exhibited the opposite effect with �.5-2x stronger binding to ssRNA containing N6mA than to the corresponding DNA. We determined two structures of the YTH domain of YTHDC1 in complex with N6mA-containing ssDNA, which illustrated that YTHDC1 binds the methylated adenine in a single-stranded region flanked by duplexed DNA. We discuss the hypothesis that the writer-reader-eraser of N6mA-containining ssDNA is associated with maintaining genome stability. Structural comparison of YTH and SRA domains (the latter a DNA 5-methylcytosine reader) revealed them to be diverse members of a larger family of DNA/RNA modification readers, apparently having originated from bacterial modification-dependent restriction enzymes. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Name: N-Methyl-7H-purin-6-amine

The Article related to ythdc1 dna methylated adenine biochem structure, Placeholder for records without volume info and other aspects.Name: N-Methyl-7H-purin-6-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Liu, Dan; Xue, Aiqi; Wang, Haifeng; Luan, Tian; Li, Xue published an article in 2022, the title of the article was Design, synthesis and biological evaluation of 4-amino-quinolines as antitumor agents.Recommanded Product: N-(3-Aminopropyl)-imidazole And the article contains the following content:

Fifteen novel 4-amino-quinolines (I1-III3) as antitumor agent were synthesized by p-nitroaniline and ethoxymethylene malonic ester (EMME) via condensation, cyclization, hydrolysis, decarboxylation, chlorination, nucleophilic substitution, reduction and amidation. The antitumor activity of compounds I1-III3 was evaluated on SGC-7901, BEL-7402 and A549 cancer cell lines. In vitro bioassay indicated that some compounds showed different degree activity against all tested cancer cell lines. Compound I1, I4 and II2 exhibited high effects against A549 cell lines (IC50 = 1.34渭M, 1.36渭M and 3.00渭M, resp.). In addition, the result of mol. docking showed that compound I1, I4 and II2 could dock into the pocket of EGFR. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Recommanded Product: N-(3-Aminopropyl)-imidazole

The Article related to amino quinoline antitumor agent egfr receptor, Placeholder for records without volume info and other aspects.Recommanded Product: N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Mothukuri, Ganesh K.; Kale, Sangram S.; Stenbratt, Carl L.; Zorzi, Alessandro; Vesin, Jonathan; Bortoli Chapalay, Julien; Deyle, Kaycie; Turcatti, Gerardo; Cendron, Laura; Angelini, Alessandro; Heinis, Christian published an article in 2020, the title of the article was Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries.Category: imidazoles-derivatives And the article contains the following content:

Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three building blocks are coupled sequentially in efficient alkylation reactions that eliminate the need for product purification We demonstrate the power of the approach by combinatorially reacting 15 bromoacetamide-activated tripeptides, 42 amines, and 6 bis-electrophile cyclization linkers to generate a 3780-compound library with minimal effort. Screening against thrombin yielded a potent and selective inhibitor (Ki = 4.2 �0.8 nM) that efficiently blocked blood coagulation in human plasma. Structure-activity relationship and X-ray crystallog. anal. revealed that two of the three building blocks acted synergistically and underscored the importance of combinatorial screening in macrocycle development. The three-component library synthesis approach is general and offers a promising avenue to generate macrocycle ligands to other targets. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Category: imidazoles-derivatives

The Article related to plasma thrombin prothrombin thromboplastin x, Placeholder for records without volume info and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Jenjaroenpun, Piroon; Wongsurawat, Thidathip; Wadley, Taylor D.; Wassenaar, Trudy M.; Liu, Jun; Dai, Qing; Wanchai, Visanu; Akel, Nisreen S.; Jamshidi-Parsian, Azemat; Franco, Aime T.; Boysen, Gunnar; Jennings, Michael L.; Ussery, David W.; He, Chuan; Nookaew, Intawat published an article in 2021, the title of the article was Decoding the epitranscriptional landscape from native RNA sequences.COA of Formula: C6H7N5 And the article contains the following content:

Traditional epitranscriptomics relies on capturing a single RNA modification by antibody or chem. treatment, combined with short-read sequencing to identify its transcriptomic location. This approach is labor-intensive and may introduce exptl. artifacts. Direct sequencing of native RNA using Oxford Nanopore Technologies (ONT) can allow for directly detecting the RNA base modifications, although these modifications might appear as sequencing errors. The percent Error of Specific Bases (%ESB) was higher for native RNA than unmodified RNA, which enabled the detection of ribonucleotide modification sites. Based on the %ESB differences, we developed a bioinformatic tool, epitranscriptional landscape inferring from glitches of ONT signals (ELIGOS), that is based on various types of synthetic modified RNA and applied to rRNA and mRNA. ELIGOS is able to accurately predict known classes of RNA methylation sites (AUC > 0.93) in rRNAs from Escherichia coli, yeast, and human cells, using either unmodified in vitro transcription RNA or a background error model, which mimics the systematic error of direct RNA sequencing as the reference The well-known DRACH/RRACH motif was localized and identified, consistent with previous studies, using differential anal. of ELIGOS to study the impact of RNA m6A methyltransferase by comparing wild type and knockouts in yeast and mouse cells. Lastly, the DRACH motif could also be identified in the mRNA of three human cell lines. The mRNA modification identified by ELIGOS is at the level of individual base resolution In summary, we have developed a bioinformatic software package to uncover native RNA modifications. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).COA of Formula: C6H7N5

The Article related to decoding epitranscriptional rna sequence, Placeholder for records without volume info and other aspects.COA of Formula: C6H7N5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On December 31, 2000, Petronzelli, Fiorella; Riccio, Antonio; Markham, George D.; Seeholzer, Steven H.; Genuardi, Maurizio; Karbowski, Mariola; Yeung, Anthony T.; Matsumoto, Yoshihiro; Bellacosa, Alfonso published an article.Reference of Imidazo[1,2-c]pyrimidin-5(6H)-one The title of the article was Investigation of the substrate spectrum of the human mismatch-specific DNA N-glycosylase MED1 (MBD4): fundamental role of the catalytic domain. And the article contained the following:

The human DNA repair protein MED1 (also known as MBD4) was isolated as an interactor of the mismatch repair protein MLH1 in a yeast two-hybrid screening. MED1 has a tripartite structure with an N-terminal 5-methylcytosine binding domain (MBD), a central region, and a C-terminal catalytic domain with homol. to bacterial DNA damage-specific glycosylases/lyases. Indeed, MED1 acts as a mismatch-specific DNA N-glycosylase active on thymine, uracil, and 5-fluorouracil paired with guanine. The glycosylase activity of MED1 preferentially targets G:T mismatches in the context of CpG sites; this indicates that MED1 is involved in the repair of deaminated 5-methylcytosine. Interestingly, frameshift mutations of the MED1 gene have been reported in human colorectal, endometrial, and pancreatic cancers. For its putative role in maintaining genomic fidelity at CpG sites, it is important to characterize the biochem. properties and the substrate spectrum of MED1. Here we show that MED1 works under a wide range of temperature and pH, and has a limited optimum range of ionic strength. MED1 has a weak glycosylase activity on the mutagenic adduct 3,N4-ethenocytosine, a metabolite of vinyl chloride and Et carbamate. The differences in glycosylase activity on G:U and G:T substrates are not related to differences in substrate binding and likely result from intrinsic differences in the chem. step. Finally, the isolated catalytic domain of MED1 retains the preference for G:T and G:U substrates in the context of methylated or unmethylated CpG sites. This suggests that the catalytic domain is fundamental, and the 5-methylcytosine binding domain dispensable, in determining the substrate spectrum of MED1. The experimental process involved the reaction of Imidazo[1,2-c]pyrimidin-5(6H)-one(cas: 55662-66-3).Reference of Imidazo[1,2-c]pyrimidin-5(6H)-one

The Article related to dna glycosylase med1 catalytic domain substrate specificity, mbd4 dna glycosylase catalytic domain substrate specificity, Enzymes: Structure-Conformation-Active Site and other aspects.Reference of Imidazo[1,2-c]pyrimidin-5(6H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Tang, Shengzhuang; Chen, Jesse; Cannon, Jayme; Cao, Zhengyi; Baker, James R. Jr; Wang, Su He published an article in 2021, the title of the article was Dendrimer-based posaconazole nanoplatform for antifungal therapy.Safety of N-(3-Aminopropyl)-imidazole And the article contains the following content:

We examined formulating a new antifungal agent, posaconazole (POS) and its derivatives, with different mol. vehicles. Several combinations of drug and carrier mols. were synthesized, and their antifungal activities were evaluated against Aspergillus fumigatus. Posaconazole and four of its derivatives were conjugated to either generation 5 (G5) dendrimers or partially modified G5 dendrimers. The in vitro antifungal activities of these compounds suggest that conjugates with specific chem. linkages showed better fungistatic activity than direct conjugates to POS. In particular, a polyethylene glycol (PEG)-imidazole modified G5 dendrimer demonstrated improved antifungal efficacy relative to the parent G5 mol. Further studies were then conducted with POS derived mols. coupled to PEG-imidazole modified G5 dendrimers to achieve a highly soluble and active conjugate of POS. This conjugated macromol. averaged 23 POS mols. per G5 and had a high solubility with 50 mg/mL, which improved the molar solubility of POS from less than 0.03 mg/mL to as high as 16 mg/mL in water. The primary release profile of the drug in human plasma was extended to over 72 h, which is reflected in the in vitro inhibition of A. fumigatus growth of over 96 h. These POS-polymer conjugates appear to be novel and efficient antifungal agents. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Safety of N-(3-Aminopropyl)-imidazole

The Article related to posaconazole nanoplatform dendrimer antifungal therapy, demethylase inhibitor, antifungal drug, biocompatible, polymer, Placeholder for records without volume info and other aspects.Safety of N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On December 31, 2022, Guan, Qian; Lin, Huiran; Miao, Lei; Guo, Huiqin; Chen, Yongping; Zhuo, Zhenjian; He, Jing published an article.Name: N-Methyl-7H-purin-6-amine The title of the article was Functions, mechanisms, and therapeutic implications of METTL14 in human cancer. And the article contained the following:

A review. RNA modification plays a crucial role in many biol. functions, and its abnormal regulation is associated with the progression of cancer. Among them, N6-methyladenine (m6A) is the most abundant RNA modification. Methyltransferase-like 14 (METTL14) is the central component of the m6A methylated transferase complex, which is involved in the dynamic reversible process of m6A modification. METTL14 acts as both an oncogene and tumor suppressor gene to regulate the occurrence and development of various cancers. The abnormal m6A level induced by METTL14 is related to tumorigenesis, proliferation, metastasis, and invasion. To date, the mol. mechanism of METTL14 in various malignant tumors has not been fully studied. In this paper, we systematically summarize the latest research progress on METTL14 as a new biomarker for cancer diagnosis and its biol. function in human tumors and discuss its potential clin. application. This study aims to provide new ideas for targeted therapy and improved prognoses in cancer. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Name: N-Methyl-7H-purin-6-amine

The Article related to review cancer mettl14 rna modification biomarkers, cancer, drug discovery, mettl14, rna modification, m6a, Placeholder for records without volume info and other aspects.Name: N-Methyl-7H-purin-6-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Zhang, Geping; Lu, Dandan; Yin, Keyang; Godbert, Nicolas; Dong, Renhao; Li, Hongguang; Hao, Jingcheng published an article in 2022, the title of the article was Alkylated, naphthalimide-containing ionic compounds with rich thermotropic behaviour and nonlinear optical response.Recommanded Product: 5036-48-6 And the article contains the following content:

Chem. functionalization of �conjugated units plays a key role in fine tuning their supramol. organizations and functions. Herein, five 1,8-naphthalimide derivatives were prepared where the naphthalimide moiety was attached to the imidazolium ring through a Pr linker. On the other side, the imidazolium ring was modified with either a branched aliphatic chain of 2-ethyl-hexyl (C2C6, 1), 2-hexyl-decyl (C6C10, 2) and 2-decyl-tetradecyl (C10C14, 3), or a linear aliphatic chain of octyl (C8, 1� and hexadecyl (C16, 2�. Temperature-dependent structural evolution of these alkylated, naphthalimide-modified imidazolium bromides (abbreviated to a-NaphImiBrs hereafter) were investigated in detail by differential scanning calorimetry and small-angle X-ray scattering measurements as well as polarized optical microscopy observations. The compound with the shortest branched aliphatic chain (1) self-organized into a columnar oblique (Colo) phase at room temperature, which changed to a columnar rectangular (Colr) phase upon heating. In comparison, its counterpart with a linear aliphatic chain of the same carbon number (1� formed a crystal at room temperature, which shifted to a Colo phase at elevated temperature The compound with a medium branched aliphatic chain (2) showed a columnar hexagonal (Colh) organization at room temperature, which changed to a smectic (Sm) phase upon heating. Compounds with longer aliphatic chains (2� 3), regardless of whether branched or linear, only exhibit the Sm phase. Films of a-NaphImiBrs formed at room temperature were subjected to evaluations for their nonlinear optical (NLO) responses where reverse saturated absorption was observed in all the cases. It was found that 2 showed the best NLO response with a third order nonlinear absorption coefficient of up to 0.49 cm W-1. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Recommanded Product: 5036-48-6

The Article related to alkylated naphthalimide containing ionic compound rich thermotropic behavior, nonlinear optical response, Placeholder for records without volume info and other aspects.Recommanded Product: 5036-48-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On December 1, 1999, Barrett, Tracey E.; Scharer, Orlando D.; Savva, Renos; Brown, Tom; Jiricny, Josef; Verdine, Gregory L.; Pearl, Laurence H. published an article.Name: Imidazo[1,2-c]pyrimidin-5(6H)-one The title of the article was Crystal structure of a thwarted mismatch glycosylase DNA repair complex. And the article contained the following:

The bacterial mismatch-specific uracil-DNA glycosylase (MUG) and eukaryotic thymine-DNA glycosylase (TDG) enzymes form a homologous family of DNA glycosylases that initiate base-excision repair of G:U/T mismatches. Despite low sequence homol., the MUG/TDG enzymes are structurally related to the uracil-DNA glycosylase enzymes, but have a very different mechanism for substrate recognition. We have now determined the crystal structure of the Escherichia coli MUG enzyme complexed with an oligonucleotide containing a non-hydrolysable deoxyuridine analog mismatched with guanine, providing the first structure of an intact substrate-nucleotide productively bound to a hydrolytic DNA glycosylase. The structure of this complex explains the preference for G:U over G:T mispairs, and reveals an essentially non-specific pyrimidine-binding pocket that allows MUG/TDG enzymes to excise the alkylated base, 3,N4-ethenocytosine. Together with structures for the free enzyme and for an abasic-DNA product complex, the MUG-substrate analog complex reveals the conformational changes accompanying the catalytic cycle of substrate binding, base excision and product release. The experimental process involved the reaction of Imidazo[1,2-c]pyrimidin-5(6H)-one(cas: 55662-66-3).Name: Imidazo[1,2-c]pyrimidin-5(6H)-one

The Article related to crystal structure uracil dna glycosylase complex, dna uracil glycosylase conformation repair mechanism, Enzymes: Structure-Conformation-Active Site and other aspects.Name: Imidazo[1,2-c]pyrimidin-5(6H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem