Category: 15813-09-9

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH) was written by Lucas-Hourani, Marianne;Munier-Lehmann, Helene;El Mazouni, Farah;Malmquist, Nicholas A.;Harpon, Jane;Coutant, Eloi P.;Guillou, Sandrine;Helynck, Olivier;Noel, Anne;Scherf, Artur;Phillips, Margaret A.;Tangy, Frederic;Vidalain, Pierre-Olivier;Janin, Yves L.. And the article was included in Journal of Medicinal Chemistry in 2015.Recommanded Product: 4,5-Diiodo-1H-imidazole This article mentions the following:

Following our discovery of human dihydroorotate dehydrogenase (DHODH) inhibition by 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as well as 2-(4-benzyl-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-methylpyridine, we describe here the syntheses and evaluation of an array of azine-bearing analogs. As in our previous report, the structure-activity study of this series of human DHODH inhibitors was based on a phenotypic assay measuring measles virus replication. Among other inhibitors, this round of syntheses and biol. evaluation iteration led to the highly active 5-cyclopropyl-2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-3-fluoropyridine (I). Inhibition of DHODH by this compoundI was confirmed in an array of in vitro assays, including enzymic tests and cell-based assays for viral replication and cellular growth. I was found to be more active than the known inhibitors of DHODH, brequinar and teriflunomide, thus opening perspectives for its use as a tool or for the design of an original series of immunosuppressive agent. Moreover, because other series of inhibitors of human DHODH have been found to also affect Plasmodium falciparum DHODH, all the compounds were assayed for their effect on P. falciparum growth. However, the modest in vitro inhibition solely observed for two compounds did not correlate with their inhibition of P. falciparum DHODH. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Recommanded Product: 4,5-Diiodo-1H-imidazole).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. In general, organic iodides are light-sensitive and turn yellow during storage, owing to the formation of iodine. In the chemical industry, alkyl iodides serve as excellent alkylating agents and, specifically, methyl iodide is used as a methylating agent in the synthesis of various pharmaceutical drugs.Recommanded Product: 4,5-Diiodo-1H-imidazole

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Azoles. Part 4. Nucleophilic substitution reactions of haloimidazoles was written by Iddon, Brian;Khan, Nazir;Lim, Bee Lan. And the article was included in Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) in 1987.Synthetic Route of C3H2I2N2 This article mentions the following:

A number of N-protected derivatives of 2,4,5-tribromoimidazole, 4-bromo-5-nitroimidazole, and 2,4-dibromo-5-nitroimidazole were prepared by standard procedures and treated with various nucleophiles. Whereas 2,4,5-tribromo (and tri-iodo)imidazole reacted with PhSNa to give 4,5-dihaloimidazoles, 1-protected derivatives of 2,4,5-tribromoimidazole reacted with RSNa (R = Et, Pr, Ph, PhCH₂) in Me₂CHOH, by displacement of the 2-bromine atom. 1-Benzyl-5-bromo-4-nitroimidazole, 2-(5-bromo-4-nitroimidazol-1-yl) acetate, and 5-bromo-4-nitro-1-phenacylimidazole (I) reacted by displacement of the 5-bromine atom. The product arising from reaction of I with HSCH₂CO₂Et in EtOH in the presence of base, cyclized to give imidazothiazine II. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Synthetic Route of C3H2I2N2).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. In the chemical industry, alkyl iodides serve as excellent alkylating agents and, specifically, methyl iodide is used as a methylating agent in the synthesis of various pharmaceutical drugs.Synthetic Route of C3H2I2N2

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase was written by Ding, Min;He, Feng;Hudyma, Thomas W.;Zheng, Xiaofan;Poss, Michael A.;Kadow, John F.;Beno, Brett R.;Rigat, Karen L.;Wang, Ying-Kai;Fridell, Robert A.;Lemm, Julie A.;Qiu, Dike;Liu, Mengping;Voss, Stacey;Pelosi, Lenore A.;Roberts, Susan B.;Gao, Min;Knipe, Jay;Gentles, Robert G.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Category: iodides-buliding-blocks This article mentions the following:

Presented here are initial structure-activity relationship (SAR) studies on a series of novel heteroaryl fused tetracyclic indole-based inhibitors of the hepatitis C viral polymerase, NS5B. The introduction of alternative heterocyclic moieties into the indolo-fused inhibitor class significantly expands the reported SAR and resulted in the identification of pyridino analogs, typified by compounds I and II that displayed excellent potency against the NS5B polymerase of both HCV 1a and HCV 1b genotypes. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Category: iodides-buliding-blocks).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Category: iodides-buliding-blocks

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase was written by Ding, Min;He, Feng;Hudyma, Thomas W.;Zheng, Xiaofan;Poss, Michael A.;Kadow, John F.;Beno, Brett R.;Rigat, Karen L.;Wang, Ying-Kai;Fridell, Robert A.;Lemm, Julie A.;Qiu, Dike;Liu, Mengping;Voss, Stacey;Pelosi, Lenore A.;Roberts, Susan B.;Gao, Min;Knipe, Jay;Gentles, Robert G.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Category: iodides-buliding-blocks This article mentions the following:

Presented here are initial structure-activity relationship (SAR) studies on a series of novel heteroaryl fused tetracyclic indole-based inhibitors of the hepatitis C viral polymerase, NS5B. The introduction of alternative heterocyclic moieties into the indolo-fused inhibitor class significantly expands the reported SAR and resulted in the identification of pyridino analogs, typified by compounds I and II that displayed excellent potency against the NS5B polymerase of both HCV 1a and HCV 1b genotypes. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Category: iodides-buliding-blocks).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Category: iodides-buliding-blocks

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Discovery of Small-Molecule Inhibitors Selectively Targeting the DNA-Binding Domain of the Human Androgen Receptor was written by Li, Huifang;Ban, Fuqiang;Dalal, Kush;Leblanc, Eric;Frewin, Kate;Ma, Dennis;Adomat, Hans;Rennie, Paul S.;Cherkasov, Artem. And the article was included in Journal of Medicinal Chemistry in 2014.Quality Control of 4,5-Diiodo-1H-imidazole This article mentions the following:

The human androgen receptor (AR) is considered as a master regulator in the development and progression of prostate cancer (PCa). As resistance to clin. used anti-AR drugs remains a major challenge for the treatment of advanced PCa, there is a pressing need for new anti-AR therapeutic avenues. In this study, we identified a binding site on the DNA binding domain (DBD) of the receptor and utilized virtual screening to discover a set of micromolar hits for the target. Through further exploration of the most potent hit (1), a structural analog (6) was identified demonstrating 10-fold improved anti-AR potency. Further optimization resulted in a more potent synthetic analog (25) with anti-AR potency comparable to a newly FDA-approved drug Enzalutamide. Site-directed mutagenesis demonstrated that the developed inhibitors do interact with the intended target site. Importantly, the AR DBD inhibitors could effectively inhibit the growth of Enzalutamide-resistant cells as well as block the transcriptional activity of constitutively active AR splice variants, such as V7. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Quality Control of 4,5-Diiodo-1H-imidazole).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organic iodides are widely used in organic synthesis. Halogenation of aromatic hydrocarbons is a very important reaction via an electrophilic aromatic substitution. Organoiodine lubricants can be used with titanium, stainless steels, and other metals which tend to seize up with conventional lubricants: organoiodine lubricants can be used in turbines and spacecraft, and as a cutting oil in machining.Quality Control of 4,5-Diiodo-1H-imidazole

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Probing hydrogen bonding to bound dioxygen in synthetic models for heme proteins: the importance of precise geometry was written by Dube, Henry;Kasumaj, Besnik;Calle, Carlos;Felber, Beatrice;Saito, Makoto;Jeschke, Gunnar;Diederich, Francois. And the article was included in Chemistry – A European Journal in 2009.HPLC of Formula: 15813-09-9 This article mentions the following:

Distal hydrogen bonding in natural dioxygen binding proteins is crucial for the discrimination between different potential ligands such as O₂ or CO. In the present study, we probe the chem. requirements for proper distal hydrogen bonding in a series of synthetic model compounds for dioxygen-binding heme proteins. The model compounds 1-Co to 7-Co bear different distal residues. The hydrogen bonding in their corresponding dioxygen adducts is directly measured by pulse EPR spectroscopy. The geometrical requirements for this interaction to take place were found to be narrow and very specific. Only two model complexes, 1-Co and 7-Co, form a hydrogen bond to bound dioxygen, which was characterized in terms of geometry and nature of the bond. The geometry and dipolar nature of this interaction in 1-Co-O₂ is more similar to the one in natural cobalt myoglobin (Co-Mb), making 1-Co the best model compound in the entire series. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9HPLC of Formula: 15813-09-9).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organic iodides are widely used in organic synthesis. Halogenation of aromatic hydrocarbons is a very important reaction via an electrophilic aromatic substitution. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.HPLC of Formula: 15813-09-9

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Thiophene-expanded guanosine analogues of gemcitabine was written by Chen, Zhe;Ku, Therese C.;Seley-Radtke, Katherine L.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.Recommanded Product: 4,5-Diiodo-1H-imidazole This article mentions the following:

The chemotherapeutic drug Gemcitabine, 2′,2′-difluoro-2′-deoxycytidine, has long been the standard of care for a number of cancers. Gemcitabine’s chemotherapeutic properties stem from its 2′,2′-difluoro-2′-deoxyribose sugar, which mimics the natural nucleoside, but also disrupts nucleic acid synthesis, leading to cell death. As a result, numerous analogs have been prepared to further explore the biol. implications for this structural modification. In that regard, a thieno-expanded guanosine analog was of interest due to biol. activity previously observed for the tricyclic heterobase scaffold. Several analogs were prepared, including the McGuigan ProTide, however the parent nucleoside exhibited the best chemotherapeutic activity, specifically against breast cancer cell lines (89.53% growth inhibition). In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Recommanded Product: 4,5-Diiodo-1H-imidazole).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organoiodine compounds occur widely in organic chemistry, but are relatively rare in nature. A typical method for synthesis of aromatic iodides is diazotization of primary aromatic amines followed by treatment of potassium iodide. Aliphatic alcohols are converted to alkyl iodides by treating with hydrogen iodide.Recommanded Product: 4,5-Diiodo-1H-imidazole

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Synthesis of Complexes with Abnormal “Protic” N-Heterocyclic Carbenes was written by Jin, Hanpeng;Tan, Tristan Tsai Yuan;Hahn, F. Ekkehardt. And the article was included in Angewandte Chemie, International Edition in 2015.Product Details of 15813-09-9 This article mentions the following:

Neutral 4-iodo-N-ethylimidazole 3 oxidatively adds to [Pt(PPh₃)₄] to give, in the presence of different tetraalkylammonium salts, complexes trans-[4], trans-[5], and trans-[6] containing an anionic C4-bound heterocycle with an unsubstituted ring-nitrogen atom. Complex trans-[4] reacts with the proton source NH₄I under protonation of the ring-nitrogen atom to produce complex trans-[7]I which bears an NH,NR-substituted aNHC ligand. The reaction of trans-[4] with CH₃I yields the complex trans-[8]I which has a classical aNHC ligand with two alkylated ring-nitrogen atoms. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Product Details of 15813-09-9).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Iodide-containing intermediates are common in organic synthesis, because of the easy formation and cleavage of the C–I bond. Polyiodoorganic compounds are sometimes employed as X-ray contrast agents, in fluoroscopy, a type of medical imaging. This application exploits the X-ray absorbing ability of the heavy iodine nucleus.Product Details of 15813-09-9

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro was written by Thames, Joy E.;Waters, Charles D. III;Valle, Coralie;Bassetto, Marcella;Aouadi, Wahiba;Martin, Baptiste;Selisko, Barbara;Falat, Arissa;Coutard, Bruno;Brancale, Andrea;Canard, Bruno;Decroly, Etienne;Seley-Radtke, Katherine L.. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Safety of 4,5-Diiodo-1H-imidazole This article mentions the following:

Flaviviruses, such as Dengue (DENV) and Zika (ZIKV) viruses, represent a severe health burden. There are currently no FDA-approved treatments, and vaccines against most flaviviruses are still lacking. We have developed several flexible analogs (“fleximers”) of the FDA-approved nucleoside Acyclovir that exhibit activity against various RNA viruses, demonstrating their broad-spectrum potential. The current study reports activity against DENV and Yellow Fever Virus (YFV), particularly for compound 1. Studies to elucidate the mechanism of action suggest the flex-analog triphosphates, especially 1-TP, inhibit DENV and ZIKV methyltransferases, and a secondary, albeit weak, effect on the DENV RNA-dependent RNA polymerase was observed at high concentrations The results of these studies are reported herein. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Safety of 4,5-Diiodo-1H-imidazole).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. In general, organic iodides are light-sensitive and turn yellow during storage, owing to the formation of iodine. Organoiodine lubricants can be used with titanium, stainless steels, and other metals which tend to seize up with conventional lubricants: organoiodine lubricants can be used in turbines and spacecraft, and as a cutting oil in machining.Safety of 4,5-Diiodo-1H-imidazole

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Approaches to the synthesis of 5-benzylidene-2-imidazolin-4-ones was written by Prager, Rolf H.;Tsopelas, Chris. And the article was included in Australian Journal of Chemistry in 1990.Product Details of 15813-09-9 This article mentions the following:

Aromatic aldehydes, but not ketones, condensed with glycocyamidine to give the benzylideneamines. α-Alkylbenzylideneglycocyamidines were made from glycidic esters by reaction with guanidine, followed by cyclization with Ac₂O. A number of mono- and diacetylated derivatives of 6,7-dihydropyrrolo[2,3-c]azepine-4,8(1H,5H)-dione have been prepared, but failed to undergo the Darzens reaction. Bromo- and iodo-2-arylazoimidazoles, protected on N by the methoxyethoxymethyl group, failed to undergo clean lithiation. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Product Details of 15813-09-9).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organic iodides can be alkyl, alkenyl, or alkynyl, and all of them are very reactive toward with many kinds of nucleophiles. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Product Details of 15813-09-9

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com