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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Crystal structures of the free and inhibited forms of plasmepsin I (PMI) from Plasmodium falciparum, published in 2011-07-31, which mentions a compound: 117918-23-7, Name is (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, Molecular C11H19NO4S, Name: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid.

Plasmepsin I (PMI) is one of the four vacuolar pepsin-like proteases responsible for Hb degradation by the malarial parasite Plasmodium falciparum, and the only one with no crystal structure reported to date. Due to substantial functional redundancy of these enzymes, lack of inhibition of even a single plasmepsin can defeat efforts in creating effective antiparasitic agents. We have now solved crystal structures of the recombinant PMI as apoenzyme and in complex with the potent peptidic inhibitor, KNI-10006, at the resolution of 2.4 and 3.1 Å, resp. The apoenzyme crystallized in the orthorhombic space group P212121 with two mols. in the asym. unit and the structure has been refined to the final R-factor of 20.7%. The KNI-10006 bound enzyme crystallized in the tetragonal space group P43 with four mols. in the asym. unit and the structure has been refined to the final R-factor of 21.1%. In the PMI-KNI-10006 complex, the inhibitors were bound identically to all four enzyme mols., with the opposite directionality of the main chain of KNI-10006 relative to the direction of the enzyme substrates. Such a mode of binding of inhibitors containing an allophenylnorstatine-dimethylthioproline insert in the P1-P1′ positions, previously reported in a complex with PMIV, demonstrates the importance of satisfying the requirements for the proper positioning of the functional groups in the mechanism-based inhibitors towards the catalytic machinery of aspartic proteases, as opposed to binding driven solely by the specificity of the individual enzymes. A comparison of the structure of the PMI-KNI-10006 complex with the structures of other vacuolar plasmepsins identified the important differences between them and may help in the design of specific inhibitors targeting the individual enzymes.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid( cas:117918-23-7 ) is researched.Formula: C11H19NO4S.Mimoto, Tsutomu; Hattori, Naoko; Takaku, Haruo; Kisanuki, Sumitsugu; Fukazawa, Tominaga; Terashima, Keisuke; Kato, Ryohei; Nojima, Satoshi; Misawa, Satoru; Ueno, Takamasa; Imai, Junya; Enomoto, Hiroshi; Tanaka, Shigeki; Sakikawa, Hiroshi; Shintani, Makoto; Hayashi, Hideya; Kiso, Yoshiaki published the article 《Structure-activity relationship of orally potent tripeptide-based HIV protease inhibitors containing hydroxymethylcarbonyl isostere》 about this compound( cas:117918-23-7 ) in Chemical & Pharmaceutical Bulletin. Keywords: HIV protease inhibitor KNI272 allophenylnorstatine structure activity. Let’s learn more about this compound (cas:117918-23-7).

We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relationship study of HIV-1 protease inhibition, enzyme selectivity for other aspartyl proteases, the antiviral activity and pharmacokinetics in rats, KNI-227 and KNI-272, our first clin. candidate were found to be selective and orally potent HIV protease inhibitors. Moreover, an improvement of the pharmacokinetic features of KNI-272 provided two long-lasting and highly bioavailable compounds JE-2178, and JE-2179.

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Electric Literature of C21H16N2. 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: 2,4,5-Triphenylimidazole, is researched, Molecular C21H16N2, CAS is 484-47-9, about An eco-friendly, one pot synthesis of tri-substituted imidazoles in aqueous medium catalyzed by RGO supported Au nano-catalyst and computational studies.

An eco-compatible, mild and operationally simple aqueous phase protocol for the synthesis of 2,4,5-trisubstituted imidazoles I [Ar = Ph, 2-MeC6H4, 2-naphthyl, etc.] was developed with high substrate scope using supported Au nanoparticles. The catalyst could be recovered for the subsequent reactions and reused without any appreciable loss. The utility of this protocol was further explored to synthesis of fused and structurally versatile imidazole also. The synthetic attributes of imidazoles were also demonstrated through the computational studies. Furthermore, low E-factor and process mass intensity made the this method more sustainable as compared to earlier literature reports.

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Category: nitriles-buliding-blocks. 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: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Potent angiotensin II antagonists with non-β-branched amino acids in position 5.

Amino acids with lipophilic side chains that contain more than one functional group on the β-carbon, i.e. a β-branched hydrocarbon moiety, are required in position 5 of angiotensin II (AII) analogs with potent agonist activity. This requirement for agonist activity does not follow for AII analogs with potent antagonist activity. Straight-chain amino acids may be substituted into position 5 of [Sar1,X5,Ile8]AII (Sar = sarcosine, X = amino acid) with retention or enhancement of antagonist activity. β-Branched side chains can still enhance the antagonist activities of [Sar1,X5,Ile8]AII. An x-ray crystal structure of Me3CO2C-(βMe)Phe-OH dicyclohexylamine salt, prepared for the solid-phase synthesis of [Sar1,(βMe)Phe5,Ile8]AII, revealed an S,S-configuration for the α- and β-carbon atoms. Contrary to previous literature reports, chem. nonequivalence of the δ-protons of Pro was observed in the 1H NMR spectra of [Sar1,X5,Ile8]AII analogs bearing both β-branched X5 side chains (X5 = Ile) and non-β-branched X5 side chains (X5 = Ala, His).

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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 Tandem Gold-Catalyzed Dehydrative Cyclization/Diels-Alder Reactions: Facile Access to Indolocarbazole Alkaloids, published in 2015-04-03, which mentions a compound: 166329-43-7, mainly applied to indolocarbazole alkaloid synthesis tandem dehydrative cyclization Diels Alder cycloaddition, Quality Control of tert-Butyl (2-(bromomethyl)phenyl)carbamate.

A gold-catalyzed synthesis of cyclic 2-oxodienes from readily prepared propargyl alcs. and the subsequent Diels-Alder reaction are reported. The dehydrative cyclization reactions proceeded smoothly, and the dienes formed in situ were demonstrated to undergo cycloaddition with a variety of dienophiles. This method offers a new strategy for the synthesis of indolocarbazole alkaloids, whereby the convergent synthetic design allows for differentiation between the indole nitrogens.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2,4,5-Triphenylimidazole( cas:484-47-9 ) is researched.Recommanded Product: 2,4,5-Triphenylimidazole.Naidoo, Shivani; Jeena, Vineet published the article 《Molecular iodine/DMSO mediated oxidation of internal alkynes and primary alcohols using a one-pot, two step approach towards 2,4,5-trisubstituted imidazoles: Substrate scope and mechanistic studies》 about this compound( cas:484-47-9 ) in Tetrahedron. Keywords: imidazole preparation green chem; aryl alkyne primary alc tandem oxidation. Let’s learn more about this compound (cas:484-47-9).

An efficient, eco-friendly and practical oxidation of internal alkynes R1CCR2 (R1 = Ph, 4-bromophenyl; R2 = Ph, 4-bromophenyl, 4-chlorophenyl) and primary alcs. R3CH2OH (R3 = furan-2-yl, naphthalen-2-yl, cyclohexyl, etc.) as key steps towards the synthesis of 2,4,5-trisubstituted imidazoles I is reported. This green synthetic methodol. employed an acid and metal-free mol. iodine/DMSO system to afford a variety of substituted imidazoles I in moderate to good yields, with a range of functionalities tolerated. Mechanistic studies revealed two distinct oxidation pathways, which ultimately form the benzil and benzaldehyde that serve as key intermediates in the multicomponent domino synthesis.

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Quality Control of 2,4,5-Triphenylimidazole. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,4,5-Triphenylimidazole, is researched, Molecular C21H16N2, CAS is 484-47-9, about Expedient access To 2,4,5-trisubstituted imidazoles by simple grinding using kaolin impregnated ZnO/SiO2 nanocomposite: homo-lumo, in vitro and in silico studies. Author is Avvadukkam, Jayashree; Badiadka, Narayana; Kunhanna, Sarojini B..

The convergent synthesis of 2,4,5-trisubstituted imidazoles I [R = H, 4-Cl, 3,4-di-OMe, etc.] was studied using the newly introduced catalytic system of kaolin-impregnated ZnO/SiO2 nanocomposite. The catalyst was effective enough to run the reaction under solvent-free conditions by grinding benzil, substituted benzaldehydes and ammonium acetate at room temperature The characterization of synthesized catalyst by means of FESEM and XRD anal. revealed that the combination of the individual components retained its morphol. and crystallinity. The HOMO-LUMO anal. was helped to understand the charge transfer within the mols. The mol. docking studies showed that all newly synthesized mols. fit the active site of the β-Ketoacyl-acyl carrier protein synthase III enzyme (FabH) and represent a promising extension for the existing antibacterial agents.

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Synthetic Route of C21H16N2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 2,4,5-Triphenylimidazole, is researched, Molecular C21H16N2, CAS is 484-47-9, about Multicomponent reactions synthesis of triaryl-1H imidazoles using reductive-oxidative reactions by MnO2-FeSO4 as a catalyst. Author is Raheem, Ali A.; Saleh, Ali T..

Some novel triaryl-imidazoles I [R = H, Cl, OH] were synthesized using one-pot multicomponent reaction of benzil, benzaldehydes and ammonium acetate in the presence of MnO2/FeSO4 as a reductive-oxidative catalyst under mild conditions. The obtained compounds were nontoxic, excellent yields and environmentally friendly. The catalytic mixture was prepared by ground them together in a mortar with a pestle at room temperature for several minutes; after that, they purified by column chromatog.

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Application In Synthesis of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid. 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: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Small-Sized Human Immunodeficiency Virus Type-1 Protease Inhibitors Containing Allophenylnorstatine to Explore the S2′ Pocket. Author is Hidaka, Koushi; Kimura, Tooru; Abdel-Rahman, Hamdy M.; Nguyen, Jeffrey-Tri; McDaniel, Keith F.; Kohlbrenner, William E.; Molla, Akhteruzzaman; Adachi, Motoyasu; Tamada, Taro; Kuroki, Ryota; Katsuki, Noriko; Tanaka, Yoshiaki; Matsumoto, Hikaru; Wang, Jun; Hayashi, Yoshio; Kempf, Dale J.; Kiso, Yoshiaki.

A series of HIV protease inhibitors based on the allophenylnorstatine structure with various P2′ moieties were synthesized. Among these analogs, it was discovered that a small allyl group (R1) would maintain potent enzyme inhibitory activity compared to the o-methylbenzyl moiety in clin. candidate I (R1 = 2-MeC6H4CH2; R2 = 3-HO-2-MeC6H3) (KNI-764, also known as JE-2147, AG-1776, or SM-319777). Introduction of an anilinic amino group to I (R1 = t-Bu; R2 = 2,6-Me2C6H3OCH2) (KNI-727) improved water-solubility and anti-HIV-1 activity. X-ray crystallog. anal. of I (R1 = H2C:CMeCH2; R2 = 4-H2N-2,6-Me2C6H2OCH2) [KNI-1689; (II)] with a β-methallyl group at P2′ position revealed hydrophobic interactions with Ala28, Ile84, and Ile50′ similar to that of KNI-764. The presence of an addnl. Me group on the allyl group in compound II significantly increased anti-HIV activity over KNI-764 while providing a rational drug design for structural minimization and improving membrane permeability.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Dipeptide-type inhibitors targeting plasmepsins from Plasmodium falciparum, published in 2003, which mentions a compound: 117918-23-7, Name is (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, Molecular C11H19NO4S, Safety of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid.

A symposium report. A series of dipeptide-type inhibitors containing allophenylnorstatine-dimethylthioproline scaffold against malarial aspartic protease plasmepsin II (Plm II) was synthesized. Among these compounds, KNI-10006 which has aminoindanol at the P2′ position was found to inhibit Plm II with a Ki value of 0.5 nM. From a SAR study, it is concluded that both the hydroxyl group and the indan structure of the aminoindanol of KNI-10006 are important for its tight binding.

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Reference:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts