Category: 117918-23-7

Related Products of 117918-23-7. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Effect of dipeptidomimetics on malaria parasite proliferation inhibition targeting plasmepsin. Author is Hidaka, Koushi; Kimura, Tooru; Uemura, Tsuyoshi; Ruben, Adam J.; Freire, Ernesto; Kiso, Yoshiaki.

To improve the antimalarial activity of peptidomimetic plasmepsin (Plm) inhibitors, we attached substituents on a structure of the highly potent Plm inhibitor KNI-10006. Among the derivatives, we identified a methylamino compound, i.e., KNI-10283, with 15-fold enhanced antimalarial activity, to the sub-micromolar level, maintaining Plm inhibitory activity and low cytotoxicity.

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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, Article, Archiv der Pharmazie (Weinheim, Germany) called A novel dipeptide-based HIV protease inhibitor containing allophenylnorstatine, Author is Abdel-Rahman, Hamdy M.; El-Koussi, Nawal A.; Alkaramany, Gamal S.; Youssef, Adel F.; Kiso, Yoshiaki, which mentions a compound: 117918-23-7, SMILESS is O=C([C@H]1N(C(OC(C)(C)C)=O)CSC1(C)C)O, Molecular C11H19NO4S, Name: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid.

Dipeptide analogs, such as I and II [P2′ = NHCMe2Ph, NHN(Me)Ph, NH2CH2C6H4-2-OMe, etc.] incorporating allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition state mimic at the scissile bond, were designed and synthesized in the hope of obtaining a novel KNI series of HIV protease inhibitors. Improved activity of most of the members of series II relative to their analogs of series I can be partially attributed to the differences in the structures of the P2 moieties. Positional isomerism in the P2′ moieties significantly affected the activity and polarity of the target.

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Reference of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid. 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 Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.

Plasmepsin (Plm) is a potential target for new antimalarial drugs, but most reported Plm inhibitors have relatively low antimalarial activities. We synthesized a series of dipeptide-type HIV protease inhibitors, which contain an allophenylnorstatine-dimethylthioproline scaffold to exhibit potent inhibitory activities against Plm II. Their activities against Plasmodium falciparum in the infected erythrocyte assay were largely different from those against the target enzyme. To improve the antimalarial activity of peptidomimetic Plm inhibitors, we attached substituents on a structure of the highly potent Plm inhibitor KNI-10006. Among the derivatives, we identified alkylamino compounds such as 44 (KNI-10283) and 47 (KNI-10538) with more than 15-fold enhanced antimalarial activity, to the sub-micromolar level, maintaining their potent Plm II inhibitory activity and low cytotoxicity. These results suggest that auxiliary substituents on a specific basic group contribute to deliver the inhibitors to the target Plm.

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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 Hybrid phase ligation for efficient synthesis of histone proteins, published in 2016, which mentions a compound: 117918-23-7, mainly applied to histone protein synthesis hybrid phase ligation refolding; solid phase peptide synthesis NCL desulfurization, COA of Formula: C11H19NO4S.

We introduce a hybrid solid-solution phase ligation approach that combines the efficiency of solid phase ligation with solution phase ligation in the total synthesis of modified histone proteins. A two linker strategy allows anal. throughout work on the solid phase and maximizes yields through cleavage at an external Rink, while an internal HMBA linker allows the native carboxyl terminus for any protein sequence. We demonstrate this approach for two histone proteins: triple-acetylated H4, K5ac, K12ac, K91ac, and CENP-A-K124ac.

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Recommanded Product: 117918-23-7. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus. Author is Lu, Zhijian; Raghavan, Subharekha; Bohn, Joann; Charest, Mark; Stahlhut, Mark W.; Rutkowski, Carrie A.; Simcoe, Amy L.; Olsen, David B.; Schleif, William A.; Carella, Anthony; Gabryelski, Lori; Jin, Lixia; Lin, Jiunn H.; Emini, Emilio; Chapman, Kevin; Tata, James R..

A series of highly potent HIV protease inhibitors were designed and synthesized. These compounds are active against various clin. viral isolates as well as wild-type virus. The synthesis and biol. activity of these HIV protease inhibitors are discussed.

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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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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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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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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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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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