Category: 117918-23-7

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.Name: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid.Zhang, Meihui; Nguyen, Jeffrey-Tri; Kumada, Henri-Obadja; Kimura, Tooru; Cheng, Maosheng; Hayashi, Yoshio; Kiso, Yoshiaki published the article 《Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme》 about this compound( cas:117918-23-7 ) in Bioorganic & Medicinal Chemistry. Keywords: HTLVI protease inhibitor tetrapeptide preparation structure activity relationship. Let’s learn more about this compound (cas:117918-23-7).

Adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy are only some of the more common end results of an infection with a human T-cell leukemia virus type 1 (HTLV-I). Expanding from their previous reports, the authors have synthesized all different permutations of tetrapeptidic HTLV-I protease inhibitors using at least eight P3-cap and five P’1-cap moieties. The inhibitors exhibited over 97% inhibition against HIV-1 protease and a wide range of inhibitory activity against HTLV-I protease.

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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: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Synthesis and Structure-Activity Relationships of a Series of Penicillin-Derived HIV Proteinase Inhibitors: Heterocyclic Ring Systems Containing P1′ and P2′ Substituents.Recommanded Product: 117918-23-7.

As an extension of our earlier work based upon a single penicillin-derived thiazolidine moiety we have found that the decahydroisoquinoline grouping, also present in Ro 31-8959, is an effective replacement for one of the thiazolidine units in C2 sym. penicillin-derived dimers. Reaction of racemic epoxide I with [3S-[3α,4aα,8aα]]-decahydro-N-(1,1-dimethylethyl)-3-isoquinolinecarboxamide gave diastereoisomers (R)- and (S)-II. Reaction of the amines derived from (R)- and (S)-II with thiazolidine III gave thiazolidineacetamides (R)- and (S)-IV, resp. (S)-IV was a potent inhibitor of HIV proteinase (IC50 = 23 nM) with antiviral activity against HIV-1 in vitro (EC50 C8166 cells = 50 nM). However, a poor pharmacokinetic profile in the dog for (S)-IV and its analogs, in keeping with earlier studies on penicillin-derived dimers in three species, precluded their development as potential antivirals.

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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; Kato, Ryohei; Takaku, Haruo; Nojima, Satoshi; Terashima, Keisuke; Misawa, Satoru; Fukazawa, Tominaga; Ueno, Takamasa; Sato, Hideharu; Shintani, Makoto; Kiso, Yoshiaki; Hayashi, Hideya published the article 《Structure-Activity Relationship of Small-Sized HIV Protease Inhibitors Containing Allophenylnorstatine》 about this compound( cas:117918-23-7 ) in Journal of Medicinal Chemistry. Keywords: peptidomimetic HIV1 protease inhibitor allophenylnorstatine preparation MSBAR. Let’s learn more about this compound (cas:117918-23-7).

We designed and synthesized a new class of peptidomimetic human immunodeficiency virus (HIV) protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenyl-butyric acid], with a hydroxymethyl-carbonyl (HMC) isostere as the active moiety. A systematic evaluation of structure-activity relationships for HIV protease inhibition, anti-HIV activities, and pharmacokinetic profiles has led to the delineation of a set of structural characteristics that appear to afford an orally available HIV protease inhibitor. Optimum structures, exemplified by (I) (JE-2147), incorporated 3-hydroxy-2-methylbenzoyl groups as the P2 ligand, (R)-5,5-dimethyl-1,3-thiazolidine-4-carbonyl (Dmt) residue at the P1′ site, and 2-methylbenzyl-carboxamide group as the P2′ ligand. The present study demonstrated that I has potent antiviral activities in vitro and exhibits good oral bioavailability and plasma pharmacokinetic profiles in two species of laboratory animals.

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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 Structure-activity studies of FIV and HIV protease inhibitors containing allophenylnorstatine, published in 2001-05-31, which mentions a compound: 117918-23-7, mainly applied to FIV HIV protease inhibitor allophenylnorstatine derivative preparation; structure activity FIV HIV protease inhibitor allophenylnorstatine derivative, Electric Literature of C11H19NO4S.

The interaction of P1 and P3 side chains with the combining S1 and S3 hydrophobic subsites of HIV and FIV proteases has been explored using asym. competitive inhibitors. The inhibitors evaluated contained (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid (allophenylnorstatine) as the hydroxymethylcarbonyl isostere, (R)-5,5-dimethyl-1, 3-thiazolidine-4-carbonyl as P1′, Val as P2 and P2′ residues, and a variety of amino acids at the P3 and P3′ positions. All inhibitors showed competitive inhibition of both enzymes with higher potency against the HIV protease in vitro. Within this series, VLE776 is the most effective inhibitor against FIV protease, and it contains Phe at P3, but no P3′ residue. VLE776 also exhibited potent antiviral activities against the drug-resistant HIV mutants (G48V and V82F) and the TL3-resistant HIV mutants. Explanation of the inhibition activities was described. In addition, a new strategy was described for development of bifunctional inhibitors, which combine the protease inhibitor and another enzyme inhibitor in one mol.

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Related Products of 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 Maintaining potent HTLV-I protease inhibition without the P3-cap moiety in small tetrapeptidic inhibitors. Author is Nguyen, Jeffrey-Tri; Kato, Keiko; Kumada, Henri-Obadja; Hidaka, Koushi; Kimura, Tooru; Kiso, Yoshiaki.

The human T cell lymphotropic/leukemia virus type 1 (HTLV-I) causes adult T cell lymphoma/leukemia. The virus is also responsible for chronic progressive myelopathy and several inflammatory diseases. To stop the manufacturing of new viral components, in our previous reports, we derived small tetrapeptidic HTLV-I protease inhibitors with an important amide-capping moiety at the P3 residue. In the current study, we removed the P3-cap moiety and, with great difficulty, optimized the P3 residue for HTLV-I protease inhibition potency. We discovered a very potent and small tetrapeptidic HTLV-I protease inhibitor (KNI-10774a, IC50 = 13 nM).

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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 Allophenylnorstatine-containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P2 ligands, published in 2005-06-30, 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.

The design and development of potent HIV protease inhibitors remain an attractive target for antiviral therapy. A novel class of HIV protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4 phenylbutyric acid] as a transition state mimic have been reported. In this work we fixed P2′ (as tert-butylamino or 2-methylbenzylamino) and changed P2 moiety to provide two series of dipeptide analogs. Preliminary evaluation of the activity of the synthesized derivatives were determined as percentage of enzyme inhibition at 5 μM level. The results showed that the introduction of 2-methylbenzylamino moiety as P2′ ligands considerably improved HIV inhibitory activity in comparison with the tert-Bu amino analogs. It was found that compounds in both series retained activity still less than the lead compounds KNI-577 and KNI-727.

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Synthetic Route of C11H19NO4S. 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 Attachment of basic amino group to plasmepsin inhibitors exhibiting potent antimalarial activity. Author is Kashimoto, Keisuke; Hidaka, Koushi; Uemura, Tsuyoshi; Miura, Takuya; Freire, Ernesto; Kimura, Tooru; Kiso, Yoshiaki.

Plasmepsin (Plm) is a target for new antimalarial drugs, but most reported Plm inhibitors have relatively low antimalarial activities. So, we attached substituents on a structure of the highly potent Plm inhibitor KNI-10006. Among the derivatives, amino-substituted compound such as KNI-10538 exhibited enhanced antimalarial activity maintaining potent Plm II inhibitory activity. These results suggest that auxiliary substituents of specific basic group contribute to deliver the inhibitors to the target Plm. We further synthesized the alkylamino derivatives

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SDS of cas: 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 several small-size HTLV-I protease inhibitors with different hydrophilicity profiles. Author is Nguyen, Jeffrey-Tri; Kato, Keiko; Hidaka, Koushi; Kumada, Henri-Obadja; Kimura, Tooru; Kiso, Yoshiaki.

The human T cell leukemia/lymphotropic virus type 1 (HTLV-I) is clin. associated with adult T cell leukemia/lymphoma, HTLV-I associated myelopathy/tropical spastic paraparesis, and a number of other chronic inflammatory diseases. To stop the replication of the virus, we developed highly potent tetrapeptidic HTLV-I protease inhibitors. In a recent X-ray crystallog. study, several of our inhibitors could not form co-crystal complexes with the protease due to their high hydrophobicity. In the current study, we designed, synthesized and evaluated the HTLV-I protease inhibition potency of compounds with hydrophilic end-capping moieties with the aim of improving pharmaceutic and pharmacokinetic properties.

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Hidaka, Koushi; Kimura, Tooru; Tsuchiya, Yumi; Kamiya, Mami; Ruben, Adam J.; Freire, Ernesto; Hayashi, Yoshio; Kiso, Yoshiaki published the article 《Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II》. Keywords: allophenylnorstatine tripeptidomimetic preparation inhibitor malarial aspartic protease plasmepsin; plasmepsin inhibitor allophenylnorstatine tripeptidomimetic preparation structure activity relationship; antimalarial agent allophenylnorstatine tripeptidomimetic preparation.They researched the compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid( cas:117918-23-7 ).Application In Synthesis of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid. 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:117918-23-7) here.

Based on a highly potent allophenylnorstatine-containing inhibitor, KNI-10006, against the plasmepsins of Plasmodium falciparum, the authors synthesized a series of tripeptide-type compounds with various N-terminal moieties and evaluated their inhibitory activities against plasmepsin II (Plm II). Certain phenylacetyl derivatives exhibited extremely high affinity with Ki < 0.1 nM suggesting successful hydrophobic interactions. Compounds in my other articles are similar to this one((R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid)Application In Synthesis of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.

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Synthetic Route of C11H19NO4S. 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 Structure-activity and structure-metabolism relationships of HIV protease inhibitors containing the 3-hydroxy-2-methylbenzoyl-allophenylnorstatine structure. Author is Mimoto, Tsutomu; Terashima, Keisuke; Nojima, Satoshi; Takaku, Haruo; Nakayama, Mitsunobu; Shintani, Makoto; Yamaoka, Takashi; Hayashi, Hideya.

A series of peptidomimetic human immunodeficiency virus (HIV) protease inhibitors containing substituted allophenylnorstatine [Apns: (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid] were designed and synthesized. From the structure-metabolism relationship of this type of HIV protease inhibitors, the compounds having para substitution of the Ph ring of Apns and/or 2,6-disubstitution of the P2′ benzylamine were found to be able to avoid the P2 phenol glucuronidation that occurs with SM-319777 (formerly named JE-2147, KNI-764); one of the main metabolic pathways of SM-319777. These new analogs, such as SM-322377, had more desirable pharmacokinetic profiles and more potent antiviral activity against not only wild type HIV-1 but also the multi-drug-resistant HIV-1 than SM-319777.

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