Category: 117918-23-7

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 117918-23-7, is researched, Molecular C11H19NO4S, about Design and synthesis of dipeptide-type HIV-1 protease inhibitors with high antiviral activity, the main research direction is asym synthesis dipeptide human HIV1 protease inhibitor antiviral agent; dipeptide human HIV1 protease inhibitor antiviral agent preparation symposium.HPLC of Formula: 117918-23-7.

A symposium report. A series of peptidomimetic HIV protease inhibitors, e.g. I, containing allophenylnorstatine [Apns, (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid] with a hydroxymethylcarbonyl (HMC) isostere as a transition-state mimetic was designed and synthesized. From the structure-activity relationship studies, potent dipeptide-type inhibitors having high antiviral activity either in the absence or in the presence of 50% human serum were discovered.

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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 A concise synthesis of (2S,3S)-BocAHPBA and (R)-BocDMTA, chiral building blocks for peptide-mimetic HIV protease inhibitors, published in 2002-06-21, which mentions a compound: 117918-23-7, Name is (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, Molecular C11H19NO4S, SDS of cas: 117918-23-7.

Scalable syntheses of (2S,3S)-3-N-tert-butoxycarbonylamino-2-hydroxy-4-phenylbutanoic acid (BocAHPBA) and (R)-3-tert-butoxycarbonyl-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid (BocDMTA) have been developed. Both BocAHPBA and BocDMTA can serve as chiral building blocks in assembling JE-2147 (KNI-764), a potent HIV protease inhibitor. The synthesis of (2S,3S)-BocAHPBA is achieved in 41% overall yield from (S)-2-N,N-dibenzylamino-3-phenylpropanal in five steps where Tamao’s reagent [Me2(i-PrO)SiCH2MgCl] is employed for a one-carbon homologation, and Zhao’s oxidation protocol (TEMPO, NaClO2, NaClO) is applied to convert a 1,2-glycol moiety into an α-hydroxy acid motif. (R)-BocDMTA is synthesized with 99.4% ee in 24% yield via enantioselective hydrolysis of Me (±)-5,5-dimethyl-1,3-thiazolidine-4-carboxylate by a Klebsiella oxytoca hydrolase; the unreacted (S)-ester I can be recovered and racemized with NaOMe to afford (±)-I in 46% yield for another round of the enzymic processing.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 117918-23-7, is researched, Molecular C11H19NO4S, about KNI-577, a potent small-sized HIV protease inhibitor based on the dipeptide containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic, the main research direction is HIV protease inhibitor KNI577 allophenylnorstatine isostere; KNI577 synthesis transition state structure antiviral.Quality Control of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid.

Potent small-sized HIV protease inhibitors containing the hydroxymethylcarbonyl isostere were reported. The inhibitor KNI-727 with a dimethylmethoxyacetyl group in P2 position had a HIV protease inhibition of 95.9% at 50 nM and an anti-HIV activity EC50 of 1.73 μM in MT4 cells. Cyclization of the P2 moiety in KNI-549 resulted in the inhibitor KNI-577 (87.6% inhibition at 50 nM) with a remarkable anti-HIV-1(IIIB) activity (EC50=0.02 μM in CEM-SS cells). This antiviral activity was higher than that of the tripeptide KNI-272. KNI-577 had very low cytotoxicity (CC50>200 μM) and the bioavailability after intraduodenal administration in rats was 48%. A convenient synthetic scheme of KNI-577 was given.

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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, Peptide Science called Evaluation of peptidomimetic inhibitors against malarial protease plasmepsin, Author is Tsuchiya, Yumi; Hidaka, Koushi; Kiso, Aiko; Kimura, Tooru; Hayashi, Yoshio; Nezami, Azin; Freire, Ernesto; 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, Recommanded Product: 117918-23-7.

We synthesized a series of plasmepsin (Plm) II inhibitors containing an allophenyl norstatine-dimethylthioproline scaffold. From the SAR study of tripeptide-type inhibitor, we found that methylthiolalanine fitted to the S2 pocket. Then, we introduced aminoindanol at the P2′ position of KNI-227 and obtained KNI-10033 as a new tripeptide-type lead compound On the other hand, among KNI compounds, KNI-10125 which has a hydroxymethylphenoxyacetyl group, showed the most potent antimalarial activity.

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Recommanded Product: 117918-23-7. 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 Small dipeptide-based HIV protease inhibitors containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic.

The human immunodeficiency virus (HIV) codes for an aspartic protease is known to be essential for retroviral maturation and replication. HIV protease is formed from two identical 99 amino acid peptides. Using the thioether chem. ligation method, [(NHCH2CH2-S-CH2CO)51-52, Ala67,95]HIV-1 protease was synthesized and then the [(NHCH2CH2-S-CH2CO)51-52, Ala67,95, Cys98]HIV-1 protease dimer analog covalently linked by a disulfide bridge was prepared These HIV-1 protease analogs effectively cleaved the Tyr-Phe-type substrate, but had weak affinity to the Tyr-Pro-type substrate. Consequently, the mol. recognition of the protease analogs differs from that of the wild-type enzyme. Based on the substrate transition state, a novel class of HIV protease inhibitors containing an unnatural amino acid, (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid, named allophenylnorstatine, with a hydroxymethylcarbonyl (HMC) isostere were designed and synthesized. The stereochem. of the hydroxyl group was significant for the enzyme inhibition and the HMC group interacted excellently with the aspartic acid carboxyl groups of HIV protease active site in the essentially same hydrogen-bonding mode as the transition state. Small dipeptide-based HIV protease inhibitors containing the HMC isostere were studied as advantageous compounds Among them, a dipeptide-based HIV protease inhibitor, KNI-577, exhibited potent antiviral activities, low cytotoxicity, and good pharmacokinetic properties.

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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.Abrahamsson, K.; Andersson, P.; Bergman, J.; Bredberg, U.; Braanalt, J.; Egnell, A.-C.; Eriksson, U.; Gustafsson, D.; Hoffman, K.-J.; Nielsen, S.; Nilsson, I.; Pehrsson, S.; Polla, M. O.; Skjaeret, T.; Strimfors, M.; Wern, C.; Oelwegaard-Halvarsson, M.; Oertengren, Y. researched the compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid( cas:117918-23-7 ).Related Products of 117918-23-7.They published the article 《Discovery of AZD8165 – a clinical candidate from a novel series of neutral thrombin inhibitors》 about this compound( cas:117918-23-7 ) in MedChemComm. Keywords: human propionate prodrug thrombin inhibitor pharmacol response. We’ll tell you more about this compound (cas:117918-23-7).

A novel series of neutral thrombin inhibitors has been developed using a selection process based on docking experiments and property calculations and predictions. This work resulted in the identification of the highly potent thrombin inhibitor compound 85 (Ki = 300 pM) and the corresponding propionate prodrug 5 (AZD8165) as a candidate for clin. evaluation in the treatment of thrombosis and related diseases. AZD8165 was found to be safe and well tolerated and delivered the expected pharmacol. response in a phase I trial in healthy male volunteers.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure, the main research direction is HIV1 protease inhibitor allophenylnorstatine derivative preparation structure activity.Computed Properties of C11H19NO4S.

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-activity relation of this series of compounds, SM-309515 was found to have potent antiviral activity against wild-type and resistant HIV-1s and to possess a desirable pharmacokinetic profile in dogs.

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Application of 117918-23-7. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Search for substrate-based inhibitors fitting the S2′ space of malarial aspartic protease plasmepsin II. Author is Kiso, Aiko; Hidaka, Koushi; Kimura, Tooru; Hayashi, Yoshio; Nezami, Azin; Freire, Ernesto; Kiso, Yoshiaki.

Plasmepsin (Plm) has been identified as an important target for the development of new antimalarial drugs, since its inhibition leads to the starvation of Plasmodium falciparum. A series of substrate-based dipeptide-type Plm II inhibitors containing the hydroxymethylcarbonyl isostere as a transition-state mimic were synthesized. The general design principle was provision of a conformationally restrained hydroxyl group (corresponding to the set residue at the P2′ position in native substrates) and a bulky unit to fit the S2′ pocket.

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