Tag: M.W=200-250

Yu, Jeongjae; Armstrong, Daniel W.; Ryoo, Jae Jeong published the artcile< Synthesis of new C3 symmetric amino acid- and aminoalcohol-containing chiral stationary phases and application to HPLC enantioseparations>, Quality Control of 171877-39-7, the main research area is chiral HPLC stationary phase synthesis peptide coupling amino acid; phenylglycinol phenylglycine leucine phenyl amide HPLC stationary phase silica; HPLC enantioseparation aromatic compound; (R)-phenylglycine; (S)-leucine; (S)-leucinol; C3 symmetry; HPLC; N-phenyl amide; chiral stationary phases.

We recently reported a new C3-sym. (R)-phenylglycinol N-1,3,5-benzenetricarboxylic acid-derived chiral high-performance liquid chromatog. (HPLC) stationary phase (CSP 1) that demonstrated better results as compared to a previously described N-3,5-dintrobenzoyl (DNB) (R)-phenylglycinol-derived CSP. Over a decade ago, (S)-leucinol, (R)-phenylglycine, and (S)-leucine derivatives were used as the starting materials of 3,5-DNB-based Pirkle-type CSPs for chiral separation In this study, three new C3-sym. CSPs (CSP 2, 3, and 4) were prepared by combining the ideas and results mentioned above. Here we describe the synthetic procedures and applications of the new C3-sym. CSPs (CSP 2-CSP 4).

Chirality published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Quality Control of 171877-39-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Peixoto, Philippe A.; Severin, Rene; Tseng, Chih-Chung; Chen, David Y.-K. published the artcile< Formal Asymmetric Synthesis of Echinopine A and B>, Product Details of C10H11NS2, the main research area is echinopine sesquiterpene enantioselective formal synthesis cyclization palladium catalyst; Diels Alder reaction echinopine sesquiterpene enantioselective formal synthesis.

The asym. formal synthesis of (+)-echinopines A and B was accomplished. Particularly noteworthy were the cascade construction of the [5,6,7]tricyclic ring system I (R = SiMe2CMe3) from the acyclic enyne precursor (2Z,6R,7R)-H2C:CHCH(CH2CH2CH:CH2)CH(OSiMe2CMe3)(CH2)2CH:CHCO2Me through a palladium-catalyzed cycloisomerization with subsequent intramol. Diels-Alder reaction, and the strategic application of a late-stage ring contraction of epoxy ketone II (R = SiMe2CMe3).

Angewandte Chemie, International Edition published new progress about Cyclization. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Ogretir, Cemil; Demirayak, Seref; Duran, Murat published the artcile< Spectroscopic Determination and Evaluation of Acidity Constants for Some Drug Precursor 2-Amino-4-(3- or 4-substituted phenyl) Thiazole Derivatives>, Related Products of 57493-24-0, the main research area is spectroscopic determination acidity constant drug precursor amino phenyl thiazole.

Acid dissociation constants, Ka, of eight drug precursor 2-amino-4-(3- or 4-substituted phenyl) thiazole derivatives were determined using a UV-vis spectroscopic technique. The obtained Ka values were evaluated by structure elucidation and a protonation mechanism. The obtained tautomerization equilibrium constants, KT, indicated the predominance of amino forms for all studied compounds

Journal of Chemical & Engineering Data published new progress about Bond angle, dihedral. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Related Products of 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

He, Xiao-Yang; Zou, Peng; Qiu, Jiayin; Hou, Ling; Jiang, Shibo; Liu, Shuwen; Xie, Lan published the artcile< Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors>, SDS of cas: 10574-69-3, the main research area is gp41 inhibitor HIV 1 antiviral tetrazolylphenylpyrrole preparation; pyrrole tetrazolylphenyl preparation gp41 inhibitor HIV 1 antiviral.

Based on the structure of HIV-1 gp41 binding site for small-mol. inhibitors, optimization of a lead compound resulted in the discovery of a new series of 2,5-dimethyl-3-(5-(N-phenylrhodaninyl)methylene)-N-(3-(1H-tetrazol-5-yl)phenyl)pyrrole compounds with improved anti-HIV-1 activity. The two most active compounds exhibited significant potency against gp41 6-HB formation with IC50 values of 4.4 and 4.6 μM and against HIV-1 replication in the MT-2 cells with EC50 values of 3.2 and 2.2 μM, resp., thus providing a new starting point to develop highly potent small-mol. HIV fusion inhibitors targeting gp41.

Bioorganic & Medicinal Chemistry published new progress about AIDS (disease). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Powers, Jay P.; Piper, Derek E.; Li, Yang; Mayorga, Veronica; Anzola, John; Chen, James M.; Jaen, Juan C.; Lee, Gary; Liu, Jinqian; Peterson, M. Greg; Tonn, George R.; Ye, Qiuping; Walker, Nigel P. C.; Wang, Zhulun published the artcile< SAR and Mode of Action of Novel Non-Nucleoside Inhibitors of Hepatitis C NS5b RNA Polymerase>, Related Products of 10574-69-3, the main research area is nonnucleoside inhibitor thioxothiazolidine aryl derivative hepatitis C NS5b polymerase.

Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with sub-micromolar biochem. potency have been identified which are selective for the inhibition of HCV NS5b over other polymerases. The structures of the complexes formed between several of these inhibitors and HCV NS5b were determined by x-ray crystallog., and the inhibitors were found to bind in an allosteric binding site sep. from the active site. Structure-activity relationships and structural studies have identified the mechanism of action for compounds in this series, several of which possess drug-like properties, as unique, reversible, covalent inhibitors of HCV NS5b.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Related Products of 10574-69-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Robertson, Mark J.; Hadzic, Gordana; Ambrus, Joseph; Pome, D. Yuri; Hyde, Emily; Whiting, Ainslie; Mariana, Anna; von Kleist, Lisa; Chau, Ngoc; Haucke, Volker; Robinson, Phillip J.; McCluskey, Adam published the artcile< The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity>, Related Products of 10574-69-3, the main research area is dynamin GTPase inhibitor rhodanine analog preparation SAR; Knoevengal condensation; dynamin inhibition; rhodanine.

Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn series among the most active dynamin inhibitors reported. Two analogs were highly effective at blocking receptor-mediated endocytosis: C10 and D10 (I) with IC50(RME) = 7.0 ± 2.2 and 5.9 ± 1.0 μM, resp. These compounds are equipotent with the best reported in-cell dynamin inhibitors.

ACS Medicinal Chemistry Letters published new progress about Drug targets (endocytosis). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Related Products of 10574-69-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Huang, Gaochao; Shrestha, Ruben; Jia, Kaimin; Geisbrecht, Brian V.; Li, Ping published the artcile< Enantioselective Synthesis of Dilignol Model Compounds and Their Stereodiscrimination Study with a Dye-Decolorizing Peroxidase>, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione, the main research area is dilignol model compound enantioselective preparation surface plasmon resonance TcDyP.

A four-step enantioselective approach was developed to synthesize anti (1R,2S)-I and (1S,2R)-I containing a β-O-4 linkage in good yields. A significant difference was observed for the apparent binding affinities of four stereospecific lignin model compounds with TcDyP by surface plasmon resonance, which was not translated into a significant difference in enzyme activities. The discrepancy may be attributed to the conformational change involving a loop widely present in DyPs upon H2O2 binding.

Organic Letters published new progress about Diastereoselective synthesis. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sanichar, Randy; Carroll, Ciaran; Kimmis, Ryan; Reiz, Bela; Vederas, John C. published the artcile< Dess-Martin periodinane oxidative rearrangement for preparation of α-keto thioesters>, Application In Synthesis of 171877-39-7, the main research area is Dess Martin periodinane oxidative rearrangement alpha keto thioester preparation; keto thioester preparation oxidation beta hydroxy thioester.

A Dess-Martin Periodinane (DMP) mediated oxidative rearrangement reaction was uncovered. The reaction proceeds via oxidation of a β-hydroxy thioester to a β-keto thioester, followed by an α-hydroxylation and then further oxidation to form a vicinal thioester tricarbonyl. This product then rearranges, extruding CO2, to form an α-keto product. The mechanism of the rearrangement was elucidated using 13C labeling and anal. of the intermediates as well as the products of the reaction. This efficient process allows for easy preparation of α-keto thioesters which are potential intermediates in the synthesis of pharmaceutically important heterocyclic scaffolds such as quinoxalinones.

Organic & Biomolecular Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Application In Synthesis of 171877-39-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Akbarzadeh, Elaheh; Shockravi, Abbas; Vatanpour, Vahid published the artcile< High performance compatible thiazole-based polymeric blend cellulose acetate membrane as selective CO2 absorbent and molecular sieve>, Synthetic Route of 57493-24-0, the main research area is thiazole cellulose acetate polymeric blend membrane selective absorption property; CO(2) capture; Cellulose acetate (CA); Gas separation; Permeation; Polymeric blend membrane; Thiazole.

Green blend membranes comprise of high thermal resistance ortho-linked thiazole-based polyimine (PM-4) including thioether linkage were fabricated in combination of glassy cellulose acetate (CA). The thermal stabilities of PMs were examined using thermogravimetric anal. and differential scanning calorimetry. Morphol. aspects and functional groups of the membranes were investigated via field emission SEM and Fourier transform IR spectroscopy-attenuated total reflectance anal. resp. X-ray diffraction and mech. strength were determined as well. The effects of polyimine content, pressure and temperature were studied on CO2 permeability (P) and selectivity. The pressure changes revealed exponentially increases on CO2 permeability by plasticization, facilitated transfer and solution-diffusion mechanisms, but decreases on CH4 and N2 permeations. Remarkable permeation (P = 3000 Barrer) of CA/PM-4 (1:3% weight/weight) and ideal selectivity ratios of CO2/N2 = 59, CO2/CH4 = 33.7 were obtained at 3 bar and 35°C vs. neat CA membrane.

Carbohydrate Polymers published new progress about Absorbents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Synthetic Route of 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Nagaladinne, Nizamuddin; Abdul Ahad, Hindustan; Nayakanti, Devanna published the artcile< Design, synthesis and molecular modelling studies of 1-methyl-3-(4-substituted phenyl-1,3- thiazol-2-yl)-2-(pyridin-3-yl)-2,3-dihydroquinazolin-4(1H)-ones as potent anticancer agents>, Product Details of C9H7N3O2S, the main research area is methyl phenyl thiazolyl pyridinyl dihydroquinazolinone preparation antitumor SAR ADMET; mol modeling methyl phenyl thiazolyl pyridinyl dihydroquinazolinone preparation.

The present study involved the design, synthesis, characterization and mol. docking studies of biol. active 1-methyl-3-(4-substituted phenyl-1,3-thiazol-2-yl)-2-(pyridin-3-yl)-2,3-dihydroquinazoline-4-(1H)-ones I [R = 2-OH, 3-NH2, 4-Cl, etc.] which were synthesized by condensation of 2-amino-4-substituted phenylthiazoles with N-methylbenzoxazin-4-one. The N-methylbenzoxazin-4-one and 2-amino-4-substituted phenylthiazoles were synthesized from N-methylanthranilic acid with pyridine3-carboxylic acid and substituted aldehydes with thiourea, resp. The ADME properties determined the synthetic accessibility of compounds I by in silico Swiss ADME. The colorectal anticancer screening of compounds I was done by using cell HT-29 human colorectal adenocarcinoma based on mol. docking studies on 3GC7-the structure of p38alpha in complex with dihydroquinazolinone. Finally, compounds I [R = 4-Me, 3-NH2, 2,4-(OH)2, 2,4-(Cl)2] exhibited better activity at a concentration < 10μg/mL when compared to 5-fluorouracil. The ADME properties revealed that all the compounds I were within the range and docking studies showed the highest binding with glide score -7.19 and -7.027 Kcal/mol compared to the target protein -10.67 Kcal/mol. Asian Journal of Chemistry published new progress about Antitumor agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Product Details of C9H7N3O2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica