Day: November 10, 2022

Wang, Xingyi published the artcileBromine-Mediated C-S Bond Formation: Synthesis of Thiazoles from α-Methylene Ketones by Using Oxone Oxidative System, SDS of cas: 90323-06-1, the main research area is ethanone methanethioamide sodium bromide catalyst one pot bromination heterocyclization; thiazole preparation.

A novel method for the synthesis of various 2,4,5-trisubstituted thiazoles from methylketones and thiourea/thioacetamide/amidinothiourea using NaBr/Oxone oxidative system was developed. The three intimately connected advantages of this method, which form a whole, are that the reaction underwent a one-pot α-bromination/cyclization process, the use of more common methylene ketones as the raw material rather than α-halomethylene ketones and a cheap and easily available catalytic amount sodium bromide as the bromine source instead of stoichiometric bromine or NBS.

ChemistrySelect published new progress about C-S bond formation. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, SDS of cas: 90323-06-1.

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

Zhao, Gang published the artcileDesign and development of some thiazole-based flavanoids as novel antibacterial against pathogens causing surgical site infection for possible benefit in bone trauma via inhibition of DNA gyrase, Safety of 4-(2-Nitrophenyl)thiazole-2-amine, the main research area is thiazole flavanoid synthesis antibacterial DNA gyrase bone trauma infection; DNA gyrase; antibacterial activity; docking; flavanoid; thiazole.

In this study, a novel class of hybrid thiazole-based flavanoid derivatives were synthesized and characterized by FT-IR, 1H-NMR, 13C-NMR, mass and elemental anal. These derivatives were evaluated for antibacterial activity for possible benefit in bone trauma via inhibition of DNA gyrase enzyme. Results suggested that compounds I, II, and III showed considerable inhibition of DNA gyrase with considerable activity against tested forty strains of Staphylococcus aureus clin. isolates. Moreover, compound I showed hydrogen bonding with LYS460 along with low binding free energy of -4.36 kcal/mol against DNA gyrase enzyme. The hemolytic activity of the potent compounds showed mild to no activity together with excellent pharmacokinetics, suggesting to have a potential for the development of designed compounds as novel antibacterial agents.

Chemical Biology & Drug Design published new progress about Antibacterial agents. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Safety of 4-(2-Nitrophenyl)thiazole-2-amine.

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

Darekar, N. R. published the artcileMicrowave Assisted Synthesis and Antibacterial Activity of New 1,3,4-Thiadiazoles and 1,2,4-Triazoles Derived from 2-{2-[2-(4-Fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetohydrazide, Recommanded Product: 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, the main research area is phenyl fluorophenyl methylthiazolyl benzoimidazolyl acetyl thiosemicarbazide preparation antibacterial; methyl phenyl fluorophenyl methylthiazolyl benzoimidazolyl triazole thiol preparation antibacterial; fluorophenyl methylthiazolyl benzoimidazolyl methyl phenyl thiadiazol amine preparation antibacterial; microwave irradiation.

A series of novel derivatives of 1-(2-{2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetyl)-4-phenylthiosemicarbazide, 5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-4-phenyl-4H-1,2,4-triazole-3-thiol and 5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-N-phenyl-1,3,4-thiadiazol-2-amine was synthesized by the conventional method as well as using MW irradiation All newly synthesized compounds were tested for antibacterial activity. Several products were demonstrated moderate activity against gram pos. and gram neg. bacterial strains.

Russian Journal of General Chemistry published new progress about Antibacterial agents. 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Recommanded Product: 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid.

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

Michaelis, Lars published the artcileStudies toward the total synthesis of sorangicins: a shortened synthesis of the dioxabicyclo[3.2.1]octane core, Name: (S)-4-Benzylthiazolidine-2-thione, the main research area is sorangicin preparation antibiotic antibacterial agent.

An access to the dioxabicyclo[3.2.1]octane core of 6-methyl-8-(3,3a,8,9,10,11,12,13,14,15,18,19,22,23,25,26,28,34a-octadecahydro-11,14,15-trihydroxy-10,38-dimethyl-28-oxo-9,13-epoxy-23,26-etheno-2,5-methano-2H,5H-furo[2,3-l][1,4,14]trioxacyclotritriacontin-25-yl)-7-nonenoic acid [i.e., (+)-sorangicin A] was developed, using a keto lactone formation, a Mukaiyama-Michael reaction and an epoxide opening as the key steps. The synthesis of the target compound was achieved using (4S)-4-(phenylmethyl)-2-thiazolidinethione as a chiral auxiliary. The title compound thus formed was (8E)-2,5:3,7-dianhydro-4,6,8,9-tetradeoxy-6-methyl-9-phenyl-L-glycero-L-gluco-non-8-enitol, (8E)-2,5:3,7-dianhydro-4,6,8,9-tetradeoxy-6-methyl-9-phenyl-L-glycero-L-gluco-non-8-enose.

Synlett published new progress about Antibacterial agents. 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Name: (S)-4-Benzylthiazolidine-2-thione.

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

Deng, Xiao-Bing published the artcileA Convenient Synthesis of Thiazolidin-2-ones from Thiazolidine-2-thiones: Antibiotic Activity and Revisiting the Mechanism, Related Products of thiazole, the main research area is thiazolidinone preparation antifungal antibacterial activity; thiazolidinethione bromoethanol reactant thiazolidinone preparation.

Various substituted thiazolidin-2-ones were synthesized from the corresponding thiazolidine-2-thiones with bromoethanol in ethanol with sodium ethoxide as a base. The optimal reaction conditions and mechanism were reinvestigated in detail. The bioassay indicated that (S)-4-iso-butylthiazolidin-2-one and (S)-4-benzylthiazolidin-2-one show certain inhibitive activities against Candida albicans and Escherichia coli.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Antibacterial agents. 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Related Products of thiazole.

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

Aitken, R. Alan published the artcileSynthesis and pyrolytic behavior of thiazolidin-2-one 1,1-dioxides, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione, the main research area is thiazolidinone dioxide preparation pyrolysis.

Four examples of chiral thiazolidin-2-one 1,1-dioxides I [R1 = PhCH2; R2 = H, PhCH2, Me2CH; R3 = H, Et; R1R2 = (CH2)3] have been prepared by reaction of the appropriate amino alcs. with CS2 in aqueous sodium hydroxide to give thiazolidine-2-thiones, followed by oxidation with KMnO4 under phase-transfer conditions in the presence of benzoic acid, either directly or via the thiazolidin-2-ones. Upon flash vacuum pyrolysis (FVP) at 650°C, I (R1 = PhCH2; R2 = H, PhCH2, Me2CH; R3 = H, Et) decompose mainly by loss of SO2 to give an alkene and benzyl isocyanate together with other products from fragmentation of the N-benzyl group. A significant minor pathway involves net loss of CO2 and water to give 2-phenyl-4,5-dihydrothiazoles together with their aromatization products. A mechanism for this new heterocyclic transformation is proposed involving initial expansion to a cyclic carbamic-sulfinic anhydride (2,1,4-oxathiazin-3-one 1-oxide).

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry published new progress about Thermal decomposition. 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione.

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

Hitchin, James R. published the artcileDevelopment and evaluation of selective, reversible LSD1 inhibitors derived from fragments, Formula: C9H7N3O2S, the main research area is LSD1 inhibitor SAR anticancer acute myeloid leukemia MAOA protein.

Two series of aminothiazoles have been developed as reversible inhibitors of lysine specific demethylase 1 (LSD1) through the expansion of a hit derived from a high concentration biochem. fragment based screen of 2466 compounds The potency of the initial fragment hit was increased 32-fold through synthesis, with one series of compounds showing clear structure-activity relationships and inhibitory activities in the range of 7 to 187 μM in a biochem. assay. This series also showed selectivity against the related FAD-dependent enzyme mono-amine oxidase A (MAO-A). Although a wide range of irreversible inhibitors of LSD1 have been reported with activities in the low nanomolar range, this work represents one of the first reported examples of a reversible small mol. inhibitor of LSD1 with clear SAR and selectivity against MAO-A, and could provide a platform for the development of more potent reversible inhibitors. Herein, we also report the use of a recently developed cell-based assay for profiling LSD1 inhibitors, and present results on our own compounds as well as a selection of recently described reversible LSD1 inhibitors.

MedChemComm published new progress about Acute myeloid leukemia. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Formula: C9H7N3O2S.

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

Yamada, S. published the artcileRegio- and stereoselective synthesis of 1,4-dihydropyridines by way of an intramolecular interaction of a thiocarbonyl or carbonyl with a pyridinium nucleus, Product Details of C10H11NS2, the main research area is pyridine regioselective stereoselective preparation; thiocarbonyl interaction pyridinium; carbonyl interaction pyridinium; stereoselective regioselective nucleophilic addition acetal organometallic pyridinium salt; absolute configuration pyridine CD.

Chiral 1,4-dihydropyridines were prepared by the regio- and stereoselective addition of ketene silyl acetals and organometallic reagents to pyridinium salts. In the addition reaction, an intramol. interaction between the thiocarbonyl or carbonyl with the pyridinium nucleus plays an important role in bringing about the selectivities. The absolute configuration of the newly produced stereogenic center of the 1,4-dihydropyridines was determined by X-ray anal. and CD Cotton effects after conversion into the appropriate derivatives The working model for the stereoselectivity was proposed based on the ab initio calculations at the RHF/3-21G* level.

Tetrahedron published new progress about Absolute configuration. 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.

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

Villa, Reymundo published the artcileStructure of FD-895 Revealed through Total Synthesis, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione, the main research area is FD895 synthesis structure antitumor.

The total synthesis of FD-895 (I) was completed through a strategy that featured the use of a tandem esterification ring-closing metathesis (RCM) process to construct the 12-membered macrolide and a modified Stille coupling to append the side chain. These studies combined with detailed anal. of all four possible C16-C17 stereoisomers were used to confirm the structure of FD-895 and identify an analog with an enhanced subnanomolar bioactivity.

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

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

Yamada, Shinji published the artcileAsymmetric Acylation of sec-Alcohols with Twisted Amides Possessing Axial Chirality Induced by the Adjacent Asymmetric Center, Quality Control of 171877-39-7, the main research area is asym acylation secondary alc twisted amide axial chirality; desymmetrization meso diols twisted amide axial chirality.

This paper reports that axially chiral twisted amides serve as asym. acylating agents for sec-alcs. under neutral conditions. Kinetic resolution of various racemic sec-alcs. and desymmetrization of 1,2-, 1,3-, and 1,4-meso-diols were performed by using the twisted amides. The utility of this desymmetrization method was shown by the preparation of the synthetic intermediate for macrolide antibiotic nodusmicin and 18-deoxynargenicin. The stereoselectivity of the acylation reactions is significantly dependent on the bulkiness of both the acyl group and the C-4 substituent of the chiral auxiliary. When an amide possessing an imidazolyl group at C-4 was employed, the stereoselectivity was reversed to give R esters. A possible working model of the acylation reaction is also described on the basis of the structural studies of the twisted amides by IR and 1H and 13C NMR spectroscopies and AM1 calculations These studies suggested a rotamer that is thermodynamically more stable than the others. This rotamer has an axial chirality about its C(O)-N linkage that is induced by the adjacent chiral center. This would enable discrimination of the two enantiomeric hydroxy groups of the racemic alcs. or meso-diols.

Journal of Organic Chemistry published new progress about Absolute configuration. 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Quality Control of 171877-39-7.

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