Tag: M.W=200-250

Lakhan, R.; Rai, B. J. published the artcile< Local anesthetics. IV. Synthesis and activity of 2-(N-substituted or N,N-disubstituted aminoacetamido)-4- or -4,5-substituted thiazoles>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is local anesthetic aminoacetamidothiazole preparation; thiazole aminoacetamido anesthetic preparation.

I (R = H or Me, R1 and R2 = H or alkyl or NR1R2 = morpholino, R3 = H or m- or p-O2N) were prepared by treatment of the appropriate 2-chloroacetamidothiazole derivative with an appropriate amine. I(R = H, R1 = R2 = iso-Pr, R3 = m-O2N) [105602-34-4] and I (R = Me, R1 = R2 = Pr, R3 = H) [105602-33-3] (as HCl salt) were the most potent local onesthetics in comparison with procaine-HCl. All other I required a similar time n producing onset of anesthesia as procaine.

Farmaco, Edizione Scientifica published new progress about Local anesthetics. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Safety of 2-Amino-4-(3-nitrophenyl)thiazole.

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

Kearney, Patrick C.; Fernandez, Monica; Flygare, John A. published the artcile< Traceless Solid-Phase Synthesis of 2-Aminothiazoles>, Synthetic Route of 57493-24-0, the main research area is thiazolamine derivative preparation solid phase; ketone bromo cyclocondensation resin bound thiourea.

2-Aminothiazoles are produced under mild conditions in good yields and with high degrees of purity from a primary amine and an α-bromo ketone. The key to this method is the conversion of a resin-bound amino group to a thiourea using Fmoc-NCS.

Journal of Organic Chemistry published new progress about Cyclocondensation reaction. 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

Dutta, Satyajit; Mariappan, G.; Asada, R. K.; Bhuyan, N. R.; Mohanty, J. P. published the artcile< Synthesis and antimicrobial evaluation of aminophenylthiazole derivatives>, COA of Formula: C9H7N3O2S, the main research area is acetophenone thiourea cyclocondensation; amino aryl thiazole preparation antibacterial antifungal.

A new series of 2-aminophenylthiazole derivatives was synthesized and structures were confirmed on the basis of IR, 1H-NMR spectroscopic data. The compounds were screened for antimicrobial activity in vitro by Kirby-Bauer disk diffusion method and the compounds 2-amino-4-(3-nitro/4-chlorophenyl)phenylthiazoles showed promising activity.

Pharma Chemica published new progress about Antibacterial agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, COA of Formula: C9H7N3O2S.

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

Muthyala, Manoj Kumar; Kumar, Anil published the artcile< A novel and efficient one pot synthesis of 2,4-disubstituted thiazoles and oxazoles using phenyltrimethylammonium tribromide in ionic liquid>, COA of Formula: C9H7N3O2S, the main research area is amide ketone cyclization phenylmethylammonium tribromide ionic liquid; urea ketone cyclization phenylmethylammonium tribromide ionic liquid; oxazole green preparation; thiazole green preparation.

A novel and efficient 1-pot procedure was described for synthesis of 2,4-disubstituted thiazoles and oxazoles from substituted ketones using phenyltrimethylammonium tribromide as in-situ brominating agent followed by reaction with thioamide/thiourea and amides/ureas, resp. in [bmim][BF4] ionic liquid The advantages of the procedure include avoiding the handling of lacrymetric compounds and hazardous and toxic organic solvents along with good to excellent yields of the products.

Journal of Heterocyclic Chemistry published new progress about Cyclization. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, COA of Formula: C9H7N3O2S.

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

Sparrow, Kevin John; Carley, Sarah; Sohnel, Tilo; Barker, David; Brimble, Margaret A. published the artcile< Studies towards development of asymmetric double-Mannich reactions of chiral 2-oxocyclohexanecarboxylate derivatives with bis(aminol)ethers>, Related Products of 171877-39-7, the main research area is azabicyclooctanecarboxylic acid imide ester preparation; nonracemic oxazolidinone imide ester oxocyclohexanecarboxylic acid preparation Mannich reaction; erbium lanthanum catalyst double Mannich reaction oxocyclohexanecarboxylate aminol ether; double Mannich reaction nonracemic oxazolidinone imide ester oxocyclohexanecarboxylic acid; azabicyclooctanecarbonyl methylphenyloxazolidinone mol crystal structure.

An improved method for the double-Mannich reaction of β-ketoesters and bis(aminol)ethers (EtOCH2)2NR (R = Et, PhCH2) in the presence of Er(OTf)3 or La(OTf)3 was developed. Esters of 2-oxocyclohexanecarboxylic acid with 8-phenylmenthol, pantolactone, and trans-2-phenylcyclohexanol and imides with norephedrine-, (S)-phenylalaninol-, and (S)-α,α-diphenylvalinol-derived oxazolidinones and oxazolidinethiones were prepared Double Mannich reaction of EtN(CH2OEt)2 with the oxocyclohexanecarboxylic acid esters and imides yielded mixtures of azabicyclooctanecarboxylic acid ester and imide diastereomers. The oxocyclohexanecarboxylic acid imide with a norephedrine-derived oxazolidinone and its derived azabicyclooctanecarboxylic acid imide product were separated into their diastereomers; the structures of both reactant imide diastereomers and the major azabicyclooctanecarboxylic acid imide diastereomer were assigned by X-ray crystallog.

Tetrahedron published new progress about Chiral auxiliary. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Related Products of 171877-39-7.

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

Kozikowski, Alan P.; Chen, Yufeng; Gaysin, Arsen M.; Savoy, Doris N.; Billadeau, Daniel D.; Kim, Ki Hwan published the artcile< Chemistry, biology, and QSAR studies of substituted biaryl hydroxamates and mercaptoacetamides as HDAC inhibitors-nanomolar-potency inhibitors of pancreatic cancer cell growth>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is histone deacetylase inhibitor biaryl hydroxamate mercaptoacetamide preparation QSAR; pancreatic cancer inhibitor biaryl hydroxamate mercaptoacetamide preparation QSA.

The histone deacetylases (HDACs) are able to regulate gene expression, and inhibitors of the HDACs (HDACIs) hold promise in the treatment of cancer as well as a variety of neurodegenerative diseases. To investigate the potential for isoform selectivity in the inhibition of HDACs, we prepared a small series of 2,4′-diaminobiphenyl ligands functionalized at the para-amino group with an appendage containing either a hydroxamate or a mercaptoacetamide group and coupled to an amino acid residue at the ortho-amino group. A smaller series of substituted phenylthiazoles was also explored. Some of these newly synthesized ligands show low-nanomolar potency in HDAC inhibition assays and display micromolar to low-nanomolar IC50 values in tests against five pancreatic cancer cell lines. The isoform selectivity of these ligands for class I HDACs (HDAC1-3 and 8) and class IIb HDACs (HDAC6 and 10) together with QSAR studies of their correlation with lipophilicity are presented. Of particular interest is the selectivity of the mercaptoacetamides for HDAC6.

ChemMedChem published new progress about Antitumor agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Uppal, Archana; Kothiyal, Preeti; Singh, Anita published the artcile< Hybrid Class Phenylthiazole and 1,2,3,4-Tetrahydronaphthalene Target Sertraline Transporter for Antidepressant Action Revealed by Molecular Docking Studies>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is phenylthiazolyltetrahydronaphthalene derivative preparation antidepressant activity; epoxytetrahydronaphthalene preparation amine addition.

Phenylthiazolyl-substituted 1,2,3,4-tetrahydronaphthalene derivatives e. g., I, were synthesized, and their chem. structures were elucidated by Fourier transform IR, 1H-NMR, 13C-NMR spectral data and elemental analyses. Antidepressant-like activities of these compounds were screened using both Porsolt’s behavioral despair on albino mice and tail suspension tests. Open field test was also performed for the examination of probable neurol. deficits, which may interfere with the test results. The test compounds exhibited different levels of antidepressant activities. Addnl., the key ligand was further substantiated by docking experiment to explore plausible mode of binding in mol. dynamics overflow. The studies elucidates role of a hydrophilic H-bonding region and pi-cation binding as a major driving force for biol. activity.

Journal of Heterocyclic Chemistry published new progress about Addition reaction. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Rezania, Jafar; Behzadi, Hadi; Shockravi, Abbas; Ehsani, Morteza; Akbarzadeh, Elahe published the artcile< Synthesis and DFT calculations of some 2-aminothiazoles>, Name: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is aminothiazole preparation green chem DFT calculation; ketone aryl thiourea cyclization iodine catalyst.

A series of 2-aminothiazole derivatives I (R = C6H5, 3-pyridyl, 3-O2NC6H4, etc.) has been synthesized by the reaction of acetyl compounds RC(O)CH3 with thiourea and iodine as catalyst under solvent-free condition, a green chem. method. The quantum chem. calculations at the DFT/B3LYP level of theory in gas phase were carried out for starting acetyl derivatives The HOMO and LUMO and related reactivity descriptor of acetyl derivatives, as well as, enthalpy of reactions are calculated in order to investigate the reaction properties of acetyl compounds and yields of the reactions. The calculated reactivity descriptors are well correlated to activity of different acetyl derivatives

Journal of Molecular Structure published new progress about Alkyl aryl ketones Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Name: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Al-Shamkhani, Zeki A. Naser; Al-Hazam, Hanan A. published the artcile< Microwave Assisted Synthesis, Characterizations and Antibacterial Activity of Some of Thiazole Derivatives>, Quality Control of 57493-24-0, the main research area is thiazole amino preparation antibacterial microwave.

A series of substituted 2-amino thiazole compounds I (R = H, 4-OH, 2-F, etc.) were synthesized by reaction of substituted acetophenone with thiourea and iodine in microwave oven. The biol. screening data of the synthesized compounds I were also studied.

Research Journal of Pharmaceutical, Biological and Chemical Sciences published new progress about Antibacterial agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Quality Control of 57493-24-0.

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

Kosaki, Yusuke; Ogawa, Narihito; Wang, Qian; Kobayashi, Yuichi published the artcile< Synthesis of Coronafacic Acid via TBAF-Assisted Elimination of the Mesylate and Its Conversion to the Isoleucine Conjugate>, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione, the main research area is coronafacic acid preparation quaternary ammonium fluoride elimination mesylate; isoleucine conjugate coronafacic acid preparation.

An aldol reaction followed by elimination of the derived mesylate was used to construct the side chain that was designed to afford the cyclohexene ring of coronafacic acid via intramol. alkylation. Elimination of the mesylate proceeded with TBAF. The alkylation was achieved with t-BuOK in THF, and then hydrolysis afforded coronafacic acid, which upon condensation with unprotected L-isoleucine using ClCO2Bui furnished coronafacoyl-L-isoleucine, the L-Ile conjugate.

Organic Letters published new progress about Aldol addition. 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