Category: 90323-06-1

Breinholt, Jens published the artcileSynthesis of 2-amino-4H-thiazolo[5,4-b]indole and characterization of its colored conversion products with protein tyrosine phosphatase inhibitory activity, Category: thiazole, the main research area is thiazoloindolamine preparation reaction; protein tyrosine phosphatase inhibitor thiazoloindolamine reaction product.

In DMSO solution 2-amino-4H-thiazolo[5,4-b]indole (I) is converted to a complex mixture of colored products. The three major conversion end products, two of which are inhibitors of protein tyrosine phosphatases, were isolated by chromatog. methods and their structures characterized by spectroscopic anal., including NMR and MS combined with computer assisted structure elucidation, and, finally, confirmed by independent chem. synthesis. Synthesis of I as well as its N-acetyl derivatives from either oxindole or 2-bromo-1-(2-nitrophenyl)ethanone is described.

Journal of Heterocyclic Chemistry published new progress about thiazoloindolamine preparation reaction; protein tyrosine phosphatase inhibitor thiazoloindolamine reaction product. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Category: thiazole.

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

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

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

Yan, Gang published the artcile2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies, Product Details of C9H7N3O2S, the main research area is thiazolyl imidazolyl acetamide preparation mol docking BACE1 inhibitor human; Alzheimer’s disease; BACE-1 inhibitors; BBB; Docking study; PAMPA; Permeability; Surface Plasmon Resonance (SPR).

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives, I (R1 = Ph, 4-MeC6H4, 2-O2NC6H4, etc.; R2 = 2-MeOC6H4,3-MeOC6H4, 4-MeOC6H4, 3-EtOC6H4), II (R3 = Ph, 3,5-Cl2-4-NH2Ph; R4 = 3-MeOPh, 3-EtOPh), were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biol. evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog II (R3 = Ph; R4 = 3-EtOC6H4) (IC50 = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization.

European Journal of Medicinal Chemistry published new progress about Alzheimer disease. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Product Details of C9H7N3O2S.

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

Kozikowski, Alan P. published the artcileChemistry, biology, and QSAR studies of substituted biaryl hydroxamates and mercaptoacetamides as HDAC inhibitors-nanomolar-potency inhibitors of pancreatic cancer cell growth, Name: 4-(2-Nitrophenyl)thiazole-2-amine, 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. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Name: 4-(2-Nitrophenyl)thiazole-2-amine.

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

Jiang, Cheng published the artcileDesign of novel thiazole bearing pyrazole derivatives and their dual activities as ACE inhibitors and calcium channel blockers in cardiovascular disease, Product Details of C9H7N3O2S, the main research area is cardiovascular disease thiazole pyrazole derivative ACE inhibitor calcium channel.

In an attempt to develop drugs for cardio-vascular disease, present manuscript deal with the development of dual acting agents targeting angiotensin converting enzyme (ACE) and calcium channel to treat hypertension. These mols. were developed via efficient multi-step synthetic route in excellent yield. In ACE inhibitors assay, these compounds showed considerable percentage of inhibition (32-94 %) with IC50 = 1.2 and 1.5 μM for most promising compound 6e and 6o, resp. In mol. docking study with ACE, compound 6e revealed similar fashion of mol. interaction with catalytic residues His353, Ala 354, Tyr 523, Tyr 520, and Glu 152, comparable with standard lisinopril. Addnl., in rat aortic strip model, these mols. significantly induce vasorelaxation via inhibiting Ca2+ channel in dose dependent manner.

Latin American Journal of Pharmacy published new progress about Angiotensin-converting enzyme inhibitors. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Product Details of C9H7N3O2S.

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

Ohkubo, Mitsuru published the artcileStudies on cerebral protective agents. VIII. Synthesis of 2-aminothiazoles and 2-thiazolecarboxamides with anti-anoxic activity, Quality Control of 90323-06-1, the main research area is antianoxic aminothiazole thiazolecarboxamide structure cerebral protection; aminothiazole preparation antianoxic cerebral protection structure; thiazolecarboxamide preparation antianoxic cerebral protection structure.

Various 2-aminothiazoles and 2-thiazolecarboxamides, possessing a nitrogenous basic moiety at the C-2 position of the thiazole ring, were prepared and tested for anti-anoxic (AA) activity in mice. Among them, N-[2-(4-morpholinyl)ethyl]-4-(3-trifluoromethylphenyl)-2-thiazolecarboxyamide hydrochloride (FR108143) (min. EDs of 3.2 mg/kg i.p. and 10 mg/kg p.o., resp.) exhibited more potent AA activity than either FK360 or FR75039, each of which has a nitrogenous basic moiety at the C-5 position. The structure-activity relationships with regard to AA activity of this series of compounds are discussed, and the three-dimensional electrostatic potentials (3D-MEP) around the basic nitrogen atom of FK360 and the thiazole derivative (FR108143) are compared.

Chemical & Pharmaceutical Bulletin published new progress about Electrostatic potential. 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Quality Control of 90323-06-1.

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

Buchstaller, Hans-Peter published the artcileParallel solution-phase synthesis of a 2-aminothiazole library including fully automated work-up, Recommanded Product: 4-(2-Nitrophenyl)thiazole-2-amine, the main research area is thiazole thiazolamine preparation chem library.

A straightforward and effective procedure for a solution phase preparation of a 2-aminothiazole combinatorial library is described. The synthesis of the target compounds was achieved by a reaction, work-up and isolation of these thiazolamine derivatives as free bases by a fully automated method using the Chemspeed ASW 2000 automated synthesizer. The compounds were obtained in good yields and excellent purity without any further purification requirements.

Combinatorial Chemistry & High Throughput Screening published new progress about Amines Role: SPN (Synthetic Preparation), PREP (Preparation). 90323-06-1 belongs to class thiazole, name is 4-(2-Nitrophenyl)thiazole-2-amine, and the molecular formula is C9H7N3O2S, Recommanded Product: 4-(2-Nitrophenyl)thiazole-2-amine.

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