Category: 57493-24-0

Bansal, Akhil; Bali, Alka; Balaini, Ajitesh published the artcile< Synthesis and Evaluation of Substituted Aryl Thiazoles With Antioxidant Potential as Gastro-sparing Anti-inflammatory Agents>, COA of Formula: C9H7N3O2S, the main research area is antioxidant potential gastro sparing antiinflammatory agent aryl thiazole.

NSAIDs are used as first-line drugs for the treatment of various inflammatory disorders. Chronic use of NSAIDs is known to be associated with gastrointestinal and renal toxicity. Local generation of reactive oxygen species finally resulting in cellular apoptosis is one of the accepted mechanisms for NSAID-induced toxicity. The objective of the present study was to design and synthesize a series of 2-methane sulfonamido substituted arylthiazole derivatives by including structural features of combined antiulcer and anti-inflammatory activity utilizing as the structural core, thiazole nucleus with potential for antioxidant effect. Compounds were designed based on three dimensional and field similarity studies. The synthesized compounds were evaluated for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Rofecoxib and indomethacin were taken as standard drugs for comparison. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. The compounds 6 and 7 showed good anti-inflammatory activity comparable to the standard group and were also non ulcerogenic at the test doses. Compounds 1-7 displayed varying degrees of reducing power in the (PFRAP) assay and the methanesulfonamido derivatives 4-7 showed the highest antioxidant activity (EC50 values 3.7-5.1 μmol/mL vs ascorbic acid 7.4 μmol/mL). Theor. ADME profiling of the compounds based on selected physicochem. properties showed excellent compliance with Lipinski′s rule. A series of compounds have been designed and synthesized having dual antioxidant and anti-inflammatory activity with activities comparable to standard drugs.

Letters in Drug Design & Discovery published new progress about Anti-inflammatory 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

Qi, Qingqing; Shen, Qilong; Lu, Long published the artcile< Polyfluoroalkylation of 2-aminothiazoles>, Product Details of C9H7N3O2S, the main research area is thiazolamine polyfluoroalkylation.

An efficient, highly selective method for polyfluoroalkylation of 2-aminothiazole derivatives is described. Interestingly, defluorinated 2-amino-5-(1,1,1,3,3,3-hexafluoroprop-2-yl)thiazole derivative was obtained in moderate yields when 2-aminothiazole was reacted with (CF3)2CFI.

Journal of Fluorine Chemistry published new progress about Fluoroalkylation. 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

Rezania, Hamidreza published the artcile< Synthesis and characterization of novel functional hyperbranched polyamides from AB2 units: effect of extra functional groups>, Name: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is hyperbranched polyamide preparation thermal property; Novel AB2 monomers; functional groups; hyperbranched polymers; polyamide.

Hyperbranched polymers (HPs), which in terms of structure may be compared to the branching structure of trees, are referred to as tree-like materials, but role of leave in these tree-like polymers is neglected and much attention has only been paid to their branches. In fact, functional groups in these polymers play a vital role the same as the role of leaves in trees. Therefore, in this paper, an attempt has been made to design and synthesize three AB2 monomers containing extra hydroxyl and nitro groups. The benefits of their presence in the structure of produced hyperbranched polyamides (HPs) are investigated. The polymer structure was characterized by FT-IR and 1 H NMR. The solubility of synthesized HPs was studied in different protic and aprotic solvents. The thermal stability of the prepared HPs was investigated by thermogravimetric and differential scanning calorimetric analyses. The photoluminescent properties of the HPs were also investigated.

Designed Monomers and Polymers published new progress about Branched polymers Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 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

Yan, Gang; Hao, Lina; Niu, Yan; Huang, Wenjie; Wang, Wei; Xu, Fengrong; Liang, Lei; Wang, Chao; Jin, Hongwei; Xu, Ping published the artcile< 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies>, Application In Synthesis of 57493-24-0, 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. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application In Synthesis of 57493-24-0.

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

Raut, D. G.; Sonawane, K. D.; Jadhav, S. Y.; Sonawane, V. D.; Jadhav, D. B.; Dhanavade, M. J.; Bhosale, R. B. published the artcile< Synthesis and potential antibacterial activities of 2-chloro-N-(4-phenylthiazol-2-yl)acetamide derivatives>, Category: thiazole, the main research area is phenylthiazolyl chloroacetamide preparation antibacterial.

A series of substituted 2-chloro-N-(4-phenylthiazol-2-yl)acetamide derivatives I [R = H, 4-OMe, 3-NO2, 2,4-Cl2, etc.] were synthesized via condensation between 4-(substituted phenyl)-2-aminothiazoles with chloroacetyl chloride. The synthesized compounds were evaluated for antibacterial activity at three concentrations (25 μg/mL, 50 μg/mL and 100 μg/mL) and results were expressed in terms of zone of inhibition in millimeters by agar well diffusion method using Ampicillin 1mg/mL as reference standard drug. Among the tested compounds, compounds I [R = H, 4-OMe, 2,4-Cl2] showed the potent antibacterial activity against Gram pos. bacteria Bacillus subtilis and Gram neg. bacteria Salmonella typhimurium.

Pharma Chemica published new progress about Acetamides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Category: thiazole.

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

Jiang, Cheng; Yuan, Zhi; Wang, Ju-Fei; Fu, Jie; Jiang, Guang-Jun; Zheng, Liang-Rong published the artcile< Design of novel thiazole bearing pyrazole derivatives and their dual activities as ACE inhibitors and calcium channel blockers in cardiovascular disease>, Electric Literature of 57493-24-0, 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. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Electric Literature of 57493-24-0.

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

Hitchin, James R.; Blagg, Julian; Burke, Rosemary; Burns, Samantha; Cockerill, Mark J.; Fairweather, Emma E.; Hutton, Colin; Jordan, Allan M.; McAndrew, Craig; Mirza, Amin; Mould, Daniel; Thomson, Graeme J.; Waddell, Ian; Ogilvie, Donald J. published the artcile< Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments>, Quality Control of 57493-24-0, 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. 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

Liang, Xiao-Ping; Luo, Min; Kang, Li; Tang, Long-Xing; Liang, Qing; Liu, Yuan-Lin; Yang, Zi; Zhang, Chun-Tao; Peng, Cai-Yun; Fu, Rong-Geng published the artcile< Facile one-pot three-component strategy for the synthesis of 2-amino-4-arylthiazoles via elemental sulfur source>, Application of C9H7N3O2S, the main research area is amino arylthiazole preparation green chem; aryl methyl ketone sulfur cyanamide three component cascade.

A novel and facile metal-free method for the green synthesis of 2-amino-4-arylthiazole derivatives I (Ar = 3-nitrophenyl, 2-naphthyl, pyridin-4-yl, etc.) through the three-component cascade reaction of aromatic Me ketones ArC(O)Me, elemental sulfur and cyanamide is reported. One C-N bond and two C-S bonds were formed in one-pot protocol without using catalysts.

Tetrahedron Letters published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application of C9H7N3O2S.

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

Banerjee, Janmajoy; Mariappan, G.; Nepal, Aswini Kumar; Dahal, Prassana; Khanal, Hemanta published the artcile< Conventional methods of synthesis of novel amino(phenyl)thiazoles and their antibacterial and local anesthetics screening>, Synthetic Route of 57493-24-0, the main research area is acetamide thiazolylamino preparation anesthetic antibacterial.

Cyclocondensation of thiourea and substituted acetophenones RCOMe [R = Ph, 3-O2NC6H4, 4-O2NC6H4, 4-MeOC6H4, 2,5-(MeO)2C6H3] led to the formation of the corresponding 2-amino-4-R-thiazoles, which on further reaction with N-Ph 2-chloroacetamide gave N-Ph (thiazolylamino)acetamides I. The synthesized compounds I were investigated for their antibacterial activity by cup plate method against four bacterial strains. All the synthesized compounds exhibited mild to good antibacterial activities with I [R = 2,5-(MeO)2C6H3] showing promising activity against all strains of bacteria. The compounds I were also screened for local anesthetics activity taking lidocaine as standard, and all the compounds showed moderate activities.

International Journal of Pharmacy and Technology published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Tapadar, Subhasish; He, Rong; Luchini, Doris N.; Billadeau, Daniel D.; Kozikowski, Alan P. published the artcile< Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is histone deacetylase inhibitor preparation isoxazole moiety linker antitumor.

A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micromolar inhibitory activity against five pancreatic cancer cell lines.

Bioorganic & Medicinal Chemistry Letters 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