Tag: M.W=200-250

Uppal, Archana; Singh, Anita; Kothiyal, Preeti published the artcile< Structure-based design, synthesis and antidepressant-like activity of phenylthiazolyl-1H,2H,3H,4H-naphthalene derivatives>, Related Products of 57493-24-0, the main research area is aryl thiazolyl amino tetrahydronaphthalene preparation mol docking antidepressant.

A series of new [aryl(thiazolyl)]aminotetrahydronaphthalene derivatives I [R1 = H, OMe, Cl; R2 = H, Me; R3 = 4-CH3, 3,4-di-Cl, 4-Br, etc.] were synthesized and studied for their mol. docking properties via in silico assay in CHARMm-based CDocker program. Results indicated that these compounds showed interactions towards serotonin transporters. All the titled compounds were evaluated for antidepressant activity by forced-swimming test, tail suspention test and open-field test on albino mice and acute toxicity of compounds I [R1 = OMe; R2 = H; R3 = 4-NHC(O)CH3, 3-NO2] were also studied. Antidepressant-like effect in mice tests revealed that the most active compounds were I [R1 = OMe; R2 = H; R3 = 4-NHC(O)CH3, 3-NO2] with no any toxicity.

Asian Journal of Chemistry published new progress about Antidepressants. 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

Yadav, Jhillu S.; Kumar, Veerjala Naveen; Rao, Ramisetti Srinivasa; Srihari, Pabbaraja published the artcile< A concise stereoselective total synthesis of herbarumin III>, Computed Properties of 171877-39-7, the main research area is herbarumin III asym total synthesis.

A stereoselective total synthesis of the phytotoxic compound herbarumin III was achieved by utilizing Crimmins’ aldol approach, 1,3-syn asym. reduction, and an olefin metathesis reaction as the key steps.

Synthesis published new progress about Aldol addition (stereoselective). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Computed Properties of 171877-39-7.

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

Nizamuddin, Nd; Abdul ahad, Hindustan; Devanna, Nayakanti published the artcile< Molecular docking studies of N-methyl- 2, 3 -disubstituted quinazolin-4-ones scaffold>, SDS of cas: 57493-24-0, the main research area is methyl disubstituted quinazolinone scaffold mol docking.

In recent days, synthesis of anticancer mols. having both low adverse effects and specific protein targeting are seldom. Synthesis of anticancer mols. having both low adverse effects and specific protein targeting is challenging. The main objective of our study was to develop mols. that can target activated protein kinase P38 alpha and activin receptor (ALK2) kinase for treating carcinoma. P38 alpha is involved in cell differentiation, apoptosis, and autophagy. Activin receptor (ALK2) kinase is responsible for mutations of cancerous cells. The synthesis of N-Me – 2, 3 -Disubstituted Quinazolin-4-Ones was carried out by refluxing of 1-methyl-2-(pyridinyl)-1,2-dihydro-4H-3,1-benzoxazin-4-one with 4-substituted phenyl-1,3-thiazol-2-amines. The mol. docking of 1-methyl-3-(4-substituted phenyl-1,3-thiazol-2-yl)-2-(pyridin-3-yl)-2,3-dihydroquinazolin-4(1H)-one (5Da1-5Dk11) and 1-methyl-3-(4-substituted phenyl-1,3-thiazol-2-yl)-2-(pyridin-4-yl)-2,3-dihydroquinazolin-4(1H)-one (5Ea1-5Ek11) derivatives were carried out using Schrodinger Glide (version 2020_1) software. Twenty-two quinazoline-4-one derivatives were docked into selective P38 alpha and ACVR1 (ALK2) kinase with PDB code 3GC7, 6GI6. Based on the docking score, comparison between quinazolin-4-one derivatives, co-crystallized Ligands interaction was evaluated using 5-Fluorouracil as standard Best activity was found in compounds 5Df6, 5Dd4, 5Ed4 and 5Ef6 with ACVR1 (ALK2) kinase with score of -8.223, -7.936, -8.123, -7.907 and 5Df6, 5Dh8, 5Eb2 and 5Ee5 with P38alpha with score of -7.19, -7.027, -6.698, -6.789 Kcal/mol against enzymes responsible for treatment for cancer compare with reference drug score -5.765 and -6.195. This study will help in the design and development of a drug that gives room for the synthesis of a new selective ACVR1 (ALK2) kinase and P38alpha enzyme inhibitor with predetermined affinity and activity of the compound

International Journal of Life Science and Pharma Research published new progress about Activin receptor ACVRLK2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, SDS of cas: 57493-24-0.

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

Cochrane, Stephen A.; Surgenor, Richard R.; Khey, Kevin M. W.; Vederas, John C. published the artcile< Total Synthesis and Stereochemical Assignment of the Antimicrobial Lipopeptide Cerexin A1>, Reference of 171877-39-7, the main research area is cerexin antimicrobial lipopeptide isolation total synthesis stereochem antibacterial.

The isolation and total synthesis of the antimicrobial lipopeptide cerexin A1 is reported. This synthesis includes the preparation of orthogonally protected γ-hydroxylysine, utilizing a nitrile Reformatsky-type reaction as a key step to yield both diastereomers more efficiently than previously reported methods. The configuration of the β-hydroxyl in the lipid tail was determined by the use of a modified Ohrui-Akasaka approach. Furthermore, new cerexin analogs from Bacillus mycoides ATCC 21929 were isolated and characterized, revealing an ε-amino succinylation of a hydroxylysine residue that is unusual in a nonribosomal peptide synthetase product.

Organic Letters published new progress about Absolute configuration. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Reference of 171877-39-7.

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

Lu, Zheng; Yang, Yong-Qing; Xiong, Weixiang published the artcile< Preparation of 1,3-Thiazolidine-2-thiones by Using Potassium Ethylxanthate as a Carbon Disulfide Surrogate>, Electric Literature of 171877-39-7, the main research area is thiazolidine thione preparation green chem; amino alc potassium ethylxanthate heterocyclization.

A simple procedure is presented for preparing 1,3-thiazolidine-2-thiones, e.g., I by using potassium ethylxanthate and the corresponding β-amino alcs. as the starting materials in the presence of ethanol.

Synlett published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Electric Literature of 171877-39-7.

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

Augustin, J.; Drobnica, L.; Kristian, P. published the artcile< Antimicrobial activity of dithiocarbamates and other sulfur containing compounds>, HPLC of Formula: 10574-69-3, the main research area is sulfur compound ionization equilibrium microbicide; thiocarbamate ionization equilibrium microbicide.

The rate of decomposition of monothiocabamates, dithiocarbamates and their esters, and 3-substituted rhodanines in acidic, neutral, and alk. solutions was calculated from spectrophotometric measurements in absorption maximum in the UV region. Reactions were pH-dependent; thus, ionization equilibrium is involved in compound stability in solution and in their microbicidal activity, i.e., isothiocyanate formation.

Abhandlungen der Akademie der Wissenschaften der DDR, Abteilung Mathematik, Naturwissenschaften, Technik published new progress about Decomposition. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, HPLC of Formula: 10574-69-3.

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

Pil’o, S. G.; Brovarets, V. S.; Romanenko, E. A.; Drach, B. S. published the artcile< Reaction of 3,3-dichloro-2-[(dichloroacetyl)amino]acrylonitrile with amines>, Electric Literature of 10574-69-3, the main research area is oxazolecarbonitrile derivative preparation hydrolysis condensation reaction; polychlorinated enamidonitrile heterocyclization amine.

Polychlorinated enamidonitrile Cl2C:C(CN)NHCOCHCl2 readily reacts with primary aromatic amines, dialkylamines, piperidine, and morpholine. The reaction is accompanied by complete elimination of chlorine atoms as chloride ions with formation of 4-cyanooxazoles having the corresponding amine residue in position 5 of the ring and a CH:N or diaminomethyl moiety in position 2. The structure of 5-arylamino(dialkylamino)-4-cyano-2-formyloxazoles was confirmed by their acid hydrolysis, as well as by condensation with phenylhydrazine, N-alkylrhodanines, and Et acetoacetate in the presence of urea.

Russian Journal of General Chemistry (Translation of Zhurnal Obshchei Khimii) published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Electric Literature of 10574-69-3.

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

Peixoto, Philippe A.; Richard, Jean-Alexandre; Severin, Rene; Chen, David Y.-K. published the artcile< Total Synthesis of Echinopines A and B: Exploiting a Bioinspired Late-Stage Intramolecular Cyclopropanation [Erratum to document cited in CA155:510334]>, COA of Formula: C10H11NS2, the main research area is erratum echinopine A B synthesis intramol cyclopropanation.

On page 5724, citations were omitted from reference 1; the omitted citations are given.

Organic Letters published new progress about Cycloisomerization. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, COA of Formula: C10H11NS2.

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

Sinenko, V. O.; Slivchuk, S. R.; Pil’o, S. G.; Raenko, G. F.; Brovarets, V. S. published the artcile< Synthesis of new 1,3-thiazole derivatives from 2(5)-hydroxyalkyl-1,3-thiazole-5(2)-carbaldehydes>, Application of C10H9NOS2, the main research area is thiazole preparation; carbaldehyde thiazole acetoacetic ester urea Biginelli; phenylhydrazine isoniazid rhodanine thiazole carbaldehyde condensation.

Reactions of substituted 2-hydroxyalkyl-1,3-thiazole-5-carbaldehydes and 5-hydroxyalkyl-1,3-thiazole-2-carbaldehydes with phenylhydrazine, isoniazid, N-substituted rhodanines were performed as well as Biginelli reaction with acetoacetic ester and urea. As a result, new 1,3-thiazole derivatives were obtained. They are of interest as potential bioactive substances.

Russian Journal of General Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Application of C10H9NOS2.

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

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