Tag: M.W=100-150

Zhong, Zhao-Jin; Zhang, Da-Jun; Peng, Zong-Gen; Li, Yu-Huan; Shan, Guang-Zhi; Zuo, Li-Min; Wu, Lin-Tao; Li, Si-Yang; Gao, Rong-Mei; Li, Zhuo-Rong published the artcile< Synthesis and antiviral activity of a novel class of (5-oxazolyl)phenyl amines>, Name: Thiazole-5-carboxyaldehyde, the main research area is preparation oxazole antiviral human treatment viral infection HCV; (5-Oxazolyl)phenyl amine; Antiviral activity; Structure–activity relationships; Synthesis.

A series of novel (5-oxazolyl)phenyl amine derivatives were synthesized and their antiviral activities against the hepatitis C virus (HCV) and the coxsackie virus B3 (CVB3) and B6 (CVB6) were evaluated in vitro. Bioassays showed that the synthesized compounds 17a1, 17a4, 17a6, 17b1, 17d1, 17e2 and 17g3 exhibited potent antiviral activity against HCV (IC50 = 0.28-0.92 μM) and most synthesized compounds exhibited low cytotoxicity in Huh7.5 cells, compared to telaprevir. The compounds 17a1, 17a4, 17a5, 17a6, 17b1, 17b2, 17g1 and 17g3 showed strong activity against the CVB3 and/or CVB6 at low concentrations (IC50 < 2.0 μM). The (5-oxazolyl)phenyl amines 17a1, 17a4, 17a8, 17b1, 17d1, 17e2, 17f3 and 17g3 were identified as the most active on the biol. assays, and will be studied further. European Journal of Medicinal Chemistry published new progress about Antiviral agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Name: Thiazole-5-carboxyaldehyde.

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

Masuda, Naoyuki; Yamamoto, Osamu; Fujii, Masahiro; Ohgami, Tetsuro; Moritomo, Ayako; Kontani, Toru; Kageyama, Shunji; Ohta, Mitsuaki published the artcile< Regioselective Alkylation of Thiazolylsulfonamides: Direct and Efficient Synthesis of 3-Alkylthiazolidene Derivatives>, Recommanded Product: 5-Isopropylthiazol-2-amine, the main research area is thiazolylsulfonamide alkyl halide regioselective alkylation; thiazolidene sulfonamide preparation; alkylthiazolidene sulfonamide preparation; sulfonyliminothiazole preparation.

Various N(3)-alkylated thiazolidene sulfonamide derivatives were efficiently prepared by the direct endo-selective alkylation of thiazolyl sulfonamides. The effects of different bases and solvents were investigated, and the NaH-THF combination was found to be the most effective at conferring high yields and endo-selectivity.

Synthetic Communications published new progress about Alkylation, regioselective. 101080-15-3 belongs to class thiazole, and the molecular formula is C6H10N2S, Recommanded Product: 5-Isopropylthiazol-2-amine.

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

Hughes, Rachael A.; Thompson, Stewart P.; Alcaraz, Lilian; Moody, Christopher J. published the artcile< Total Synthesis of the Thiopeptide Antibiotic Amythiamicin D>, SDS of cas: 31825-95-3, the main research area is amythiamicin antibiotic thiopeptide total synthesis; pyridine trisubstituted preparation hetero Diels Alder reaction acetylenamine ethoxyazadiene.

The thiopeptide (or thiostrepton) antibiotics are a class of sulfur containing highly modified cyclic peptides with interesting biol. properties, including reported activity against MRSA and malaria. This work describes the total synthesis of the thiopeptide natural product amythiamicin D (I), and the key step is a biosynthesis-inspired hetero-Diels-Alder route to the pyridine core of the thiopeptide. Preliminary studies using a range of serine-derived 1-ethoxy-2-azadienes established that hetero-Diels-Alder reaction with N-acetylenamines proceeded efficiently under microwave irradiation to give 2,3,6-trisubstituted pyridines. The thiazole building blocks of the antibiotic were obtained by either classical Hantzsch reactions or by dirhodium(II)-catalyzed chemoselective carbene N-H insertion followed by thionation, and were combined to give the bis-thiazole that forms the left-hand fragment of the antibiotic. The key Diels-Alder reaction of a tris-thiazolylazadiene II with benzyl 2-(1-acetylaminoethenyl)thiazole-4-carboxylate gave the core tetrathiazolyl pyridine III, which was elaborated into the natural product by successive incorporation of glycine and bis-thiazole fragments followed by macrocyclization.

Journal of the American Chemical Society published new progress about Cyclic peptides Role: SPN (Synthetic Preparation), PREP (Preparation) (thiopeptides). 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, SDS of cas: 31825-95-3.

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

Ribeiro, Gabriel H.; Guedes, Adriana P. M.; de Oliveira, Tamires D.; de Correia, Camila R. S. T. b.; Colina-Vegas, Legna; Lima, Mauro A.; Nobrega, Joaquim A.; Cominetti, Marcia R.; Rocha, Fillipe V.; Ferreira, Antonio G.; Castellano, Eduardo E.; Teixeira, Felipe R.; Batista, Alzir A. published the artcile< Ruthenium(II) Phosphine/Mercapto Complexes: Their in Vitro Cytotoxicity Evaluation and Actions as Inhibitors of Topoisomerase and Proteasome Acting as Possible Triggers of Cell Death Induction>, Application In Synthesis of 96-53-7, the main research area is preparation ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; crystal structure ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; HSA interaction ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; cyclic voltammetry ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; DNA interaction ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; anticancer activity ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex.

A series of new ruthenium complexes of the general formula [Ru(NS)(dpphpy)(dppb)]PF6 (Ru1-Ru3), where dpphpy = diphenyl-2-pyridylphosphine, NS ligands = 2-thiazoline-2-thiol (tzdt, Ru1, 1), 2-mercaptopyrimidine (pySm, Ru2, 2), and 4,6-diamino-2-mercaptopyrimidine (damp, Ru3, 3), and dppb = 1,4-bis(diphenylphosphino)butane, were synthesized and characterized by elemental anal., spectroscopic techniques (IR, UV/visible, and 1D and 2D NMR), and x-ray diffraction. In the characterization, the correlation between the phosphorus atoms and their resp. aromatic hydrogen atoms of the compounds in the assignment stands outs, by 1H-31P HMBC experiments The compounds show anticancer activities against A549 (lung) and MDA-MB-231 (breast) cancer cell lines, higher than the clin. drug cisplatin. All of the complexes are more cytotoxic against the cancer cell lines than against the MRC-5 (lung) and MCF-10 Å (breast) nontumorigenic human cell lines. For A549 tumor cells, cell cycle anal. upon treatment with Ru2 showed that it inhibits the mitotic phase because arrest was observed in the Sub-G1 phase. Addnl., the compound induces cell death by an apoptotic pathway in a dose-dependent manner, according to annexin V-PE assay. The multitargeted character of the compounds was studied, and the biomols. were DNA, topoisomerase IB, and proteasome, as well as the fundamental biomol. in the pharmacokinetics of drugs, human serum albumin. The complexes do not target DNA in the cells. At low concentrations, the compounds showed the ability to partially inhibit the catalytic activity of topoisomerase IB in the process of relaxation of the DNA plasmid. Among the complexes assayed in cultured cells, complex Ru3 was able to diminish the proteasomal chymotrypsin-like activity to a greater extent. New ruthenium phosphine complexes show anticancer activities against A549 (lung) and MDA-MB-231 (breast) cancer cell lines, higher than the clin. drug cisplatin. For A549 tumor cells, cell cycle anal. upon treatment with Ru2 showed that it inhibits the mitotic phase because arrest was observed in the Sub-G1 phase and induces cell death by an apoptotic pathway. The multitargeted character of the compounds was studied with the biomols. DNA, topoisomerase IB, and proteasome.

Inorganic Chemistry published new progress about Antitumor agents. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application In Synthesis of 96-53-7.

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

Sieng, Bora; Maldonado, Matias Funes; Romagnoli, Carlo; Amedjkouh, Mohamed published the artcile< One-Pot Alkynylation of Azaaryl Aldehydes and Spontaneous Base-Free Rearrangement into Enone Esters: an Autoinductive Mechanism>, Formula: C4H3NOS, the main research area is unsaturated ketoester diastereoselective preparation; butyllithium methylzinc catalyst addition propiolate heteroaryl aldehyde stereoselective rearrangement; isotope labeling allenoate trapping mechanism addition rearrangement propargylic alc.

When heteroaromatic aldehydes are reacted with Et propiolate in the presence of Me2Zn or BuLi, γ-oxo-α,β-unsaturated esters were generated by spontaneous rearrangements of the intermediate propargylic alcs.; in some cases, the propargyl alcs. were formed without rearrangement. The mechanism of the rearrangement was studied using isotope labeling and trapping of a proposed allenoate intermediate; an autocatalytic mechanism is proposed.

European Journal of Organic Chemistry published new progress about Addition reaction. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Formula: C4H3NOS.

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

Yu, Ming; Lizarzaburu, Mike; Motani, Alykhan; Fu, Zice; Du, Xiaohui; Liu, Jiwen; Jiao, Xianyun; Lai, SuJen; Fan, Peter; Fu, Angela; Liu, Qingxiang; Murakoshi, Michiko; Nara, Futoshi; Oda, Kozo; Okuyama, Ryo; Reagan, Jeff D.; Watanabe, Nobuaki; Yamazaki, Mami; Xiong, Yumei; Zhang, Ying; Zhuang, Run; Lin, Daniel C.-H.; Houze, Jonathan B.; Medina, Julio C.; Li, Leping published the artcile< Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies>, SDS of cas: 1003-32-3, the main research area is amrinone phenylalanine carboxylic acid preparation GPR142 agonist structure design; pharmacokinetics bioavailability diabetes amrinone phenylalanine carboxylic acid antidiabetic prodrug; glucose tolerance insulin secretagogue human islet transplant CYP450 hERG; GPR142 agonist; aminopyrazole−phenylalanine; human islet transplant; insulin secretagogue; oral glucose tolerance test; prodrug; type 2 diabetes.

Herein, we report the lead optimization of amrinone-phenylalanine based GPR142 agonists. Structure-activity relationship studies led to the discovery of aminopyrazole-phenylalanine carboxylic acid I, which exhibited good agonistic activity, high target selectivity, desirable pharmacokinetic properties, and no cytochrome P 450 or hERG liability. Compound I, together with its orally bioavailable Et ester prodrug II, were found to be suitable for in vivo proof-of-concept studies. Compound II displayed good efficacy in a mouse oral glucose tolerance test (OGTT). CompoundI showed GPR142 dependent stimulation of insulin secretion in isolated mouse islets and demonstrated a statistically significant glucose lowering effect in a mouse model bearing transplanted human islets.

ACS Medicinal Chemistry Letters published new progress about Antidiabetic agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, SDS of cas: 1003-32-3.

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

Diop, Aboubacar; Diop, Tidiane; Kama, Antoine Blaise; Diop, Cheikh Abdou Khadre; Tumanov, Nikolay published the artcile< Catena-Poly[[chloridotris(1,3-thiazolidine-2-thione-κS)cadmium(II)]-μ-chlorido]>, Safety of 4,5-Dihydrothiazole-2-thiol, the main research area is catena polychloridotris thiazolidine thione cadmium chlorido crystal structure.

The synthesis and characterization of poly[dichloridotri(1,3-thiazolidine-2-thione)cadmium(II)], [CdCl2(C3H5NS2)3]n, prepared from CdCl2·H2O and C3H5NS2 (tzdSH) in a 1:3 ratio, are described. The CdII cation is coordinated by three 1,3-thiazolidine-2-thione mols. and three Cl- anions in a distorted octahedral environment. The Cd metal centers are connected via Cl- ligands, creating polymeric chains running along the a-axis direction. The conformation of the chains is stabilized by N-H···Cl hydrogen bonds.

IUCrData published new progress about Asymmetry. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Safety of 4,5-Dihydrothiazole-2-thiol.

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

Chen, Fei; Chai, Hui; Su, Ming-Bo; Zhang, Yang-Ming; Li, Jia; Xie, Xin; Nan, Fa-Jun published the artcile< Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors>, Quality Control of 31825-95-3, the main research area is bisthiazole histone deacetylase inhibitor preparation evaluation exptl autoimmune encephalomyelitis; Histone deacetylase inhibitors; bisthiazole; largazole.

Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors was prepared and evaluated. Compound I was evaluated in vivo in an exptl. autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clin. symptoms of EAE in mice.

ACS Medicinal Chemistry Letters published new progress about Experimental allergic encephalomyelitis (model for multiple sclerosis). 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, Quality Control of 31825-95-3.

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

Wei, Yuan; Lang, Xiaolong; Hore, Michael J. A. published the artcile< A correspondence between the Flory-Rehner theory for microgels and the Daoud-Cotton model for polymer-grafted nanoparticles>, Synthetic Route of 96-53-7, the main research area is Flory Rehner microgel Daoud Cotton model polymer grafted nanoparticle.

Poly(N-iso-Pr acrylamide) (PNIPAM) is a commonly investigated thermoresponsive polymer that exhibits a number of interesting phys. behaviors. Here, we use small-angle neutron scattering (SANS) measurements to determine the conformation of PNIPAM in two regions of the chain when it is grafted at moderate grafting densities to the surface of SiO2 nanoparticles (rNP ≈ 10 nm). At these grafting densities, polymer chains may adopt two primary conformations, depending on the specific value of the second virial coefficient, the mol. weight of the chains, and other properties. The nanoparticles are studied in D2O and ethanol-d6 to ascertain the effect of solvent quality on the chain conformation in both the inner and outer regions of the brush. The SANS measurements are interpreted using a modified Daoud-Cotton model that connects the Flory-Rehner theory of microgel thermodn. to the structure of polymer-grafted nanoparticles. (c) 2020 American Institute of Physics.

Journal of Applied Physics (Melville, NY, United States) published new progress about Hydrodynamic radius. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Synthetic Route of 96-53-7.

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

Sun, Wencheng; Teng, Qiaoling; Cheng, Dongping; Li, Xiaonian; Xu, Xiaoliang published the artcile< The hydrodebromination of 1,1-dibromoalkenes via visible light catalysis>, Computed Properties of 1003-32-3, the main research area is dibromoalkene preparation iridium photocatalyst diastereoselective hydrodebromination green chem; bromoalkene preparation.

A hydrodebromination reaction of 1,1-dibromoalkenes was established via visible light catalysis. A variety of structurally different vinyl bromides were obtained in moderate to excellent yields.

Tetrahedron Letters published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Computed Properties of 1003-32-3.

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