Tag: M.W=100-150

Aulakh, Virender S.; Ciufolini, Marco A. published the artcile< An improved synthesis of pyridine-thiazole cores of thiopeptide antibiotics>, Synthetic Route of 31825-95-3, the main research area is pyridinethiazole core thiopeptide antiobiotic preparation.

The oxidation of 2-methylthiazoles to 2-formylthiazoles simplifies the implementation of the Bagley variant of the Bohlmann-Rahtz reaction as a key step in a concise route to pyridine cores of thiopeptide antibiotics.

Journal of Organic Chemistry published new progress about Bohlmann-Rahtz reaction. 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, Synthetic Route of 31825-95-3.

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

Mack, Daniel J.; Isoe, Jun; Miesfeld, Roger L.; Njardarson, Jon T. published the artcile< Distinct biological effects of golgicide a derivatives on larval and adult mosquitoes>, COA of Formula: C4H3NOS, the main research area is golgicide A derivative larvicidal insecticide mosquito larva.

A collection of Golgicide A (GCA) analogs has been synthesized and evaluated in larval and adult mosquito assays. Com. available GCA is a mixture of four compounds One enantiomer (GCA-2) of the major diastereomer in this mixture was shown to be responsible for the unique activity of GCA. Structure-activity studies (SAR) of the GCA architecture suggested that the pyridine ring was most easily manipulated without loss or gain in new activity. Eighteen GCA analogs were synthesized of which five displayed distinct behavior between larval and adult mosquitos, resulting in complete mortality of both Aedes aegypti and Anopheles stephensi larvae. Two analogs from the collection were shown to be distinct from the rest in displaying high selectivity and efficiency in killing An. stephensi larvae.

Bioorganic & Medicinal Chemistry Letters published new progress about Aedes aegypti. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, COA of Formula: C4H3NOS.

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

da Silva, Monize M.; de Camargo, Mariana S.; Castelli, Silvia; de Grandis, Rone A.; Castellano, Eduardo E.; Deflon, Victor M.; Cominetti, Marcia R.; Desideri, Alessandro; Batista, Alzir A. published the artcile< Ruthenium(II)-mercapto complexes with anticancer activity interact with topoisomerase IB>, Name: 4,5-Dihydrothiazole-2-thiol, the main research area is rutheniumII mercapto anticancer activity topoisomerase IB lung liver cancer.

Herein we present four new ruthenium(II) complexes: [Ru(mtz)2(dppb)] (1), [Ru(mmi)2(dppb)] (2), [Ru(dmp)2(dppb)] (3), and [Ru(mpca)2(dppb)] (4), where mtz = 2-mercaptothiazoline; mmi = 2-mercapto-1-methyl-imidazole; dmp = 4,6-diamino-2-mercaptopyrimidine; mpca = 6-mercaptopyridine-3-carboxylic acid; dppb = 1,4-bis(diphenylphosphino)butane. In vitro cell culture experiments revealed cytotoxic activity for complexes 2, 3 and 4 against MCF-7 (breast, non-invasive), MDA-MB-231 (breast, invasive), A549 (lung), DU-145 (prostate) and HepG2 (liver) tumor cells, in some cases lower than the half maximal inhibitory concentration (IC50) for the reference drug (cisplatin). The DNA (DNA) interactions studied by viscosity measurements, gel electrophoresis and square-wave voltammetry indicated that the DNA binding affinity primarily occurs through non-covalent interactions. Only complex 2 was able to fully inhibit the DNA supercoiled relaxation mediated by human topoisomerase IB (Top IB). The anal. indicates that complex 2 inhibits the cleavage and the reconnection steps of the catalytic cycle, being both a poison and a catalytic inhibitor.

Journal of the Brazilian Chemical Society published new progress about Antitumor agents. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Name: 4,5-Dihydrothiazole-2-thiol.

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

Ford, Kevin A.; Gulevich, Alexander G.; Swenson, Tami L.; Casida, John E. published the artcile< Neonicotinoid Insecticides: Oxidative Stress in Planta and Metallo-oxidase Inhibition>, Recommanded Product: Thiazole-5-carboxyaldehyde, the main research area is neonicotinoid insecticide oxidative stress plant metallooxidase inhibition.

Neonicotinoids not only control insect pests but also sometimes independently alter plant growth and response to stress. We find that imidacloprid, thiacloprid, acetamiprid, thiamethoxam, and clothianidin but not nitenpyram and dinotefuran induce foliar lesions and peroxidative damage in soybean (Glycine max) seedlings assayed with the 3,3′-diaminobenzidine stain. The chloropyridinyl-carboxylic acid (COOH) but not the -carboxaldehyde (CHO) metabolites induce peroxidative damage but in a different pattern. Surprisingly, the chlorothiazolyl -CHO and -COOH metabolites induce chlorosis but no clear superimposable peroxidative damage or cell death. Four metallo-oxidases known to modulate reactive oxygen species were not sensitive in vitro to the parent neonicotinoid itself but were to several CHO and COOH metabolites and related compounds, with a sensitivity order of CHO > COOH and tyrosinase > xanthine oxidase and aldehyde oxidase > catalase. Although metallo-oxidase inhibition does not correlate overall with lesion formation, it may play an as yet unknown role in plant response to neonicotinoids.

Journal of Agricultural and Food Chemistry published new progress about Chlorosis (plant). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Recommanded Product: Thiazole-5-carboxyaldehyde.

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

Seganish, W. Michael; Bercovici, Ana; Ho, Ginny D.; Loozen, Hubert J. J.; Timmers, Cornelis M.; Tulshian, Deen published the artcile< A synthesis of dihydroimidazo[5,1-a]isoquinolines using a sequential Ugi-Bischler-Napieralski reaction sequence>, Product Details of C4H3NOS, the main research area is isonitrile aldehyde carboxylate ammonia sequential Ugi Bischler Napieralski; hydroimidazoisoquinoline preparation.

A flexible route to analogs of dihydroimidazo[5,1-a]isoquinolines was described. The synthesis hinges on a sequential Ugi coupling, followed by a Bischler-Napieralski reaction to form the imidazole-isoquinoline core. This route facilitates the introduction of a range of substitutions throughout the C framework.

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, Product Details of C4H3NOS.

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

Roe, Caroline; Hobbs, Heather; Stockman, Robert A. published the artcile< One-Pot Synthesis of Chiral Nonracemic Amines>, Computed Properties of 1003-32-3, the main research area is chiral nonracemic amine preparation green chem; sulfinamide preparation green chem; oxathiazolidine oxide.

One-pot five-component reactions of oxathiazolidine-S-oxides with mesitylmagnesium bromide, lithium bis(trimethylsilyl)amide, aldehydes and Grignard reagents afford chiral nonracemic amines or sulfinamides in good yields and high stereoselectivities.

Journal of Organic Chemistry published new progress about Amines Role: SPN (Synthetic Preparation), PREP (Preparation). 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

Lynn, Geoffrey M.; Chytil, Petr; Francica, Joseph R.; Lagova, Anna; Kueberuwa, Gray; Ishizuka, Andrew S.; Zaidi, Neeha; Ramirez-Valdez, Ramiro A.; Blobel, Nicolas J.; Baharom, Faezzah; Leal, Joseph; Wang, Amy Q.; Gerner, Michael Y.; Etrych, Tomas; Ulbrich, Karel; Seymour, Leonard W.; Seder, Robert A.; Laga, Richard published the artcile< Impact of Polymer-TLR-7/8 Agonist (Adjuvant) Morphology on the Potency and Mechanism of CD8 T Cell Induction>, Electric Literature of 96-53-7, the main research area is polymer toll like receptor agonist vaccine adjuvant block copolymer.

Small mol. Toll-like receptor-7 and -8 agonists (TLR-7/8a) can be used as vaccine adjuvants to induce CD8 T cell immunity but require formulations that prevent systemic toxicity and focus adjuvant activity in lymphoid tissues. Here, we covalently attached TLR-7/8a to polymers of varying composition, chain architecture and hydrodynamic behavior (∼300 nm submicrometer particles, ∼10 nm micelles and ∼4 nm flexible random coils) and evaluated how these parameters of polymer-TLR-7/8a conjugates impact adjuvant activity in vivo. Attachment of TLR-7/8a to any of the polymer compositions resulted in a nearly 10-fold reduction in systemic cytokines (toxicity). Moreover, both lymph node cytokine production and the magnitude of CD8 T cells induced against protein antigen increased with increasing polymer-TLR-7/8a hydrodynamic radius, with the submicrometer particle inducing the highest magnitude responses. Notably, CD8 T cell responses induced by polymer-TLR-7/8a were dependent on CCR2+ monocytes and IL-12, whereas responses by a small mol. TLR-7/8a that unexpectedly persisted in vaccine-site draining lymph nodes (T1/2 = 15 h) had less dependence on monocytes and IL-12 but required Type I IFNs. This study shows how modular properties of synthetic adjuvants can be chem. programmed to alter immunity in vivo through distinct immunol. mechanisms.

Biomacromolecules published new progress about CD8-positive T cell. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Electric Literature of 96-53-7.

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

Wu, Yue-Xiao; Peng, Kang; Hu, Zhi-Chao; Fan, Yong-Hao; Shi, Zhen; Hao, Er-Jun; Dong, Zhi-Bing published the artcile< Iodine-Mediated Cross-Dehydrogenative Coupling of Heterocyclic Thiols with Amines: An Easy and Practical Formation of S-N Bond>, Application of C3H5NS2, the main research area is amine heteroaryl thiol iodine promoter cross dehydrogenative coupling; heteroaryl sulfenamide preparation.

An efficient iodine-mediated construction of S-N bond was developed. Such a cross-dehydrogenative coupling of heterocyclic thiols with amines proceeded smoothly under metal-free and base-free conditions, and afforded a series of sulfenamides in good to excellent yields. The easily available substrates and convenient synthetic procedure illustrate potential synthetic value of this protocol for the preparation of sulfenamide related biol. or pharmaceutically active compounds

European Journal of Organic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application of C3H5NS2.

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

Ling, Xing; Lu, Weiwei; Miao, Lin; Marcaurelle, Lisa A.; Wang, Xuan; Ding, Yun; Lu, Xiaojie published the artcile< Divergent On-DNA Transformations from DNA-Linked Piperidones>, Computed Properties of 1003-32-3, the main research area is DNA linked heterocycle preparation.

A group of highly efficient and divergent transformations for constructing multiple DNA-linked chemotypes based on piperidones e.g., I core is successfully developed. The first procedure for the synthesis of DNA-conjugated piperidines II (R = H, Bn, (4-cyanophenyl)methyl, (3,4,5-trifluorophenyl)methyl, etc.; R1 = 2,2-dimethoxyethyl, Bn, 3-cyclohexylpropanoyl, etc.) intermediate under basic conditions was reported. Subsequently, this substructure was subjected to addnl. reactions to generate several privileged scaffolds, including 4-aminopiperidines II, fused [1,2,4]triazolo[1,5-a]pyrimidines III (R2 = methanesulfonyl, (3-fluorophenyl)methyl, benzenesulfonamido), and a quinoline derivative e.g., IV. These transformations paved the way for constructing focused scaffold-based DNA-encoded libraries with druglike properties.

Journal of Organic Chemistry published new progress about Acids 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

Bataille, Carole J. R.; Brennan, Meabh B.; Byrne, Simon; Davies, Stephen G.; Durbin, Matthew; Fedorov, Oleg; Huber, Kilian V. M.; Jones, Alan M.; Knapp, Stefan; Liu, Gu; Nadali, Anna; Quevedo, Camilo E.; Russell, Angela J.; Walker, Roderick G.; Westwood, Robert; Wynne, Graham M. published the artcile< Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family>, Synthetic Route of 1003-32-3, the main research area is thiazolidine preparation serine threonine kinase inhibitor anticancer agent; Knoevenagel condensation Sukuki coupling; Anti-cancer; High throughput screen; Kinase inhibitor; PIM kinase; Thiazolidine.

The PIM family of serine/threonine kinases have become an attractive target for anti-cancer drug development, particularly for certain hematol. malignancies. Here, we describe the discovery of a series of inhibitors of the PIM kinase family using a high throughput screening strategy. Through a combination of mol. modeling and optimization studies, the intrinsic potencies and mol. properties of this series of compounds was significantly improved. An excellent pan-PIM isoform inhibition profile was observed across the series, while optimized examples show good selectivity over other kinases. Two PIM-expressing leukemic cancer cell lines, MV4-11 and K562, were employed to evaluate the in vitro anti-proliferative effects of selected inhibitors. Encouraging activities were observed for many examples, with the best example (44) giving an IC50 of 0.75 μM against the K562 cell line. These data provide a promising starting point for further development of this series as a new cancer therapy through PIM kinase inhibition.

Bioorganic & Medicinal Chemistry 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, Synthetic Route of 1003-32-3.

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