Day: November 29, 2022

Rogovoy, Maxim I. published the artcileSelf-assembly of Ag(I)-based complexes and layered coordination polymers bridged by (2-thiazolyl)sulfides, COA of Formula: C4H5NS2, the publication is Inorganica Chimica Acta (2019), 19-26, database is CAplus.

Dinuclear complex, [Ag₂(2-Mt)₂(MeCN)₂(NO₃)₂] (1) as well as layered (2D) coordination polymers (CPs), [Ag₂(2-Mt)₂(NO₃)₂]_n (2) and [Ag₄(2-Mt)₄(NO₃)₄·2H₂O]_n (3), are self-assembled from 2-(methylthio)thiazole (2-Mt) and AgNO₃ under different conditions. These compounds contain a [Ag₂(2-Mt)₂] unit consisting of two metal atoms bridged by 2-Mt ligands (μ₂-N,S) in head-to-tail (for 1 and 2) and head-to-head (for 3) manner. 2-(Methylthio)benzothiazole (2-Mbt) reacts with AgNO₃ to assemble complex [Ag₂(2-Mbt)₂(MeCN)₂(NO₃)₂] (4), showing interesting dual emission behavior associated with the presence of fluorescence and phosphorescence, contributions of which depends on the excitation wavelength.

Inorganica Chimica Acta published new progress about 5053-24-7. 5053-24-7 belongs to thiazole, auxiliary class Thiazole,sulfides, name is 2-(Methylthio)thiazole, and the molecular formula is C4H5NS2, COA of Formula: C4H5NS2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Artem’ev, Alexander V. published the artcileCuI-based coordination polymers with 2-thiazolyl sulfide ligands: First examples, COA of Formula: C4H5NS2, the publication is Polyhedron (2018), 171-176, database is CAplus.

The reaction of CuI with 2-(methylthio)thiazole (MTT) in a 1:1 or 2:1 molar ratio (MeCN, rt, 1h) leads to the coordination polymer [CuI(MTT)]_n (CP1) or [(CuI)₂(MTT)]_n (CP2), resp. CP1 consists of (-Cu-I-Cu-I-)_n zigzag chains wherein the adjacent Cu atoms are bridged by the MTT ligand through the thiazole N and sulfide S atoms. 1-D chains of CP2 are assembled from corner-sharing [CuI₃N] and [CuI₃S] tetrahedra, which alternate in a zigzag fashion. By contrast, 2-(methylthio)benzothiazole (MTBT) reacts with CuI, regardless of the reactants ratio, to give the dinuclear complex [Cu₂I₂(MTBT)₂], where the planar [Cu(μ₂-I)]₂ core is supported by the two ligands in the N-monodentate manner. At ambient temperature, CP1 exhibits a weak yellow luminescence (λ_max=570nm), while CP2 emits in the deep-red region (λ_max=705nm).

Polyhedron published new progress about 5053-24-7. 5053-24-7 belongs to thiazole, auxiliary class Thiazole,sulfides, name is 2-(Methylthio)thiazole, and the molecular formula is C4H5NS2, COA of Formula: C4H5NS2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ichihara, Osamu published the artcileDevelopment of self-indicating resin, Computed Properties of 92-36-4, the publication is Combinatorial Chemistry & High Throughput Screening (2007), 10(4), 261-267, database is CAplus and MEDLINE.

The development and application of self-indicating resins (SIR), materials which can indicate the presence or absence of amines in the reaction solution by the conspicuous color change of a phenolsulfophthalein type dye immobilized on resin beads has been reported. Although the functionality necessary for attaching the dye to the resins could be readily introduced by the Suzuki-Miyaura coupling during the synthesis of the SIR, this approach was only applicable to the dyes containing suitable functionality for the cross-coupling reaction. A new approach to immobilizing the indicating dyes onto the resin support is now reported. The dyes suitable for loading onto aminomethyl polystyrene (PS) resin were prepared by Friedel-Crafts reaction of 2-sulfoterephthalic anhydride with a wide range of phenols. Using this new route, polymer-supported dye I was readily prepared in >100g quantities. Use of I in the synthesis of a 144 member urea library was demonstrated and the SIR successfully indicated the endpoint of the reaction between amines and isocyanates.

Combinatorial Chemistry & High Throughput Screening published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Computed Properties of 92-36-4.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Prasad, V. S. R. published the artcileVersatile synthesis of 2-aryl[1,2,4]triazolo[3′,2′:2,3]thiazolo[5,4-b]pyridines, Safety of 5-Chlorothiazolo[5,4-b]pyridin-2-amine, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (1991), 30B(5), 517-18, database is CAplus.

The reaction of aminothiazolopyridines I (R = Cl, OMe) with RC₆H₄CN ( R = H, 2-, 4-Me, 2-, 4-Cl, 4-NO₂) in the presence of AlCl₃ gave arylamidines II, which on dehydrogenation-cyclization with Pb(OAc)₄ in benzene gave triazolothiazolopyridines III.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C6H4ClN3S, Safety of 5-Chlorothiazolo[5,4-b]pyridin-2-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Prasad, V. S. R. published the artcileFormation and pyrolysis of 1-(2-thiazolo[5,4-b]pyridyl)-5-aryltetrazoles, Recommanded Product: 5-Chlorothiazolo[5,4-b]pyridin-2-amine, the publication is Synthetic Communications (1990), 20(13), 1983-8, database is CAplus.

The reaction of 2-amino-5-chlorothiazolo[5,4-b]pyridine or 2-amino-5-methoxythiazolo[5,4-b]pyridine with RC₆H₄COCl (R = H, 4-Me, 2-Cl, 4-Cl, 4-MeO) gave the resp. amides which were treated with PCl₅ and then with NaN₃ to give (thiazolopyridyl)phenyltetrazole derivatives The latter were pyrolyzed to give 2-aryl-1,2,4-triazolo[3′,2′:2,3]thiazolo[5,4-b]pyridines I (same R), presumably via a nitrene intermediate.

Synthetic Communications published new progress about 31784-71-1. 31784-71-1 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorothiazolo[5,4-b]pyridin-2-amine, and the molecular formula is C6H4ClN3S, Recommanded Product: 5-Chlorothiazolo[5,4-b]pyridin-2-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Giovannucci, Tatiana A. published the artcileInhibition of the ubiquitin-proteasome system by an NQO1-activatable compound, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine, the publication is Cell Death & Disease (2021), 12(10), 914, database is CAplus and MEDLINE.

Malignant cells display an increased sensitivity towards drugs that reduce the function of the ubiquitin-proteasome system (UPS), which is the primary proteolytic system for destruction of aberrant proteins. Here, we report on the discovery of the bioactivatable compound CBK77, which causes an irreversible collapse of the UPS, accompanied by a general accumulation of ubiquitylated proteins and caspase-dependent cell death. CBK77 caused accumulation of ubiquitin-dependent, but not ubiquitin-independent, reporter substrates of the UPS, suggesting a selective effect on ubiquitin-dependent proteolysis. In a genome-wide CRISPR interference screen, we identified the redox enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1) as a critical mediator of CBK77 activity, and further demonstrated its role as the compound bioactivator. Through affinity-based proteomics, we found that CBK77 covalently interacts with ubiquitin. In vitro experiments showed that CBK77-treated ubiquitin conjugates were less susceptible to disassembly by deubiquitylating enzymes. In vivo efficacy of CBK77 was validated by reduced growth of NQO1-proficient human adenocarcinoma cells in nude mice treated with CBK77. This first-in-class NQO1-activatable UPS inhibitor suggests that it may be possible to exploit the intracellular environment in malignant cells for leveraging the impact of compounds that impair the UPS.

Cell Death & Disease published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Shad, Naveed Akhtar published the artcileLamellar shape lead tungstate (PbWO4) nanostructures as synergistic catalyst for peroxidase mimetic activity, Computed Properties of 30931-67-0, the publication is Materials Research Express (2020), 7(1), 015520, database is CAplus.

Tungstate based nanomaterials have emerged as important class in transition metal oxide. In this study, Lead tungstate (PbWO₄) nanostructures with lamellar morphol. were prepared by hydrothermal method. The synthesized materials were characterized by XRD, SEM, FTIR, DLS, BET and PL. Nitrogen adsorption-desorption measurements indicated that the surface area of the synthesized lamellar morphol. was _∼86.225 m² g^-1. The lamellar-like morphol. showed enhanced peroxidase-like activity owing to the large surface area, higher substrate interaction and efficient electron transportation. The results indicated higher reaction velocity (V_max = 13.56 × 10^-8 M s^-1) and low Michaelis-Menten constant (km = 0.325 mM) value for nanostructures, providing evidence for higher affinity of novel structures towards the substrate and increased peroxidase-like activity. Finally, biocompatibility test was conducted by performing cytotoxicity experiments of PbWO₄ nanostructures on MTT assays.

Materials Research Express published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C10H10O3, Computed Properties of 30931-67-0.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Tzanopoulou, Stamatia published the artcileEvaluation of Re and 99mTc Complexes of 2-(4′-Aminophenyl)benzothiazole as Potential Breast Cancer Radiopharmaceuticals, Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Journal of Medicinal Chemistry (2010), 53(12), 4633-4641, database is CAplus and MEDLINE.

The synthesis of M(I)(CO)₃(NNO) (M = Re, ^99mTc) complexes conjugated to the antitumor agent 2-(4′-aminophenyl)benzothiazole and to its 6-Me derivative, as well as their in vitro and in vivo biol. evaluation as breast cancer radiopharmaceuticals, is reported. The Re complexes displayed under the fluorescence microscope clear uptake by the sensitive to the 2-(4′-aminophenyl)benzothiazole pharmacophore breast cancer cell lines MCF-7 and T47D, while uptake by less sensitive lines and by normal fibroblasts was much weaker. In accordance, uptake of the corresponding radioactive ^99mTc complexes was clearly higher in the breast cancer cell lines MCF-7 and MDA-231 compared to normal fibroblasts. Biodistribution of the ^99mTc complexes in SCID mice bearing MCF-7 xenografts showed appreciable tumor uptake. A tumor/muscle ratio of 2.2 was measured for the complex conjugated to 2-(4′-aminophenyl)benzothiazole that led to successful tumor imaging. The results render the 2-(4′-aminophenyl)benzothiazole complexes potential candidates for imaging (^99mTc) and targeted radiotherapy (¹⁸⁸Re) of breast cancer.

Journal of Medicinal Chemistry published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C16H12O, Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Liudvinaviciute, Dovile published the artcileAdsorption of caffeic acid on chitosan powder, COA of Formula: C18H24N6O6S4, the publication is Polymer Bulletin (Heidelberg, Germany) (2021), 78(4), 2139-2154, database is CAplus.

Abstract: Adsorption of caffeic acid (CA) on chitosan (CH) powder from aqueous solution has been investigated to obtain insoluble CA-CH complex powders having different amount of CA. The pseudo-second kinetic model and the Langmuir, Freundlich and Dubinin-Radushkevich adsorption models were used to describe the kinetic and equilibrium adsorption of CA on CH. With the increase of adsorption temperature, the rate of adsorption increased while the amount of adsorbed CA decreased. The Langmuir adsorption model predicted that adsorption of CA takes place on the ionized amino groups of CH. However, with the increase of adsorption temperature the ion-exchange between carboxylic groups of CA and amino groups of CH became moderately difficult. The thermodn. characteristics of adsorption have been evaluated. CA-CH complex formation was confirmed by FT-IR spectroscopy. With increasing amount of adsorbed CA the CA-CH powder was becoming more hydrophobic. 2,2′-Azinobis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS) assay confirmed that CA retained the antioxidant activity when immobilized on chitosan power.

Polymer Bulletin (Heidelberg, Germany) published new progress about 30931-67-0. 30931-67-0 belongs to thiazole, auxiliary class Salt,Hydrazine,Amine,Benzothiazole, name is Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), and the molecular formula is C18H24N6O6S4, COA of Formula: C18H24N6O6S4.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ambure, Pravin published the artcileExploring Structural Requirements of Imaging Agents Against Aβ Plaques in Alzheimer’s Disease: A QSAR Approach, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Combinatorial Chemistry & High Throughput Screening (2015), 18(4), 411-419, database is CAplus and MEDLINE.

Exploring mol. imaging agents against the beta amyloid (Aβ) plaques for an early detection of Alzheimer’s disease (AD) is one of the emerging research areas in medicinal chem. In the present <i>in-silico</i> study, a congeneric series of 44 imaging agents, including 17 positron emission tomog. (PET) and 27 single photon emission computed tomog. (SPECT) imaging agents, was utilized to understand the structural features required for having essential binding affinity against Aβ plaques. Here, 2D-quant. structure-activity relationship (2D-QSAR) and group-based QSAR (G-QSAR) models have been developed using genetic function approximation (GFA) and validated using various statistical metrics. Both the models showed satisfactory performance signifying the reliability and robustness of the developed QSAR models. The vital information gained from both the QSAR models will be useful in developing new PET and SPECT imaging agents and also in predicting their binding affinity against Aβ plaques. The results of this study would be important in view of the widespread clin. applicability of the SPECT imaging agents, especially in the developing countries. In this study, we have also designed some imaging agents based on the information provided by the models. Some of these designed compounds were predicted to be similar to or more active than the most active imaging agents present in the original dataset.

Combinatorial Chemistry & High Throughput Screening published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica