Day: November 25, 2022

Zhao, Haiwei published the artcile[Ph₄P]⁺[Cu(CF₂H)₂]^–: A Powerful Difluoromethylating Reagent Inspired by Mechanistic Investigation, Category: thiazole, the publication is Angewandte Chemie, International Edition (2022), 61(42), e202210151, database is CAplus and MEDLINE.

The quest of the active species in copper-mediated difluoromethylation of aryl halides led to the discovery of a powerful difluoromethylating reagent [Ph₄P]⁺[Cu(CF₂H)₂]^–. [Ph₄P]⁺[Cu(CF₂H)₂]^– complex was able to difluoromethylate a variety of electrophiles including electron-deficient and electron-rich aryl iodides, heteroaryl iodides, activated heteroaryl bromides, chloride and aryl bromides with a directing group, as well as other electrophiles such as alkenyl iodide, benzyl bromides, allyl bromides, alkyl iodide, allyl carbonates and acid chloride. In addition, in the presence of an oxidant, [Ph₄P]⁺[Cu(CF₂H)₂]^– complex reacted with various lithium nbutyl arylboronic acid pinacol esters, alkyne and heteroarene. Moreover, [Ph₄P]⁺[Cu(CF₂H)₂]^– complex could transmetalate the difluoromethyl reagent to other metals such as [Ph₄P]⁺[CuCl₂]^– complex and [(DPPF)PdCl₂].

Angewandte Chemie, International Edition published new progress about 791614-90-9. 791614-90-9 belongs to thiazole, auxiliary class Boronate Esters,Boronic acid and ester,Boronic acid and ester, name is 2-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]thiazole, and the molecular formula is C14H14N2O2, Category: thiazole.

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

Megill, Andrea published the artcileA tetra(ethylene glycol) derivative of benzothiazole aniline enhances Ras-mediated spinogenesis, Name: 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Journal of Neuroscience (2013), 33(22), 9306-9318, database is CAplus and MEDLINE.

The tetra(ethylene glycol) derivative of benzothiazole aniline, BTA-EG₄, is a novel amyloid-binding small mol. that can penetrate the blood-brain barrier and protect cells from Aβ-induced toxicity. However, the effects of Aβ-targeting mols. on other cellular processes, including those that modulate synaptic plasticity, remain unknown. We report here that BTA-EG₄ decreases Aβ levels, alters cell surface expression of amyloid precursor protein (APP), and improves memory in wild-type mice. Interestingly, the BTA-EG₄-mediated behavioral improvement is not correlated with LTP, but with increased spinogenesis. The higher dendritic spine d. reflects an increase in the number of functional synapses as determined by increased miniature EPSC (mEPSC) frequency without changes in presynaptic parameters or postsynaptic mEPSC amplitude. Addnl., BTA-EG₄ requires APP to regulate dendritic spine d. through a Ras signaling-dependent mechanism. Thus, BTA-EG₄ may provide broad therapeutic benefits for improving neuronal and cognitive function, and may have implications in neurodegenerative disease therapy.

Journal of Neuroscience 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, Name: 2-(4-Aminophenyl)-6-methylbenzothiazole.

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

Park, Hokoon published the artcileSynthesis and biological activities of C-3 heterocyclyl carbon-substituted new cephalosporins, Name: 2-(Methylthio)thiazole, the publication is Journal of Antibiotics (1994), 47(5), 606-8, database is CAplus and MEDLINE.

Title compounds I [R = (un)substituted 2-thienyl, 5-thiazolyl, 2-pyrrolyl, 2-furyl, 5-isoxazolyl] were prepared via reaction of 3-chloromethyl-7-phenylacetamidocephem with RSnBu₃ and transacylation. Most I were superior to cefixime against gram-pos. organisms, but were inactive against Klebsiella aerogenes, Pseudomonas aeruginosa, and Enterobacter cloacae.

Journal of Antibiotics 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, Name: 2-(Methylthio)thiazole.

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

Tomczyk, Danuta published the artcileApplication of column chromatography in the analysis of intermediates and dyes. III. Photometric determination of dehydrothio-p-toluidine in crude product, Related Products of thiazole, the publication is Chemia Analityczna (Warsaw, Poland) (1974), 19(6), 1247-51, database is CAplus.

Crude dehydrothio-p-toluidine (I) [92-36-4] dissolved in EtOH was separated by chromatog. on a cellulose powder column with EtOH as the mobile phase followed by photometric determination of collected I at 460 nm after its reaction with p-Me2NC6H4CHO. Standard deviation was 0.75% for the crude product containing 65% I and time of determination was 2.5 hr.

Chemia Analityczna (Warsaw, Poland) 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 C4H8F3NO, Related Products of thiazole.

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

Korobkov, V. S. published the artcileElectronic spectra of 2,1,3-benzothiadiazole and its derivatives, Recommanded Product: 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine, the publication is Spektroskopiya, Metody i Primenenie, Akad. Nauk SSSR, Sibirsk. Otd. (1964), 130-1, database is CAplus.

The ultraviolet absorption spectra, 2110-4400 A., were obtained for 2,1,3-benzothiadiazole, 4,7-dibromo-, 4-amino-5-chloro-, 4-amino-5-bromo-, 4-amino-5,7-dichloro-, 4-amino-5,7-dibromo-, and tetrabromotetrahydro-2,1,3-benzothiazole, 3′,4′-dichlorohydro-1,2-naphth-1,2,3-thiadiazole, and 4′-chloro-1′,2′-naphth-2,1,3-thiadiazole. In general, the typical spectra of condensed aromatic rings were found.

Spektroskopiya, Metody i Primenenie, Akad. Nauk SSSR, Sibirsk. Otd. published new progress about 30536-19-7. 30536-19-7 belongs to thiazole, auxiliary class Other Aromatic Heterocyclic,Chloride,Amine, name is 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine, and the molecular formula is C6H4ClN3S, Recommanded Product: 5-Chlorobenzo[c][1,2,5]thiadiazol-4-amine.

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

Mishra, Chandra Bhushan published the artcileDiscovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations, HPLC of Formula: 95-24-9, the publication is Journal of Medicinal Chemistry (2021), 64(6), 3100-3114, database is CAplus and MEDLINE.

Two sets of benzenesulfonamide-based effective human carbonic anhydrase (hCA) inhibitors have been developed using the tail approach. The inhibitory action of these novel mols. was examined against four isoforms: hCA I, hCA II, hCA VII, and hCA XII. Most of the mols. disclosed low to medium nanomolar range inhibition against all tested isoforms. Some of the synthesized derivatives selectively inhibited the epilepsy-involved isoforms hCA II and hCA VII, showing low nanomolar affinity. The anticonvulsant activity of selected sulfonamides was assessed using the maximal electroshock seizure (MES) and s.c. pentylenetetrazole (s.c.-PTZ) in vivo models of epilepsy. These potent CA inhibitors effectively inhibited seizures in both epilepsy models. The most effective compounds17(I) and 22(II) showed long duration of action and abolished MES-induced seizures up to 6 h after drug administration. These sulfonamides were found to be orally active anticonvulsants, being nontoxic in neuronal cell lines and in animal models.

Journal of Medicinal Chemistry 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, HPLC of Formula: 95-24-9.

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

Kain, Dolly published the artcileMetabolic characterization, antioxidant capacity, and In vitro antiurolithiatic potential of Achillea millefolium L., Computed Properties of 30931-67-0, the publication is Journal of Young Pharmacists (2021), 13(3), 211-216, database is CAplus.

The current study investigated the antioxidant and antiurolithiatic potential of A. millefolium along with its metabolic characterization. A. millefolium has been collected at vegetative (V) and mature (Inflorescence (I) and Stem and Leaves (S+L)) stages and extracted in ethanol. Antioxidant potential has been determined by total phenolic content, total flavonoid content, ferric reducing antioxidant potential, total antioxidants through phosphomolybdate assay and free radical scavenging assays (1,1-diphenyl-2-picrylhydrazyl) and 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid). In vitro antiurolithiatic activity is determined by turbidity changes in artificial urine, nucleation assay, and aggregation assay. Fourier transform-IR spectroscopy and gas chromatog.-mass spectrometry has been used to characterize the active metabolites of plant A. millefolium. Maximum antioxidant activity was observed in Inflorescence with values 76.58 mg of GAE/g of extract, 18.82 mg of RE/g of extract, 199.799 mg of AAE/g of extract and 327.95 mg of AAE/g of extract for TPC, TFC, FRAP and total antioxidants through phosphomolybdate assay resp. Maximum radical scavenging activity was also observed in inflorescence with 86.3% and 69.655 % inhibition against DPPH and ABTS free radicals at 1000μg/mL concentration resp. Maximum in vitro antiurolithiatic potential of plant A. millefolium observed in inflorescence i.e. 80 %, 41.84% and 63.41 % inhibition at 1000μg/mL concentration for turbidity changes in artificial urine method, nucleation assay and aggregation assay resp. FT- IR and GCMS of inflorescence of A. millefolium confirmed the presence of major functional groups and active metabolic compounds resp. Inflorescence of plant A. millefolium is an excellent source of natural antioxidants with significant antiurolithiatic potential.

Journal of Young Pharmacists 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, Computed Properties of 30931-67-0.

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

Shrivastava, A. K. published the artcile2-Amino-4-arylthiazoles and their thiazolylamides as antifungal agents. 1, Recommanded Product: 4-(Naphthalen-1-yl)thiazol-2-amine, the publication is Journal of the Institution of Chemists (India) (1997), 69(4), 113-115, database is CAplus.

Thirty-six title compounds were prepared by standard procedures and their fungicidal activity tested against Fusarium solani. The amides showed greater fungitoxicity than the parent thiazoles in all cases.

Journal of the Institution of Chemists (India) published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C25H47NO8, Recommanded Product: 4-(Naphthalen-1-yl)thiazol-2-amine.

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

Shrivastava, A. K. published the artcileSyntheses of some 2-amino-4-(aryl/substituted aryl)thiazoles and their thiazolylamides as potential antifungal agents. II, Product Details of C13H10N2S, the publication is Journal of the Institution of Chemists (India) (1997), 69(6), 167-168, database is CAplus.

Thiazolylamides I [R¹ = (un)substituted Ph, 1-naphthyl, 1-hydroxy-2-naphthyl, 4-nitroanilino; R² = 2-HOC₆H₄CO, PhCH₂CO, ClCH₂CO, 3-MeC₆H₄CO, p-xylene-2-sulfonyl] were prepared by reaction of I (same R¹, R² = H) with acid chlorides. The amides were tested for fungicidal and bactericidal activity.

Journal of the Institution of Chemists (India) published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C18H10, Product Details of C13H10N2S.

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

Muthyala, Manoj Kumar published the artcileA novel and efficient one pot synthesis of 2,4-disubstituted thiazoles and oxazoles using phenyltrimethylammonium tribromide in ionic liquid, SDS of cas: 56503-96-9, the publication is Journal of Heterocyclic Chemistry (2012), 49(4), 959-964, database is CAplus.

A novel and efficient 1-pot procedure was described for synthesis of 2,4-disubstituted thiazoles and oxazoles from substituted ketones using phenyltrimethylammonium tribromide as in-situ brominating agent followed by reaction with thioamide/thiourea and amides/ureas, resp. in [bmim][BF₄] ionic liquid The advantages of the procedure include avoiding the handling of lacrymetric compounds and hazardous and toxic organic solvents along with good to excellent yields of the products.

Journal of Heterocyclic Chemistry published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C13H10N2S, SDS of cas: 56503-96-9.

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