Heterocyclic Building Blocks-Thiazole

Lan, Xiaohao published the artcileScreening and identification of Lassa virus endonuclease-targeting inhibitors from a fragment-based drug discovery library, HPLC of Formula: 95-24-9, the publication is Antiviral Research (2022), 105230, database is CAplus and MEDLINE.

Lassa virus (LASV) belongs to the Old World genus Mammarenavirus, family Arenaviridae, and order Bunyavirales. Arenavirus contains a segmented neg.-sense RNA genome, which is in line with the bunyavirus and orthomyxoviruses. The segmented neg.-sense RNA viruses utilize a cap-snatching strategy to provide primers cleavaged from the host capped mRNA for viral mRNA transcription. As a similar strategy and the conformational conservation shared with these viruses, the endonuclease (EN) would serve as an attractive target for developing broad-spectrum inhibitors. Using the LASV minigenome (MG) system, we screened a fragment-based drug discovery library and found that two hits, F1204 and F1781, inhibited LASV MG activity. Both hits also inhibited the prototype arenavirus Lymphocytic choriomeningitis virus (LCMV) MG activity. Furthermore, both hits effectively inhibited authentic LCMV and severe fever with thrombocytopenia syndrome virus (SFTSV) infections. Similarly, both hits could inhibit the activity of LASV, LCMV, and SFTSV EN. The combination of either compound with an arenavirus entry inhibitor had significant synergistic antiviral effects. Moreover, both hits were found to be capable of binding to LASV EN with a binding affinity at the micromolar level. These findings provide a basis for developing the hits as potential candidates for the treatment of segmented neg.-sense RNA virus infections.

Antiviral Research 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

Guan, Ai-jiao published the artcileEthyl-substitutive Thioflavin T as a highly-specific fluorescence probe for detecting G-quadruplex structure, Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Scientific Reports (2018), 8(1), 1-12, database is CAplus and MEDLINE.

G-quadruplex has attracted considerable attention due to their prevalent distribution in functional genomic regions and transcripts, which can importantly influence biol. processes such as regulation of telomere maintenance, gene transcription and gene translation. Artificial receptor study has been developed for accurate identification of G-quadruplex from DNA species, since it is important for the G-quadruplex related basic research, clin. diagnosis, and therapy. Herein, fluorescent dye ThT-E, a derivative of the known fluorescence probe Thioflavin T (ThT), was designed and synthesized to effectively differentiate various G-quadruplex structures from other nucleic acid forms. Compared with Me groups in ThT, three Et groups were introduced to ThT-E, which leads to strengthened affinity, selectivity and little inducing effect on the G-quadruplex formation. More importantly, ThT-E could be served as a visual tool to directly differentiate G-quadruplex solution even with naked eyes under illumination of UV light. Thus, this probe reported herein may hold great promise for high-throughput assay to screen G-quadruplex, which may widely apply to G-quadruplex-based potential diagnosis and therapy.

Scientific Reports 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, Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole.

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

Li, Ai-Tao published the artcileIsolation of Rhodococcus sp. strain ECU0066, a new sulfide monooxygenase-producing strain for asymmetric sulfoxidation, Related Products of thiazole, the publication is Applied and Environmental Microbiology (2009), 75(2), 551-556, database is CAplus and MEDLINE.

A new and efficient sulfide monooxygenase-producing strain, ECU0066, was isolated and identified as a Rhodococcus sp. that could transform phenylmethyl sulfide (PMS) to (S)-sulfoxide with 99% enantiomeric excess via two steps of enantioselective oxidations Its enzyme activity could be effectively induced by adding PMS or phenylmethyl sulfoxide (PMSO) directly to a rich medium at the early log phase (6 h) of fermentation, resulting in over 10-times-higher production of the enzyme. This bacterial strain also displayed fairly good activity and enantioselectivity toward seven other sulfides, indicating a good potential for practical application in asym. synthesis of chiral sulfoxides.

Applied and Environmental Microbiology 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, Related Products of thiazole.

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

Liu, Dengyue published the artcileFirst Discovery of Novel Pyrido[1,2-a]pyrimidinone Mesoionic Compounds as Antibacterial Agents, COA of Formula: C4H3Cl2NS, the publication is Journal of Agricultural and Food Chemistry (2019), 67(43), 11860-11866, database is CAplus and MEDLINE.

Plant bacterial diseases cause tremendous decreases in crop yield and quality, and there is a lack of highly effective and low-risk antibacterial agents. A series of novel pyrido[1,2-a]pyrimidinone mesoionic compounds containing vanillin moieties were synthesized, and the application of these mesoionic compounds as plant antibacterial agents was reported here for the first time. The bioassay results revealed that the mesoionic compounds had good antibacterial activity. Of these compounds, compound (I) showed excellent in vitro activity against Xanthomonas oryzae pv. oryzae, with an EC₅₀ value of 1.1μg/mL, which was substantially better than that of bismerthiazol (92.7μg/mL) and thiodiazole copper (105.4μg/mL). Moreover, greenhouse condition trials indicated that the protective and curative activities of compound I against rice bacterial leaf blight were 75.12% and 72.04%, resp., which were better than those of bismerthiazol (62.24% and 50.83%, resp.) and thiodiazole copper (53.35% and 65.04%, resp.). These results provide a basis for the application of mesoionic vanillin moieties as new antibacterial agents.

Journal of Agricultural and Food Chemistry published new progress about 50398-77-1. 50398-77-1 belongs to thiazole, auxiliary class Thiazoles, name is 5-Chloro-2-(chloromethyl)-1,3-thiazole, and the molecular formula is C4H3Cl2NS, COA of Formula: C4H3Cl2NS.

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

Szponder, Tomasz published the artcileEffects of topical treatment of foot rot in sheep using ozonated olive ointment, Safety of Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate), the publication is Journal of Veterinary Research (2021), 65(3), 369-374, database is CAplus and MEDLINE.

Foot rot in small ruminants is highly contagious, causes severe lameness, and impairs fertility and wool and meat production It is usually treated with parenteral antibiotics, with attendant antibiotic resistance risk, and with bactericidal footbaths, potentially harmful to humans and the environment. An alternative treatment in sheep is proposed based on repeated topical ozonated ointment application. Its effectiveness and safety were evaluated by estimation of acute-phase response, biochem. indicators of organic damage, and antioxidant/oxidant balance (AOB). The study was conducted on ten sheep with Egerton scale 2-3 lesions. Ozone application was repeated every day for seven days. Blood was drawn first (T0) after foot cleaning and before ozonation, then (T1) seven days after the first ozone application, and finally (T2) four days after the last application. High clin. effectiveness was observed, with total recovery by 28 days from the start of treatment. A significant increase in antiradical activity was noted on the basis of a 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assay from 1.16 ± 0.04 μmolTe/mL at T0 to 1.23 ± 0.03 μmolTe/mL at T1, with a slight decrease in oxidative stress. Calculated on the basis of antiradical capacity, AOB was higher at T1 (130 ± 19%) and decreased to 110 ± 16% at T2. Calculated on the basis of reducing power, it was 169 ± 22% at T1 and 131 ± 17% at T2. These results indicated that the AOB is efficient enough to prevent oxidative organ injury and the applied doses of ozone are safe for animals.

Journal of Veterinary Research 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 C6H9N3O2S, Safety of Ammonium 2,2′-(hydrazine-1,2-diylidene)bis(3-ethyl-2,3-dihydrobenzo[d]thiazole-6-sulfonate).

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

Yanachkov, Ivan published the artcileSelf-neutralizing oligonucleotides with enhanced cellular uptake, Product Details of C5H7N3S3, the publication is Organic & Biomolecular Chemistry (2017), 15(6), 1363-1380, database is CAplus and MEDLINE.

There is tremendous potential for oligonucleotide (ON) therapeutics, but low cellular penetration due to their polyanionic nature is a major obstacle. We addressed this problem by developing a new approach for ON charge neutralization in which multiple branched charge-neutralizing sleeves (BCNSs) are attached to the internucleoside phosphates of ON by phosphotriester bonds. The BCNSs are terminated with pos. charged amino groups, and are optimized to form ion pairs with the neighboring phosphate groups. The new modified ONs can be prepared by standard automated phosphoramidite chem. in good yield and purity. They possess good solubility and hybridization properties, are not involved in non-standard intramol. aggregation, have low cytotoxicity, adequate chem. stability, improved serum stability, and above all, display significantly enhanced cellular uptake. Thus, the new ON derivatives exhibit properties that make them promising candidates for the development of novel therapeutics or research tools for modulation of the expression of target genes.

Organic & Biomolecular Chemistry published new progress about 1192027-04-5. 1192027-04-5 belongs to thiazole, auxiliary class Other Aliphatic Heterocyclic,Amine, name is N,N-Dimethyl-N’-(3-thioxo-3H-1,2,4-dithiazol-5-yl)formimidamide, and the molecular formula is C8H5IO, Product Details of C5H7N3S3.

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

Koperniku, Ana published the artcileThe Reaction of N -Trimethylsilyl-Substituted Heteroarylamines with Esters and Thioesters: An Efficient Protocol To Access Diheteroarylamides, Quality Control of 95-24-9, the publication is Synthesis (2019), 51(8), 1779-1790, database is CAplus.

The S-benzyl thioester and Me ester derivatives of a representative 4-pyridinone-based carboxylic acid were sufficiently activated to react efficiently in amide coupling reactions with the amide anion generated in situfrom the N-trimethylsilyl derivative of different weakly nucleophilic heteroarylamines. In acetonitrile as solvent, the precipitated diheteroarylamide products were isolated in pure form by vacuum filtration. This simple amide bond forming protocol can be readily adapted to the parallel synthesis of compound libraries.

Synthesis 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, Quality Control of 95-24-9.

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

Jamal Gilani, Sadaf published the artcileNovel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation, Computed Properties of 95-24-9, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(14), 1825-1830, database is CAplus and MEDLINE.

In the present study, a series of newer benzothiazole derivatives containing thiazolidin-4-one and azetidin-2-one, were synthesized by the cyclization of benzothiazolyl arylidene hydrazine carboxamide derivatives with thioglycolic acid and chloroacetyl chloride, resp. Results of in vivo anticonvulsant screening revealed that compounds I (R = 2,4-Cl₂, 4-NO₂) and II (R = 4-NO₂) have promising anticonvulsant activities without any neurotoxicity. Selected compounds were also evaluated for their in vitro GABA AT inhibition. The results indicated that compound I (R = 2,4-Cl₂, IC₅₀ 15.26 μM) exhibited excellent activity as compared to the standard drug vigabatrin (IC₅₀ 39.72 μM) suggesting the potential of these benzothiazole analogs as new anticonvulsant agents.

Bioorganic & Medicinal Chemistry Letters 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, Computed Properties of 95-24-9.

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

Jiang, Chen Hao published the artcileBioinformatics-based screening of key genes for transformation of liver cirrhosis to hepatocellular carcinoma, Computed Properties of 95-24-9, the publication is Journal of Translational Medicine (2020), 18(1), 40, database is CAplus and MEDLINE.

Abstract: Background: The aims of the present study were to identify key genes related to the transformation of cirrhosis into HCC, and explore the associated mol. mechanisms. Methods: GSE89377, GSE17548, GSE63898 and GSE54236 mRNA microarray datasets from Gene Expression Omnibus (GEO) were analyzed to obtain differentially expressed genes (DEGs) between HCC and liver cirrhosis tissues, and network anal. of protein-protein interactions (PPIs) was carried out. String and Cytoscape were used to analyze modules and identify hub genes, Kaplan-Meier Plotter and Oncomine databases were used to explore relationships between hub genes and disease occurrence, development and prognosis of HCC, and the mol. mechanism of the main hub gene was probed using Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway anal. Results: In total, 58 DEGs were obtained, of which 12 and 46 were up- and down-regulated, resp. Three hub genes (CDKN3, CYP2C9 and LCAT) were identified and associated prognostic information was obtained. CDKN3 may be correlated with the occurrence, invasion, and recurrence of HCC. Genes closely related to changes in the CDKN3 hub gene were screened, and Kyoto Encyclopedia of Genes and Genomes (KEGGs) pathway anal. identified numerous cell cycle-related genes. Conclusion: CDKN3 may affect the transformation of liver cirrhosis into HCC, and represents a new candidate mol. marker of the occurrence and progression of HCC.

Journal of Translational Medicine 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, Computed Properties of 95-24-9.

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

Wang, Junren published the artcileEosin Y as a high-efficient photooxidase mimic for colorimetric detection of sodium azide, Category: thiazole, the publication is Analytical and Bioanalytical Chemistry (2020), 412(27), 7595-7602, database is CAplus and MEDLINE.

Abstract: The reported fluorescent dye-based artificial light-responsive oxidase mimics are suffering from their low catalytic efficiency. To overcome the limitation, we report the photooxidase-mimicking activity of Eosin Y which can catalyze the oxidation of various chromogenic substrates such as 3,3′,5,5′-tetramethylbenzydine (TMB), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), 3,3′-diaminobenzidine (DAB), and o-phenylenediamine (OPD) by dissolved oxygen. The photooxidase-like activity of Eosin Y is highly efficient for TMB substrate, and its catalytic efficiency is higher than that of the reported fluorescein (130 fold) and 9-mesityl-10-methylacridinium ion (7.7-fold) mimetic photooxidase. Moreover, the photosensitized Eosin Y-TMB chromogenic system is utilized for colorimetric detection of highly toxic and explosive sodium azide (NaN₃) in a linear range from 5 to 500 μM with a limit of detection of 3.5 μM. The resulting colorimetric assay is selective and applied to determine NaN₃ in real lake water samples.

Analytical and Bioanalytical Chemistry 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 C40H35N7O8, Category: thiazole.

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