Day: November 21, 2022

Abdelhamid, Abdou O. published the artcileReactions with hydrazonoyl halides. XIII. Synthesis of some new thiadiazoline, arylazothiazole and pyrazole derivatives, COA of Formula: C13H10N2S, the publication is Phosphorus, Sulfur and Silicon and the Related Elements (1996), 181-191, database is CAplus.

Hydrazonoyl halide RCOCBr:NNHAr (I, R = 1-naphthyl, Ar = Ph, 4-MeC₆H₄, 4-ClC₆H₄) reacts with sodium thiophenolate and sodium benzenesulfinate to give the corresponding hydrazones. I also, reacts with thiourea, potassium thiocyanate and β-ketosulfones, to give arylazothiazoles II, thiadiazolines III, and pyrazole IV, resp. R’COCCl:NNHAr (R’ = OEt, Ar = Ph; R’ = Me, Ar = Ph, 4-MeC₆H₄, 4-ClC₆H₄; R’ = Ar = Ph) reacts with substituted thioanilide to afford pyrazoles V. The structures of the newly synthesized compounds were assigned and confirmed on the basis of their elemental analyses, spectral data and alternate synthesis whenever possible.

Phosphorus, Sulfur and Silicon and the Related Elements 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, COA of Formula: C13H10N2S.

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

Barilli, Alessio published the artcileFrom High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents, Application of 5-Chlorothiazole-2-ethanone, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5931-5955, database is CAplus and MEDLINE.

Transient receptor potential cation channel subfamily M member 5 (TRPM5) is a nonselective monovalent cation channel activated by intracellular Ca²⁺ increase. Within the gastrointestinal system, TRPM5 is expressed in the stoma, small intestine, and colon. In the search for a selective agonist of TRPM5 possessing in vivo gastrointestinal prokinetic activity, a high-throughput screening was performed and compound 1 was identified as a promising hit. Hit validation and hit to lead activities led to the discovery of a series of benzo[d]isothiazole derivatives Among these, compounds 61 and 64 showed nanomolar activity and excellent selectivity (>100-fold) vs. related cation channels. The in vivo drug metabolism and pharmacokinetic profile of compound 64 was found to be ideal for a compound acting locally at the intestinal level, with minimal absorption into systemic circulation. Compound 64 was tested in vivo in a mouse motility assay at 100 mg/kg, and demonstrated increased prokinetic activity.

Journal of Medicinal Chemistry published new progress about 774230-95-4. 774230-95-4 belongs to thiazole, auxiliary class Thiazole,Chloride,Aldehyde, name is 5-Chlorothiazole-2-ethanone, and the molecular formula is C5H4ClNOS, Application of 5-Chlorothiazole-2-ethanone.

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

Barilli, Alessio published the artcileFrom High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents, COA of Formula: C4H3Cl2NS, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5931-5955, database is CAplus and MEDLINE.

Transient receptor potential cation channel subfamily M member 5 (TRPM5) is a nonselective monovalent cation channel activated by intracellular Ca²⁺ increase. Within the gastrointestinal system, TRPM5 is expressed in the stoma, small intestine, and colon. In the search for a selective agonist of TRPM5 possessing in vivo gastrointestinal prokinetic activity, a high-throughput screening was performed and compound 1 was identified as a promising hit. Hit validation and hit to lead activities led to the discovery of a series of benzo[d]isothiazole derivatives Among these, compounds 61 and 64 showed nanomolar activity and excellent selectivity (>100-fold) vs. related cation channels. The in vivo drug metabolism and pharmacokinetic profile of compound 64 was found to be ideal for a compound acting locally at the intestinal level, with minimal absorption into systemic circulation. Compound 64 was tested in vivo in a mouse motility assay at 100 mg/kg, and demonstrated increased prokinetic activity.

Journal of Medicinal 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

Barilli, Alessio published the artcileFrom High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents, Category: thiazole, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5931-5955, database is CAplus and MEDLINE.

Transient receptor potential cation channel subfamily M member 5 (TRPM5) is a nonselective monovalent cation channel activated by intracellular Ca²⁺ increase. Within the gastrointestinal system, TRPM5 is expressed in the stoma, small intestine, and colon. In the search for a selective agonist of TRPM5 possessing in vivo gastrointestinal prokinetic activity, a high-throughput screening was performed and compound 1 was identified as a promising hit. Hit validation and hit to lead activities led to the discovery of a series of benzo[d]isothiazole derivatives Among these, compounds 61 and 64 showed nanomolar activity and excellent selectivity (>100-fold) vs. related cation channels. The in vivo drug metabolism and pharmacokinetic profile of compound 64 was found to be ideal for a compound acting locally at the intestinal level, with minimal absorption into systemic circulation. Compound 64 was tested in vivo in a mouse motility assay at 100 mg/kg, and demonstrated increased prokinetic activity.

Journal of Medicinal Chemistry published new progress about 101012-16-2. 101012-16-2 belongs to thiazole, auxiliary class Thiazole,Chloride,Carboxylic acid, name is 5-Chlorothiazole-2-carboxylic acid, and the molecular formula is C4H2ClNO2S, Category: thiazole.

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

Adeyemi, Kazeem D. published the artcileGrowth Performance, Carcass Traits, Muscle Fatty Acids, Intramuscular Fat, Cholesterol, and Antioxidant Status in Rabbits Supplemented with Kigelia pinnata Leaf Meal, Category: thiazole, the publication is European Journal of Lipid Science and Technology (2022), 124(8), 2200014, database is CAplus.

The effects of dietary Kigelia pinnata leaf (KPL) on growth, carcass, muscle fatty acids, antioxidant status, cholesterol, physicochem. properties, and sensory profile of Longissimus thoracis et lumburum (LTL) muscle in rabbits are investigated. Seventy-two, 32 d old male New Zealand rabbits (684 ± 18 g) are randomly assigned to diets containing either no KPL (KPL-0), 5% KPL (KPL-5) or 10% KPL (KPL-10) for eight weeks, and euthanized, and the LTL is refrigerated for 6 days. Dietary KPL does not influence growth performance and carcass cuts in rabbits. Abdominal fat is lower in KPL- rabbits than in the KPL-0 rabbits. Supplemented LTL has lower i.m. fat and cholesterol, and higher crude protein, polyphenol content, glutathione reductase, and catalase compared with the control LTL. Concentration of C18:3n-3, C22:6n-3, and C20:5n-3 is higher in supplemented LTL than the control LTL. Supplemented meat has lower cook loss than the KPL-0 meat at 24 h postmortem. The KPL-10 meat has higher redness and lower malondialdehyde content than other meats on d 6 postmortem. Juiciness and overall acceptance of the supplemented meat are higher than that of the KPL-0 meat. Supplementation with KPL-10 enhances muscle n-3 fatty acids, sensorial quality, and oxidative stability of rabbit meat. Rabbit meat is replete in n-6 polyunsaturated fatty acid (PUFA) but low in n-3 PUFA, which heightens its n-6/n-3 ratio. Higher n-6/n-3 PUFA intake can pose serious health risks to consumers. This suggests a need to ameliorate the n-3 PUFA of rabbit meat. Dietary KPL causes ‘147-184% increase in n-3 PUFA and a 66-77% decrease in n-6/n-3 ratio in rabbit meat. Moreover, KPL improves sensorial quality and oxidative stability and lowers i.m. fat and cholesterol content of rabbit meat. These results support the delivery of a healthier rabbit meat that responds to consumer demands. This study explicates the potential of KPL in ameliorating the nutritional value and sensory quality of rabbit meat.

European Journal of Lipid Science and Technology 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, Category: thiazole.

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

Jethava, Divya J. published the artcileDesign, synthesis, biological evaluation and computational study of novel triazolo[4,3-a]pyrazine analogues, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine, the publication is Journal of Molecular Structure (2019), 168-192, database is CAplus.

In search of suitable potent drug candidate, the design, synthesis, characterization, biol. activities and computation study of novel triazolo[4,3-a]pyrazine analogs was reported. The newly synthesized compounds were evaluated for their in vitro biol. activities such as anti-malarial, anti-tuberculosis, anti-bacterial and anti-fungal activities against plasmodium falciparum, H₃₇Rv, various bacterial and fungal strains, resp. The mol. docking study was carried out with enzyme aspartic proteinase zymogen proplasmepsin II from plasmodium falciparum to analyze their binding orientation in the active site of the aspartic proteinase enzyme. The best docking complex was subjected to mol. dynamics simulation to illustrate the stability of these complexes and the most prominent interactions during the simulated trajectory. ADMET properties of all the synthesized compounds to predict the pharmacokinetic properties for the selection of the active and bioavailability of compounds has been calculated

Journal of Molecular Structure 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

Goya-Jorge, Elizabeth published the artcileDiscovery of 2-aryl and 2-pyridinylbenzothiazoles endowed with antimicrobial and aryl hydrocarbon receptor agonistic activities, Application In Synthesis of 92-36-4, the publication is European Journal of Pharmaceutical Sciences (2020), 105386, database is CAplus and MEDLINE.

Benzothiazole is a privileged scaffold in medicinal chem. present in diverse bioactive compounds with multiple pharmacol. applications such as analgesic, anticonvulsant, antidiabetic, anti-inflammatory, anticancer and radioactive amyloidal imagining agents. We reported in this work the study of sixteen functionalized 2-aryl and 2-pyridinylbenzothiazoles as antimicrobial agents and as aryl hydrocarbon receptor (AhR) modulators. The antimicrobial activity against Gram-pos. (S. aureus and M. luteus) and Gram-neg. (P. aeruginosa, S. enterica and E. coli) pathogens yielded MIC ranging from 3.13 to 50μg/mL and against the yeast C. albicans, the benzothiazoles displayed MIC from 12.5 to 100μg/mL. All compounds showed promising antibiofilm activity against S. aureus and P. aeruginosa. The arylbenzothiazole 12 displayed the greatest biofilm eradication in S. aureus (74%) subsequently verified by fluorescence microscopy. The ability of benzothiazoles to modulate AhR expression was evaluated in a cell-based reporter gene assay. Six benzothiazoles (7, 8-10, 12, 13) induced a significant AhR-mediated transcription and interestingly compound 12 was also the strongest AhR-agonist identified. Structure-activity relationships are suggested herein for the AhR-agonism and antibiofilm activities. Furthermore, in silico predictions revealed a good ADMET profile and druglikeness for the arylbenzothiazole 12 as well as binding similarities to AhR compared with the endogenous agonist FICZ.

European Journal of Pharmaceutical Sciences 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 In Synthesis of 92-36-4.

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

Shehata, Mohamed G. published the artcileOptimization conditions of ultrasound-assisted extraction of phenolic compounds from orange peels using response surface methodology, SDS of cas: 30931-67-0, the publication is Journal of Food Processing and Preservation (2021), 45(10), e15870, database is CAplus.

This study focused on optimizing the extraction conditions of bioactive compounds from orange peels using response surface methodol. (RSM) to decrease the number of exptl. trials and increase the yield of bioactive compounds Ultrasonic extraction time, extraction temperature, and ethanol concentration have been optimized. Twenty exptl. trials have been carried out to optimize the extraction conditions. The RSM results showed that the extraction temperature and ethanol concentration had a remarkable effect on the total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity. The optimal ultrasound-assisted extraction conditions were 44 min extraction time, 50°C extraction temperature, and 57.7% ethanol concentration Under these optimal conditions, TPC and TFC were 292.158μg GAE/g and 191.144μg catechol/g, resp., whereas antioxidant activities were 5.199 and 2.96μg/mL for 2,2-diphenyl-1-picrylhydrazyl and 2,20-azino-bis(3-ethylbenzothiazoline-60-sulfonic acid) diammonium salt, resp. RSM saves the extraction time and effective for optimizing extraction conditions with the highest efficiency and yield. The findings of the current work emphasized usefulness of ultrasound assisted extraction for elevation the extraction efficiency with decreasing the extraction time. The extraction temperature and ethanol concentration are the main effective factors of extraction efficiency. The optimal extraction time was 44 min at 50°C extraction temperature, and the optimal ethanol concentration was 57.7%. These optimal conditions were giving the highest yield of TPC and TFC that were 292.158μg GAE/g and 191.144μg catechol/g. These novel optimized extraction conditions could be useful in different food and pharmaceutical applications.

Journal of Food Processing and Preservation 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 C13H15NO6S, SDS of cas: 30931-67-0.

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

Al-Hamdani, Uhood J. published the artcileChloro-benzothiazole Schiff base ester liquid crystals: synthesis and mesomorphic investigation, Safety of 6-Chlorobenzothiazol-2-ylamine, the publication is Liquid Crystals, database is CAplus.

Nine new rod-like chlorobenzothiazole based liquid crystals – containing Schiff base and ester linking groups bearing different terminal substituents I [R = H, Cl; R¹ = (4-methoxyphenyl), nonyl, (4-octylsulfanylphenyl), etc.] and II [R² = acetyl, ethoxycarbonyl, [(3,4,5-trimethoxyphenyl)methyleneamino], etc.] were described. Although a few similar chloro substituted benzothiazole compounds were known, none was studied for their liquid crystal properties. All these compounds I and II possess liquid crystal behavior except compds I [R = Cl; R¹ = (3,4,5-trimethoxyphenyl)] and II [R² = [(3,4,5-trimethoxyphenyl)methyleneamino]]. The effect of the nature of the terminal groups on thermal stability and optical properties of the mesomorphic compounds I and II was evaluated. With the exception of compound I [R = H; R¹ = (4-octylsulfanylphenyl)] , all the other compounds possess polarity resulting from the polar chloride atom substituted at position-6 of the benzene ring of the benzothiazole moiety which provides a polar group at the one terminal end of the mols. The presence of the fused-ring system (benzothiazole) adds a mol. width that contributes to increase the mol. breadth, causing a thickening effect which disrupts the liquid crystalline packing. New compounds I and II were prepared via reaction of phenolic Schiff bases with the corresponding carboxylic acids or the carboxyl Schiff bases with the corresponding phenols. The synthesized compounds I and II were characterized using ¹H- and ¹³C-NMR and FT-IR spectroscopy, mass spectrometry and elemental anal. Polarised optical microscope and thermal properties were measured to study the thermal and mesophase behaviors.

Liquid Crystals 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, Safety of 6-Chlorobenzothiazol-2-ylamine.

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

P, Keerthana published the artcileAn Efficient Inclusion Complex Based Fluorescent Sensor for Mercury (II) and its Application in Live-Cell Imaging, Recommanded Product: 6-Chlorobenzothiazol-2-ylamine, the publication is Journal of Fluorescence (2022), 32(3), 1109-1124, database is CAplus and MEDLINE.

The formation of an inclusion complex between hydroxypropyl-β-cyclodextrin (H-CD) and 4-acetylphenyl-4-(((6-chlorobenzo[d]thiazol-2-yl)-imino)-methyl)-benzoate (L) was investigated by FT-IR, 1H-NMR, X-ray diffraction (XRD), FT-Raman, scanning electron microscope (SEM) techniques in the solid-state, absorption and emission spectroscopy in the liquid state and the virtual state as mol. docking technique. The binding properties of the inclusion complex (H-CD: L) with cations in deionized water was observed via absorbance and photoluminescence (PL) emission spectroscopy. The fluorescence probe (H-CD: L) inclusion complex (IC) was examined for several heavy metal cations, and identified that the PL emission wavelength of the complex displayed a continuous rise in the fluorescence intensity for Hg2+. A linearity range of 1 x 10-8 – 11 x 10-8 M and limit of detection value of 2.71 x 10-10 M was found to be achieved for the detection of Hg2+. This outcome proves that the inclusion complex H-CD: L would be a promising material for the development a solid-state fluorescence probe for detecting Hg2+. It also shows application in real sample anal. and cell imaging.

Journal of Fluorescence 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