Day: September 21, 2022

Xu, Jing;Gao, Liangqin;Liang, Huiqing;Chen, Shao-dong published 《In silico screening of potential anti-COVID-19 bioactive natural constituents from food sources by molecular docking》 in 2021. The article was appeared in 《Nutrition (New York, NY, United States)》. They have made some progress in their research.Application of 55981-09-4 The article mentions the following:

The aim of this study was to seek potential natural compounds that can resist COVID-19 using computer virtual screening technol. through mol. docking of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL hydrolytic enzyme (3CL^pro) and angiotensin-converting enzyme 2 (ACE2). Mol. docking was achieved by using the Autodock Vina software. The natural phytocompounds acting on 3CL^pro and ACE2 were then selected from the Traditional Chinese Medicine Systems Pharmacol. Database and Anal. Platform. This was followed by speculation on the mechanism of action of phytocompounds. Six potential natural anti-COVID-19 phytocompounds were selected and were evaluated for absorption, distribution, metabolism and excretion (ADME) and Lipinski rules. The content of the six phytocompounds in various fruits and vegetables was determined via a literature search. Red wine, Chinese hawthorn, and blackberry were recommended as supplements because they contained antiviral phytocompounds. Red wine, Chinese hawthorn, and blackberry show promise for resisting COVID-19 and are thus recommended as supplements to prevent the infection of COVID-19 during its outbreak period. To complete the study, the researchers used 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4) has been approved as an orphan drug for the treatment of diarrhea in children (age, 1–11 years) and is associated with giardiasis, but it also is approved for diarrhea caused by crytosporidiosis in patients with AIDS.Application of 55981-09-4

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

Chidrawar, Anil B. published 《Antifungal activity of pyrimido benzothiazole derivatives by disc diffusion method》 in 2018. The article was appeared in 《World Journal of Pharmaceutical Research》. They have made some progress in their research.Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

2-Substituted derivatives of 3-Cyano-4-imino-2-methylthio-8-nitro-4H-pyrimido [2,1-b] [1,3] benzothiazole obtained by the multicomponent reaction of 2-amino-6-nitro benzothiazole and bis methylthio methylene malononitrile on refluxed independently with aryl amines / phenols / heteryl amines / compounds containing active methylene group in the presence of 5 mL of DMF with a pinch of anhydrous K₂CO₃.6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) were involved in the experimental procedure.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine) is an antimicrobial agent that inhibits bacterial growth by cleaving the peptide bonds of proteins. It has been shown to be active against a number of microorganisms, including Gram-positive and Gram-negative bacteria, as well as fungi.

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

Formula: C7H5N3O2SIn 2021, Mikherdov, Alexander S.;Popov, Roman A.;Kinzhalov, Mikhail A.;Haukka, Matti;Polukeev, Valeriy A.;Boyarskiy, Vadim P.;Roodt, Andreas published 《Reaction mechanism of regioisomerization in binuclear (diaminocarbene)Pd^II complexes》. 《Inorganica Chimica Acta》published the findings. The article contains the following contents:

A series of binuclear Pd^II carbene complexes were synthesized via the treatment of cis-[PdCl₂(CNXyl)₂] (1) with benzo-1,3-thiazol-2-amines (2–6) and structurally characterized. In every case the reaction leads to the mixture of two regioisomers, which are able to interconvert. The study of the regioisomerization of the binuclear diaminocarbene species showed that it is a first-order reaction, i.e., it occurs intramolecularly, and was analyzed with the Hammett function. Electron-withdrawing substituents in the benzothiazole moiety of the complexes as well as increasing the solvent polarity accelerate the reaction. The solvent donor strength correlates less well with the isomerization rates. Based on the obtained activation parameters the studied regioisomerization could be defined as the interchange/dissociative process type. A combined approach including kinetic and mass spectrometric studies allowed the conclusion that the rate-determining step of the isomerization is breaking the carbon-nitrogen bond in the carbene fragment of the binuclear complex. The experimental procedure involved many compounds, such as 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Formula: C7H5N3O2S) is an antimicrobial agent that inhibits bacterial growth by cleaving the peptide bonds of proteins. It has been shown to be active against a number of microorganisms, including Gram-positive and Gram-negative bacteria, as well as fungi.

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

Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2022, Prathapan, Praveen published 《A determination of pan-pathogen antimicrobials?》. 《Medicine in Drug Discovery》published the findings. The article contains the following contents:

A review. While antimicrobial drug development has historically mitigated infectious diseases that are known, COVID-19 revealed a dearth of ‘in-advance’ therapeutics suitable for infections by pathogens that have not yet emerged. Such drugs must exhibit a property that is antithetical to the classical paradigm of antimicrobial development: the ability to treat infections by any pathogen. Characterization of such ‘pan-pathogen’ antimicrobials requires consolidation of drug repositioning studies, a new and growing field of drug discovery. In this review, a previously-established system for evaluating repositioning studies is used to highlight 4 therapeutics which exhibit pan-pathogen properties, namely azithromycin, ivermectin, niclosamide, and nitazoxanide. Recognition of the pan-pathogen nature of these antimicrobials is the cornerstone of a novel paradigm of antimicrobial development that is not only anticipatory of pandemics and bioterrorist attacks, but cognisant of conserved anti-infective mechanisms within the host-pathogen interactome which are only now beginning to emerge. Ultimately, the discovery of pan-pathogen antimicrobials is concomitantly the discovery of a new class of antivirals, and begets significant implications for pandemic preparedness research in a world after COVID-19. To complete the study, the researchers used 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Kachare, Snehal D.;Baheti, Kamalkishor G.;Yasar, Qazi;Jangam, Sampada S. published 《Design, synthesis and evaluation of benzothiazole urea derivatives as an anticonvulsant agent》 in 2021. The article was appeared in 《Pharma Chemica》. They have made some progress in their research.Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

A series of 1-((-6-substituted-2-yl)-3-(4H-1,2,4 triazole-3-yl))ureas I (R = H, OMe, Cl, NO₂, etc.) and (1-((3-(6-substituted-2-yl)ureido)methyl)cyclohexyl)acetic acids II were designed, synthesized using appropriate synthetic route and screened for CNS depressant and anticonvulsant activities. The synthesized compounds I and II were also analyzed for ADME properties. The results of In-Silico ADME Screening showed that compounds I and II could be exploited as an oral drug candidate. Mol. docking studies were performed for all the synthesized compounds I and II against γ-amino butyric acid amino transferase enzyme (1OHV), and all the compounds I and II exhibited docking score in the range of -7.5 to -8.4, among which compound II (R = Cl) had shown the highest docking scores as compared to the standard drug phenytoin. Animal study for anticonvulsant indicated that compounds I (R = NO₂, H) and II (R = Cl) were exhibited significant activity at a dose 200 mg/kg. All these compounds I and II were also evaluated for CNS depressant activity using actophotometer. The results of CNS depressant and anticonvulsant activities and docking study showed that synthesized compounds I and II had potential CNS depressant and anticonvulsant activities and can be further optimized and developed as a lead compound And 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) was used in the research process.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine) inhibits the activity of amines, which are small molecules found in many pharmaceuticals. The chemical structure of this drug contains one or more methylene groups that can be activated by diazonium salt to form an intermediate molecule with a reactive amine group.

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

Singh, Abhishek Kumar;Kewalramani, Neelam;Mani, Veena;Sharma, Amit;Kumari, Punita;Pal, Ravi Prakash published 《Effects of boric acid supplementation on bone health in crossbred calves under tropical condition》 in 2021. The article was appeared in 《Journal of Trace Elements in Medicine and Biology》. They have made some progress in their research.Category: thiazole The article mentions the following:

Boron (B) is thought to play key role in proper bone growth and development as well as have some role in regulation of minerals such as calcium (Ca), phosphorus (P) and magnesium (Mg) which act synergistically with vitamin D. Present study was planned in two phases to assess the effect of optimum and supranutritional levels of (B) in the form of boric acid (BA) supplementation on bone health of growing cross bred calves. During Phase-1, twenty four male crossbred calves were blocked into four groups (n = 6) on the basis of their body weight (154.83 ± 8.5 kg), age (7-9 mo) and were supplemented with 0 (C), 2.6 (T-1), 5.4 (T-2) and 10.7 (T-3) g BA for appropriate B (0.175 adjustment factor to calculate B form BA) consumption i.e. 0, 100, 200 and 400 ppm in each group resp., for 90 days. During phase 2, twenty-one male crossbred calves were divided into 3 groups (n = 7) on the basis of their body weight (103.76 ± 4.34 kg) and age (5-8 mo). All the groups were on similar dietary regimen with addnl. supplementation of boric acid as 0 g (control); 3.6 g (200 ppm B; T-1) and 10.8 g (600 ppm B; T-2), resp. for a period of 120 d. From the first experiment it is reported that plasma levels of bovine alk. phosphatase (BALP), type I collagen crosslinked N-telopeptide (NTx) and Ca were significantly (P < 0.05) affected in T-2 and T-3 groups as compared to T-1 and control groups. Whereas, plasma osteocalcin (OCN) concentration was found to be higher in T-2 and T-3 groups as compared to control group. However, plasma concentrations (ng/mL) of tartrate resistant acid phosphatase (TRAP) remained unaltered due to dietary treatments. Based on the results, another experiment was conducted to validate the above findings and further to determine the effect of still higher i.e supranutritional levels of BA supplementation on bone health of calves. Results revealed that supplementation of BA in T-2 group had no beneficial effect on bone health as the plasma concentration of BALP, OCN, NTx, 25 (OH) vitamin D and Ca as compared to T-1 group in phase 2. Other possible attributes of bone health i.e. plasma concentration of Mg, P, parathyroid hormone (PTH), and calcitonin were not affected by BA supplementation at any levels. Overall from present study it can be concluded that supplementation of boric acid 3.6 g/d (equivalent to 200 ppm B) in the diet of growing animals has pos. effect on bone health related biomarkers (OCN, NTx and BALP) and supplementation of supranutritional level of BA i.e. 10.8 g (equivalent to 600 ppm B) level had neither addnl. beneficial nor harmful effect on bone health of calves. And 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) was used in the research process.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Category: thiazole

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

Quality Control of 6-Nitrobenzo[d]thiazol-2-amineIn 2020, Pugh, Kyler W.;Zhang, Zheng;Wang, Jian;Xu, Xiuzhi;Munthali, Vitumbiko;Zuo, Ang;Blagg, Brian S. J. published 《From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition》. 《ACS Medicinal Chemistry Letters》published the findings. The article contains the following contents:

Heat shock protein 90 (Hsp90) is a mol. chaperone that is responsible for the folding and maturation of client proteins that are associated with all ten hallmarks of cancer. Hsp90 N-terminal pan inhibitors have experienced unfavorable results in clin. trials due to induction of the heat shock response (HSR), among other concerns. Novobiocin, a well characterized DNA gyrase B inhibitor, was identified as the first Hsp90 C-terminal inhibitor that manifested anticancer effects without induction of the HSR. In this letter, a library of Hsp90 C-terminal inhibitors derived from a benzothiazole-based scaffold, known to inhibit DNA gyrase B, was designed, synthesized, and evaluated. Several compounds were found to manifest low micromolar activity against both MCF-7 and SKBr3 breast cancer cell lines via Hsp90 C-terminal inhibition.6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) were involved in the experimental procedure.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Quality Control of 6-Nitrobenzo[d]thiazol-2-amine) inhibits the activity of amines, which are small molecules found in many pharmaceuticals. The chemical structure of this drug contains one or more methylene groups that can be activated by diazonium salt to form an intermediate molecule with a reactive amine group.

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

Kallur, H. J.;Mathapati, Prabhudev S.;C., Kishore Singh;Malpani, Ashok published 《Synthesis, characterization and anthelmintic screening of some new benzothiophene derivatives》 in 2020. The article was appeared in 《World Journal of Pharmaceutical Research》. They have made some progress in their research.Recommanded Product: 6285-57-0 The article mentions the following:

The proposed work was carried out by following Schemes. In the Scheme-I the starting material cinnamic acid was reacted with thionyl chloride, in presence of pyridine in chlorobenzene medium to yield 3- chlorobenzo[b]thiophene-2-carbonylchloride. Where as in the Scheme-II the 2-amino-6-substituted benzothiazoles I (R = Me, COOEt, Cl, OMe, F, nitro) was prepared by the reaction of 4-substituted anilines 4-RC₆H₄NH₂ and potassium thiocyanate in presence of bromine in acetic acid. In the scheme-III, the compound N-(6-substituted-1,3-benzothiazol-2-yl)-3-chloro-1-benzothiophene-2-carboxamides II was prepared by reacting 3-chlorobenzo[b]thiophene-2-carbonylchloride and 2-amino-6-substituted benzothiazoles I in pyridine medium refluxed for 10-15 h. The synthesized compounds II were evaluated for the anthelmintic activity. And 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) was used in the research process.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Recommanded Product: 6285-57-0) inhibits the activity of amines, which are small molecules found in many pharmaceuticals. The chemical structure of this drug contains one or more methylene groups that can be activated by diazonium salt to form an intermediate molecule with a reactive amine group.

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

Upadhyay, Neha;Tilekar, Kalpana;Safuan, Sabreena;Kumar, Alan P.;Schweipert, Markus;Meyer-Almes, Franz-Josef;Ramaa, Cs published 《Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2》 in 2021. The article was appeared in 《Future Medicinal Chemistry》. They have made some progress in their research.Category: thiazole The article mentions the following:

Angiogenesis deregulation is often linked to cancer and is thus an essential target. Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity. B1, PB11 and PB16 showed HUVEC′s IC₅₀ scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range: 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies. These compounds can target VEGFR-2 and are endowed with in vitro and in vivo antiangiogenic activity. The experimental procedure involved many compounds, such as 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Category: thiazole) inhibits the activity of amines, which are small molecules found in many pharmaceuticals. The chemical structure of this drug contains one or more methylene groups that can be activated by diazonium salt to form an intermediate molecule with a reactive amine group.

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

Smith, Tania;Hoyo-Vadillo, Carlos;Adom, Akosua Agyeman;Favari-Perozzi, Liliana;Gastine, Silke;Dehbi, Hakim-Moulay;Villegas-Lara, Beatriz;Mateos, Eduardo;Gonzalez, Yessica Sara Perez;Navarro-Gualito, Maria D.;Cruz-Carbajal, Alejandra S.;Cortes-Vazquez, Miguel A.;Bekker-Mendez, Carolina;Aguirre-Alvarado, Charmina;Aguirre-Gil, Gisela;Delgado-Pastelin, Lucero;Owen, Andrew;Lowe, David;Standing, Joseph;Escobedo, Jorge published 《Favipiravir and/or nitazoxanide: a randomized, double-blind, 2×2 design, placebo-controlled trial of early therapy in COVID-19 in health workers, their household members, and patients treated at IMSS (FANTAZE)》 in 2022. The article was appeared in 《Trials》. They have made some progress in their research.Formula: C12H9N3O5S The article mentions the following:

Abstract: Background: The 2020 pandemic of SARS-CoV-2 causing COVID-19 disease is an unprecedented global emergency. COVID-19 appears to be a disease with an early phase where the virus replicates, coinciding with the first presentation of symptoms, followed by a later ′inflammatory′ phase which results in severe disease in some individuals. It is known from other rapidly progressive infections such as sepsis and influenza that early treatment with antimicrobials is associated with a better outcome. The hypothesis is that this holds for COVID-19 and that early antiviral treatment may prevent progression to the later phase of the disease. Methods: Trial design: Phase IIA randomised, double-blind, 2 x 2 design, placebo-controlled, interventional trial. Randomisation: Participants will be randomised 1:1 by stratification, with the following factors: gender, obesity, symptomatic or asymptomatic, current smoking status presence or absence of comorbidity, and if the participant has or has not been vaccinated. Blinding: Participants and investigators will both be blinded to treatment allocation (double-blind). Discussion: We propose to conduct a proof-of-principle placebo-controlled clin. trial of favipiravir plus or minus nitazoxanide in health workers, their household members and patients treated at the Mexican Social Security Institute (IMSS) facilities. Participants with or without symptomatic COVID-19 or who tested pos. will be assigned to receive favipiravir plus nitazoxanide or favipiravir plus nitazoxanide placebo. The primary outcome will be the difference in the amount of virus (′viral load′) in the upper respiratory tract after 5 days of therapy. Secondary outcomes will include hospitalization, major morbidity and mortality, pharmacokinetics, and impact of antiviral therapy on viral genetic mutation rate. If favipiravir with nitazoxanide demonstrates important antiviral effects without significant toxicity, there will be a strong case for a larger trial in people at high risk of hospitalization or intensive care admission, for example older patients and/or those with comorbidities and with early disease. Trial registration: ClinicalTrials.govNCT04918927. Registered on June 9, 2021. And 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) was used in the research process.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), a thiazolide compound, is a antiparasitic drug with structure similar to niclosamide.Formula: C12H9N3O5S

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