Month: September 2022

Bhandari, Ranjana;Khanna, Garima;Kuhad, Anurag published 《Pharmacological insight into potential therapeutic agents for the deadly Covid-19 pandemic》. The research results were published in《European Journal of Pharmacology》 in 2021.Electric Literature of C12H9N3O5S The article conveys some information:

A review. Coronaviruses are pleomorphic, enveloped, or spherical viruses, which have a size ranging from 80 to 120 nm. These viruses act on receptors that cause the triggering of fusion. Coronaviruses were first described after cultivation from patients with common colds by Tyrell and Bynoe in 1966. There are various subtypes of coronavirus, 7 out of these can cause infection in human beings. The Alpha subtype is responsible for mild infection showing symptoms or infection without any prevailing symptoms. On the other hand, the beta subtype is responsible for very serious diseases leading to fatality. The lineage of this novel SARS-CoV-2 falls under the beta lineage of the beta coronavirus which has been observed to have a relation to the MERS and SARS coronavirus. In the Huanan market selling seafood, the transition of this novel virus in humans from animals has occurred. It has the potential to be the cause of widespread fatality amongst the people of the globe. On August 16, 2020, the World Health Organization had reported 2,1294,845 cases which are confirmed to date out of which 413,372 deaths have occurred. Currently, no targeted antiviral vaccines or drugs to fight against COVID-19 infection have been approved for use in humans. This pandemic is fast emerging and drug repurposing is the only ray of hope which can ensure quick availability. Vaccine development is progressing each day with various platforms such as DNA, Live Attenuated Virus, Non-Replicating Viral Vector, Protein Subunit, and RNA, being utilized for the development. COVID-19 attacks the immune system of the host & this can result in a cytokine storm. As a result, various herbal agents both acting as antivirals and immunomodulatory can also be used. Convalescent Plasma Therapy and Mesenchymal Stem Cell therapy are also being explored as a plausible therapeutic. There remains a considerable unmet need for therapeutics to be addressed. The development and availability of accessible and efficient therapy are essential for the treatment of patients. This review discusses the epidemiol., pathogenesis, the tale of origin, and transmission of COVID-19 or Sars-Cov2 virus and gives evidence of potential therapeutic agents that can be explored to cast away this pandemic. 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 used: to test its anti-viral activity against chikungunya virus as an antiprotozoal agent to test its effect on cell viability in various cancer cell lines; to test its effect on human cytomegalovirus (HCMV) infected human fibroblast HFF cellsElectric Literature of C12H9N3O5S

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

HPLC of Formula: 6285-57-0《On water catalyst-free synthesis of benzo[d]imidazo[2,1-b] thiazoles and novel N-alkylated 2-aminobenzo[d]oxazoles under microwave irradiation》 was published in 2020. The authors were Mukku, Narasimharao;Maiti, Barnali, and the article was included in《RSC Advances》. The author mentioned the following in the article:

A highly efficient unprecedented catalyst-free microwave-assisted procedure for synthesizing benzo[d]imidazo[2,1-b]thiazoles and N-alkylated 2-aminobenzo[d]oxazoles in green media was developed. The transformation provided rapid access to functionalized benzo[d]imidazo[2,1-b]thiazoles from 2-aminobenzothiazole and N-alkylated 2-aminobenzo[d]oxazole from 2-aminobenzoxazole scaffolds under mild transition-metal-free conditions. This synthetic manipulation was expected to greatly expand the repertoire of reaction types in heterocyclic chem. and pave the way for new syntheses of bioactive compounds6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) were involved in the experimental procedure.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0HPLC of Formula: 6285-57-0) has been shown to lower blood pressure in mice by inhibiting angiotensin converting enzyme and potassium channels. This drug also has a protective effect on the heart and brain from ischemia reperfusion injury.

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

Tilekar, Kalpana;Hess, Jessica D.;Upadhyay, Neha;Schweipert, Markus;Flath, Felix;Gutierrez, Denisse A.;Loiodice, Fulvio;Lavecchia, Antonio;Meyer-Almes, Franz-Josef;Aguilera, Renato J.;Ramaa, C. S. published 《HDAC4 Inhibitors with Cyclic Linker and Non-hydroxamate Zinc Binding Group: Design, Synthesis, HDAC Screening and in vitro Cytotoxicity evaluation.》 in 2021. The article was appeared in 《ChemistrySelect》. They have made some progress in their research.Electric Literature of C7H5N3O2S The article mentions the following:

Recent evidences highlight the usefulness of small mol. (Histone deacetylase 4) HDAC4 inhibitors in the several preclin. paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non-hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) derivatives with pyridine as cyclic linker and TZD ring as zinc binding group was designed and screened in a panel of isoenzymes of HDACs, wherein the most potent compounds exhibiting HDAC4 IC₅₀-values<5 μM were 5 v, 5 w, 5 y and 5 z (IC₅₀=4.2±1 μM, 0.75±0.03 μM, 4.9±0.5 and 2.3±0.5 μM, resp.). The docking studies displayed the unique binding mode of this series of compound at active site of HDAC4, wherein TZD ring was indicated as zinc binding group. Further, 5 w and 5 y were found as the most potent antiproliferative agent in lymphoblastic leukemia (CCRF-CEM) and breast cancer MDA-MB-231 cells. Compound 5 y was found to induce the apoptosis and DNA fragmentation of CEM cells. The western blotting anal. of 5 y also showed the presence of cleaved caspases supporting their apoptotic nature. Further, Class IIa (HDAC4) selectivity of 5 y was also supported by western blotting observations, wherein 5 y caused the accumulation of acetylated H3 but not of acetylated Tubulin. Thus, our findings endorse the further investigation of this series of compounds for their potential as targeted cancer therapeutic agents. And 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) was used in the research process.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0Electric Literature of C7H5N3O2S) has been shown to lower blood pressure in mice by inhibiting angiotensin converting enzyme and potassium channels. This drug also has a protective effect on the heart and brain from ischemia reperfusion injury.

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

Recommanded Product: 6-Nitrobenzo[d]thiazol-2-amine《An efficient green synthesis of new benzothiazoles containing sulfonamide or cyclic imide moieties》 was published in 2020. The authors were Bougheloum, Chafika;Alioua, Sabrina;Belghiche, Robila;Benali, Nesma;Messalhi, Abdelrani, and the article was included in《Journal of Heterocyclic Chemistry》. The author mentioned the following in the article:

An efficient and convenient protocol for one-pot synthesis of new benzothiazoles bearing sulfonamide I (R = 4-methylphenyl, NH(CH₂)₃CH₃, 1,2,3,4-tetrahydroisoquinolin-2-yl, etc.; R¹ = H, 6-Me, 6-NO₂, etc.; X = (CH₂)₂, CH=CH, ClC=CCl, etc.) and 1-N-(1,3-benzothiazol-2-yl)-2-N-[(4-methylbenzene)sulfonyl]benzene-1,2-dicarboxamide or cyclic imide moieties II and 2-(6-methoxybenzo[d]thiazol-2-yl)isoindoline-1,3-dione using cesium salt of Wells-Dawson heteropolyacid (Cs₅HP₂W₁₈O₆₂) as solid catalyst and water as solvent under ultrasound irradiation was reported. The reaction speed was remarkably catalyzed with the aid of ultrasound irradiation Moreover, this approach prepares multiple other benefits such as operational ease, higher yields, and energy performance.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 Recommanded Product: 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

Jiao, Peili;Wang, Yuxi;Mao, Beibei;Wang, Bingding;Zhong, Yi;Jin, Hongwei;Zhang, Lihe;Zhang, Liangren;Liu, Zhenming published 《Discovery of 2-(2-aminobenzo[d]thiazol-6-yl) benzo[d]oxazol-5-amine derivatives that regulated HPV relevant cellular pathway and prevented cervical cancer from abnormal proliferation》 in 2020. The article was appeared in 《European Journal of Medicinal Chemistry》. They have made some progress in their research.Computed Properties of C7H5N3O2S The article mentions the following:

Herein, virtual screening was performed and 2-(2-aminobenzo[d]thiazol-6-yl) benzo[d]oxazol-5-amine derivatives I (R¹ = H, NH₂; R² = H, NH₂, NHC(O)NHC₂H₅) were designed, synthesized as antineoplastic agents, and evaluated for their anti-tumor activities. Among them, the most promising compound I (R = R¹ = NH₂) (II) showed specific anti-proliferation ability against HeLa cells (IC₅₀ = 380 nM) as well as excellent inhibition of tumor growth in the HeLa xenograft model without inducing obvious side effects. It is interesting that compound II displayed significant inhibition against HPV18-pos. cervical cell lines (HeLa) but not for HPV16-pos. cervical cell lines (SiHa). Further study demonstrated that a low concentration of compound II could lead to a cell cycle blockage at the G1 phase and promote cell apoptosis slightly (8.77%). Compound II also exhibited transcription repression, especially those associated with the oncoprotein E7 cellular pathway like E7/Rb/E2F-1/DNMT1, which were essential in tumorigenesis. Proteomics anal. revealed that E7 might be degraded through E3 ubiquitin ligases, which aligned with decreasing expression of E7 following the treatment of compound II. Taken together, it indicated that compound II could be a promising potential agent for cervical cancer treatment. To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0) has been used:
as model analyte for voltammetric determination of electrochemically reducible organic substances;
in the synthesis of 2-methyl-4-nitro-2H-pyrazole-3-carboxylic acid[2-(cyclohexanecarbonylamino)benzothiazol-6-yl]amide derivatives;
in the preparation of push-pull nonlinear optical chromophores containing thiazole and benzothiazole acceptors;
as a base in dye production by diazotation reaction.

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

Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《Lipoic acid (LA) dose-dependently protects bone losses in the mandible of rats during the development of osteopenia by inhibiting oxidative stress and promoting bone formation》 was published in 2022. The authors were Radzki, Radoslaw Piotr;Bienko, Marek;Wolski, Dariusz;Oniszczuk, Tomasz;Radzka-Pogoda, Agnieszka;Polak, Pawel;Borzecki, Andrzej;Stasiak, Mateusz, and the article was included in《Biomedicine & Pharmacotherapy》. The author mentioned the following in the article:

Our study was carried out to evaluate the effect of lipoic acid (LA) on the densitometric properties, structure and mech. strength of the mandible of Wistar rats with developing osteopenia. The study used 42 sham-operated (SHO) and ovariectomized (OVX) rats. The OVX rats were randomly divided (n = 6) onto two controls treated s.c. with physiol. saline (OVX-PhS) and 17β-estradiol (OVX-E2), resp., and onto four exptl. OVX groups that received LA in the doses of 12.5, 25, 50 and 100 mg/kg/day for 28 days. The results demonstrated that the lack of estrogen brought about osteopenic bone changes, especially in the trabecular compartment. In addition, while the usage of LA in the doses of 12.5 and 25 LA had no effect in OVX rats, the dose of 100 effectively inhibited osteopenic changes of the mandible. This dose maintained structural, densitometric and mech. parameters at levels like that in the SHO and OVX-E2 groups by inhibiting the destructive influence of oxidative stress. Dose 50, however, was revealed to be the most effective. It not only inhibited atrophic changes and the influence of oxidative stress, but also stimulated the formation of mandibular bone tissue. Our results suggest that the administration of LA is effective in preventing atrophic changes in the mandibular bone tissue in conditions of ovarian hormone deficiency and suggest its potential in the therapy of osteoporosis. 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) has been used: to test its anti-viral activity against chikungunya virus as an antiprotozoal agent to test its effect on cell viability in various cancer cell lines; to test its effect on human cytomegalovirus (HCMV) infected human fibroblast HFF cellsQuality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Computed Properties of C12H9N3O5SIn 2021, Sun, Haiyan;Ou, Tong;Hu, Jianyang;Yang, Ziyi;Lei, Qifang;Li, Yuqing;Wang, Gang;Li, Yongpeng;Wu, Kai;Wang, Shupeng;Wu, Song published 《Nitazoxanide impairs mitophagy flux through ROS-mediated mitophagy initiation and lysosomal dysfunction in bladder cancer》. 《Biochemical Pharmacology (Amsterdam, Netherlands)》published the findings. The article contains the following contents:

Bladder cancer is one of the most common malignancy in the urinary tract with high recurrence and drug resistance in clinics. Alternative treatments from existing drugs might be a promising strategy. Nitazoxanide (NTZ), an FDA-approved antiprotozoal drug, has got increasingly noticed because of its favorable safety profile and antitumor potential, yet the effects in bladder cancer and underlying mechanisms remain poorly understood. Herein, we find that NTZ induces mitochondrial damage and mitophagy initiation through PINK1-generated phospho-ubiquitin(pS65-Ub) and autophagy receptor-mediated pathway even in the absence of Atg5/Beclin1. Meanwhile, NTZ inhibits lysosomal degradation activity, leading to mitophagy flux impairment at late stage. Mitochondrial reactive oxygen species (ROS) production is critical in this process, as eliminating ROS with N-acetylcysteine (NAC) efficiently inhibits PINK1 signaling-mediated mitophagy initiation and alleviates lysosomal dysfunction. Co-treatment with NTZ and autophagy inhibitor Chloroquine (CQ) to aggravate mitophagy flux impairment promotes NTZ-induced apoptosis, while alleviation of mitophagy flux impairment with ROS scavenger reduces cell death. Moreover, we also discover a similar signaling response in the 3D bladder tumor spheroid after NTZ exposure. In vivo study reveals a significant inhibition of orthotopic bladder tumors with no obvious systemic toxicity. Together, our results uncover the anti-tumor activities of NTZ with the involvement of ROS-mediated mitophagy modulation at different stages and demonstrate it as a potential drug candidate for fighting against bladder tumors.2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) were involved in the experimental procedure.

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

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

Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Fahmy, Mennat-Elrahman Ahmed;Abdelaal, Amany Ahmed;Hassan, Soad Ismail;Shalaby, Maisa Ahmed;Ismail, Mousa Abdelgawad Mousa;Khairy, Rasha Ahmed;Badawi, Manal Abdelmaged;Afife, Adam Ashraf;Fadl, Hanaa Omar published 《Antiparasitic and immunomodulating effects of nitazoxanide, ivermectin and selenium on Cryptosporidium infection in diabetic mice.》. 《Revista brasileira de parasitologia veterinaria = Brazilian journal of veterinary parasitology : Orgao Oficial do Colegio Brasileiro de Parasitologia Veterinaria》published the findings. The article contains the following contents:

The present work aims to investigate the antiparasitic and the immunomodulating effects of nitazoxanide (NTZ) and ivermectin (IVC) alone or combined together or combined with selenium (Se), on Cryptosporidium infection in diabetic mice. The results revealed that the combined NTZ and IVC therapy achieved the highest reduction of fecal oocysts (92%), whereas single NTZ showed the lowest reduction (63%). Also, adding Se to either NTZ or IVC resulted in elevation of oocyst reduction from 63% to 71% and from 82% to 84% respectively. All treatment regimens, with the exception of NTZ monotherapy, showed a significant improvement in the intestinal histopathology, the highest score was in combined NTZ and IVC therapy. The unique results of immunohistochemistry in this study showed reversal of the normal CD4/CD8 T cell ratio in the infected untreated mice, however, following therapy it reverts back to a normal balanced ratio. The combined (NTZ+ IVC) treatment demonstrated the highest level of CD4 T cell expression. Taken together, NTZ and IVC combined therapy showed remarkable anti-parasitic and immunostimulatory effects, specifically towards the CD4 population that seem to be promising in controlling cryptosporidiosis in diabetic individuals. Further research is required to explore other effective treatment strategies for those comorbid patients. The experimental procedure involved many compounds, such as 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 used: to test its anti-viral activity against chikungunya virus as an antiprotozoal agent to test its effect on cell viability in various cancer cell lines; to test its effect on human cytomegalovirus (HCMV) infected human fibroblast HFF cellsName: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

SDS of cas: 6285-57-0In 2020, Tiwari, Monika R.;Patel, Navin B. published 《Synthesis, characterization and biological studies of thiazolidinone analogues》. 《Journal of Applicable Chemistry (Lumami, India)》published the findings. The article contains the following contents:

A new series of 2-(4-substituted phenyl)-3-(6-substituted benzo [d]thiazol-2-yl)thiazolidin-4-one derivatives I [R = pyridin-4-yl, 4-hydroxy-3-methylphenyl, 4-chlorophenyl, etc.; R¹ = MeO, O₂N] were prepared by hybridization of two different biol. active moieties benzothiazole and thiazolidinone. The structures of the newly synthesized compounds I were established on the basis of spectral data (IR, ¹H and ¹³C NMR) and elemental anal. All the synthesized compounds I were tested for antibacterial activity against Gram-pos. bacteria (S. aureus, S. pyogenes) and Gram-neg. bacteria (C. albicans, A. niger, A. clavatus), antifungal activity against three fungi (C. albicans, A. niger, A. clavatus) using the MIC (Minimal Inhibitory Concentration) method, anti-tubercular activity H37Rv using L. J. Slope Method. Results of biol. screening revealed that compounds I [R1 = O₂N; R = 4-chlorophenyl, 4-methylthiophenyl, 4-methylphenyl, 3-methyl-4-hydroxyphenyl, R1 = MeO; R = 4-fluorophenyl, 4-trifluoromethylphenyl] showed good antibacterial activity where as I [R1 = O₂N; 4-chlorophenyl, R1 = MeO, R = furan-2-yl] and showed good antifungal activity and compound I [R1 = O₂N; R = 4-bromophenyl] showed good antitubercular activity. To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 SDS of cas: 6285-57-0) 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, Ferreira de Lima, Nayana;de Andrade Picanco, Guaraciara;Costa, Tatiane Luiza;Vinaud, Marina Clare published 《In vitro metabolic stress induced by nitazoxanide and flubendazole combination in Taenia crassiceps cysticerci》. 《Experimental Parasitology》published the findings. The article contains the following contents:

Taenia crassiceps is often used as exptl. model for T. solium cysticercosis studies. Currently cysticercosis antiparasitic treatment is based on albendazole and praziquantel which may present side effects and parasitic resistance. The search for other antiparasitic drugs is necessary. Nitazoxanide (NTZ) and flubendazole (FLB) are broad spectrum antiparasitic drugs that present anti-cysticercosis effect. Metabolic analyses help to determine the impact of these drugs on parasites. The aim of this study was to determine the impact on the production and excretion of organic metabolites in T. crassiceps cysticerci after in vitro exposure to NTZ and FLB, isolated or in combination. T. crassiceps cysticerci were culture in RPMI medium and exposed to 10 μg/mL of NTZ, 10 μg/mL of FLB or 10 μg/mL of NTZ +10 μg/mL of FLB. 24 h after exposure, the parasites were chromatog. analyzed to determine the impact of these drugs on glycolysis, homolactic fermentation, tricarboxylic acid cycle, fatty acids oxidation and proteins catabolism. It was possible to determine that the drugs combination induced greater metabolic impact on cysticerci in comparison to the isolated drugs exposure. The drugs combination induced gluconeogenesis, metabolic acidosis, increase in tricarboxylic acid cycle and in proteins catabolism. While the NTZ isolated exposure induced metabolic acidosis and protein catabolism and the FLB isolate exposure induced gluconeogenesis and protein catabolism. These results show that the combination of drugs with different modes of action increase the antiparasitic effect and may be indicated as alternative cysticercosis treatments. 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), a thiazolide compound, is a antiparasitic drug with structure similar to niclosamide.Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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