Tag: 300-400

On October 1, 2009, Muthuppalniappan, Meyyappan; Kumar, Sukeerthi; Thomas, Abraham; Khairatkar-Joshi, Neelima; Mukhopadhyay, Indranil published a patent.Synthetic Route of 31699-14-6 The title of the patent was Preparation of phthalimide derivatives as TRPA1 modulators. And the patent contained the following:

The present invention provides TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds I [ring A = (hetero)aryl, heterocyclyl, cycloalkyl; R1 = H, OH, (un)substituted alkyl, etc.; R2 = H, CN, NO2, etc.; R3, R4 = H, OH, halo, etc.; or R3 and R4 may be joined together to form (un)substituted 3-7 membered (un)saturated cyclic ring which may optionally include at least one heteroatom such as O, S, (un)substituted NH, C(O), S(O)0-2; R5 = H, OH, (un)substituted alkyl, etc.] are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1) modulators. Forty-four compounds I were prepared Thus, coupling the acid II (multi-step synthesis was given) with 4-isopropylaniline afforded the title compound III. Exemplified compounds I were screened for TRPA1 antagonist activity using the 45Calcium uptake assay (data given). Also provided are processes for preparing compounds I, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Synthetic Route of 31699-14-6

The Article related to phthalimide amide preparation transient receptor potential a trpa1 modulator, isoindolylacetamide preparation transient receptor potential a trpa1 modulator, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Synthetic Route of 31699-14-6

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

On August 31, 2013, Koppireddi, Satish; Komsani, Jayaram Reddy; Avula, Sreenivas; Pombala, Sujitha; Vasamsetti, Satishbabu; Kotamraju, Srigiridhar; Yadla, Rambabu published an article.SDS of cas: 31699-14-6 The title of the article was Novel 2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamides as antioxidant and/or anti-inflammatory compounds. And the article contained the following:

A series of novel N-(4-aryl-1,3-thiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamides(4a-k) I and N-(1,3-benzothiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide derivatives (4l-o) II are synthesized and evaluated for their anti-inflammatory and antioxidant activity (DPPH radical scavenging, superoxide anion scavenging, lipid peroxide inhibition, erythrocyte hemolytic inhibition). Compounds 4k and 4l have exhibited good antioxidant activity in four assays, while compounds 4c, 4d, 4m, 4n and 4o have shown good DPPH radical scavenging efficacy. Compounds 4a, 4h, 4i, 4k, 4m and 4n have possessed excellent anti-inflammatory activity. N-[4-(o-methoxyphenyl)-1,3-thiazol-2-yl]-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide (4k) and N-(6-nitro-/methoxy-1,3-benzothiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide (4m and 4n) have exhibited both antioxidant and anti-inflammatory activities. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).SDS of cas: 31699-14-6

The Article related to dioxothiazolidinylacetamide antioxidant antiinflammatory, anti-inflammatory activity, erythrocyte hemolysis, lipid peroxidation, n-(1,3-benzothiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide, n-(4-aryl-1,3-thiazol-2-yl)-2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamide, superoxide anion and dpph radical scavenging and other aspects.SDS of cas: 31699-14-6

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

Computed Properties of C12H9N3O5S《Impairment of SARS-CoV-2 spike glycoprotein maturation and fusion activity by nitazoxanide: an effect independent of spike variants emergence》 was published in 2022. The authors were Riccio, Anna;Santopolo, Silvia;Rossi, Antonio;Piacentini, Sara;Rossignol, Jean-Francois;Santoro, M. Gabriella, and the article was included in《Cellular and Molecular Life Sciences》. The author mentioned the following in the article:

SARS-CoV-2, the causative agent of COVID-19, has caused an unprecedented global health crisis. The SARS-CoV-2 spike, a surface-anchored trimeric class-I fusion glycoprotein essential for viral entry, represents a key target for developing vaccines and therapeutics capable of blocking virus invasion. The emergence of SARS-CoV-2 spike variants that facilitate virus spread and may affect vaccine efficacy highlights the need to identify novel antiviral strategies for COVID-19 therapy. Here, we demonstrate that nitazoxanide, an antiprotozoal agent with recognized broad-spectrum antiviral activity, interferes with SARS-CoV-2 spike maturation, hampering its terminal glycosylation at an endoglycosidase H-sensitive stage. Engineering multiple SARS-CoV-2 variant-pseudoviruses and utilizing quant. cell-cell fusion assays, we show that nitazoxanide-induced spike modifications hinder progeny virion infectivity as well as spike-driven pulmonary cell-cell fusion, a critical feature of COVID-19 pathol. Nitazoxanide, being equally effective against the ancestral SARS-CoV-2 Wuhan-spike and different emerging variants, including the Delta variant of concern, may represent a useful tool in the fight against COVID-19 infections. 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.Computed Properties of C12H9N3O5S

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

Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Rocco, Patricia R. M.;Silva, Pedro L.;Cruz, Fernanda F.;Melo, Marco Antonio C. Jr.;Tierno, Paulo F. G. M. M.;Moura, Marcos A.;De Oliveira, Luis Frederico G.;Lima, Cristiano C.;Santos, Ezequiel A. Dos;Walter, F. Jr.;Fernandes, Ana Paula S. M.;Franchini, Kleber G.;Magri, Erick;de Moraes, Nara F.;Goncalves, Jose Mario J.;Carbonieri, Melanie N.;Santos, Ivonise S. Dos;Paes, Natalia F.;Maciel, Paula V. M.;Rocha, Raissa P.;de Carvalho, Alex F.;Alves, Pedro Augusto;Proenca-Modena, Jose Luiz;Cordeiro, Artur T.;Trivella, Daniela B. B.;Marques, Rafael E.;Luiz, Ronir R.;Pelosi, Paolo;e Silva, Jose Roberto Lapa published 《Early use of nitazoxanide in mild COVID-19 disease: randomised, placebo-controlled trial》. 《European Respiratory Journal》published the findings. The article contains the following contents:

Background: Nitazoxanide is widely available and exerts broad-spectrum antiviral activity in vitro. However, there is no evidence of its impact on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Methods: In a multicentre, randomised, double-blind, placebo-controlled trial, adult patients presenting up to 3 days after onset of coronavirus disease 2019 (COVID-19) symptoms (dry cough, fever and/or fatigue) were enrolled. After confirmation of SARS-CoV-2 infection using reverse transcriptase PCR on a nasopharyngeal swab, patients were randomised 1:1 to receive either nitazoxanide (500 mg) or placebo, three times daily, for 5 days. The primary outcome was complete resolution of symptoms. Secondary outcomes were viral load, laboratory tests, serum biomarkers of inflammation and hospitalisation rate. Adverse events were also assessed. Results: From June 8 to August 20, 2020, 1575 patients were screened. Of these, 392 (198 placebo, 194 nitazoxanide) were analyzed. Median (interquartile range) time from symptom onset to first dose of study drug was 5 (4-5) days. At the 5-day study visit, symptom resolution did not differ between the nitazoxanide and placebo arms. Swabs collected were neg. for SARS-CoV-2 in 29.9% of patients in the nitazoxanide arm vs. 18.2% in the placebo arm (p = 0.009). Viral load was reduced after nitazoxanide compared to placebo (p = 0.006). The percentage viral load reduction from onset to end of therapy was higher with nitazoxanide (55%) than placebo (45%) (p = 0.013). Other secondary outcomes were not significantly different. No serious adverse events were observed Conclusions: In patients with mild COVID-19, symptom resolution did not differ between nitazoxanide and placebo groups after 5 days of therapy. However, early nitazoxanide therapy was safe and reduced viral load significantly.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.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《Interventions in an Ambulatory Setting to Prevent Progression to Severe Disease in Patients With COVID-19: A Systematic Review》 was published in 2022. The authors were O Murchu, Eamon;Spillane, Susan;Byrne, Paula;O′Neill, Michelle;Harrington, Patricia;Ryan, Mairin, and the article was included in《Annals of Pharmacotherapy》. The author mentioned the following in the article:

A review. To conduct a systematic review on the effectiveness and safety of pharmacol. and nonpharmacol. interventions, in the ambulatory setting, aimed at preventing severe disease in patients with COVID-19. Electronic databases (PubMed, EMBASE, and EuropePMC) were searched on Jan. 6, 2021. Study Selection and Data Extraction:: A systematic review was conducted, adhering to PRISMA guidelines. The quality of individual trials was assessed using the Cochrane Risk-of-Bias Tool 2, and the certainty of evidence was assessed using GRADE. Data Synthesis:: The collective search retrieved 3818 citations. Eight trials relating to 9 pharmacol. interventions were identified. No evidence for nonpharmacol. interventions was identified. Low certainty evidence of effectiveness in preventing severe disease was found for fluvoxamine (absolute difference: -8.7%; 95% CI: -1.8% to -16.4%) and bamlanivimab plus etesevimab (absolute difference: -4.9%; 95% CI: -0.8% to -8.9%). Both trials were limited by small sample sizes and short durations of follow-up. In addition, very low certainty evidence of effect was found for ivermectin plus doxycycline and sulodexide. Based on published data, insufficient evidence of effect was found for bamlanivimab (monotherapy), casirivimab plus imdevimab, ivermectin (monotherapy), nitazoxanide, and peginterferon lambda. Relevance to Patient Care and Clin. Practice:: This review assessed all ambulatory treatments for COVID-19 that may improve patient outcomes and reduce hospitalizations. Recent trials have shown promising results for a number of pharmacol. agents to treat COVID-19 in the ambulatory setting. However, larger, more robust trials are needed to support the routine use of these agents outside of monitored clin. trials.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), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Madbouly, Neveen;El Amir, Azza;Kader, Asmaa Abdel;Rabee, Ibraheem;Farid, Alyaa published 《The immunomodulatory activity of secnidazole-nitazoxanide in a murine cryptosporidiosis model》. The research results were published in《Journal of Medical Microbiology》 in 2021.Product Details of 55981-09-4 The article conveys some information:

Cryptosporidium parvum causes intestinal parasitic infections affcting both immunosuppressed and immuno competent individuals. Given the absence of effctive treatments for cryptosporidiosis, especially in immunodeficient patients, the present study was designed to assess the therapeutic efficy of secnidazole (SEC) and its combination with nitazoxanide (NTZ) in comparison to single NTZ treatment in relation to the immune status of a murine model of C. parvum infection. The infected groups were administered NTZ, SEC or NTZ-SEC for three or five successive doses. At days 10 and 12 post-infection (p.i.), the mice were sacrified, and the efficy of the applied drugs was evaluated by comparing the histo pathol. alterations in ileum and measuring the T helper Th1 (interferon gamma; IFN-γ), Th2 [interleukin (IL)-4 and IL-10] and Th17 (IL-17) cytokine profies in serum. The NTZ-SEC combination recorded the maximal reduction of C. parvum oocyst shedding, endogenous stages count and intestinal histopathol., regardless of the immune status of the infected mice. The efficy of NTZ-SEC was dependent on the period of administration, as the 5 day-based treatment protocol was also more effctive than the 3 day-based one in terms of immunocompetence and immunosuppression. The present treatment schedule induced an immunomodulatory effect from SEC that developed a protective immune response against C. parvum infection with reduced production of serum IL-17, IFN-γ, IL-4 and IL-10. Application of NTZ-SEC combined therapy may be useful in treatment of C. parvum, especially in cases involving immunosuppression.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), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Product Details of 55981-09-4

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

Formula: C12H9N3O5SIn 2021, Elalfy, Hatem;Besheer, Tarek;El-Mesery, Ahmed;El-Gilany, Abdel-Hady;Abd Elazez, Mahmoud Soliman;Alhawarey, Ahmed;Alegezy, Mohamed;Elhadidy, Tamer;Hewidy, Asem A.;Zaghloul, Hossam;Neamatallah, Mustafa Ahmed Mohamed;Raafat, Douaa;El-Emshaty, Wafaa M.;Abo El Kheir, Nermin Y.;El-Bendary, Mahmoud published 《Effect of a combination of nitazoxanide, ribavirin, and ivermectin plus zinc supplement (MANS.NRIZ study) on the clearance of mild COVID-19》. 《Journal of Medical Virology》published the findings. The article contains the following contents:

This trial compared the rate and time of viral clearance in subjects receiving a combination of nitazoxanide, ribavirin, and ivermectin plus Zinc vs. those receiving supportive treatment. This non-randomized controlled trial included 62 patients on the triple combination treatment vs. 51 age- and sex-matched patients on routine supportive treatment. all of them confirmed cases by pos. reverse-transcription polymerase chain reaction of a nasopharyngeal swab. Trial results showed that the clearance rates were 0% and 58.1% on the 7th day and 13.7% and 73.1% on the 15th day in the supportive treatment and combined antiviral groups, resp. The cumulative clearance rates on the 15th day are 13.7% and 88.7% in the supportive treatment and combined antiviral groups, resp. This trial concluded by stating that the combined use of nitazoxanide, ribavirin, and ivermectin plus zinc supplement effectively cleared the SARS-COV2 from the nasopharynx in a shorter time than symptomatic therapy. 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 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.Formula: C12H9N3O5S

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

Yadav, Ambedkar Kumar;Wen, Siwan;Xu, Xianghuai;Yu, Li published 《Antiviral treatment in COVID-19: which is the most promising?-a narrative review.》. The research results were published in《Annals of palliative medicine》 in 2021.Recommanded Product: 55981-09-4 The article conveys some information:

The whole world is battling through coronavirus disease 2019 (COVID-19) which is a fatal pandemic. In the early 2020, the World Health Organization (WHO) declared it as a global health emergency without definitive treatments and preventive approaches. In the absence of definitive therapeutic agents, this thorough review summarizes and outlines the potency and safety of all molecules and therapeutics which may have potential antiviral effects. A number of molecules and therapeutics licensed or being tested for some other conditions were found effective in different in vitro studies as well as in many small sample-sized clinical trials and independent case studies. However, in those clinical trials, there were some limitations which need to be overcome to find the most promising antiviral against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). In conclusion, many of above-mentioned antivirals seems to have some therapeutic effects but none of them have been shown to have a strong evidence for their proper recommendation and approval in the treatment of COVID-19. Constantly evolving new evidences, exclusive adult data, language barrier, and type of study (observational, retrospective, small-sized clinical trials, or independent case series) resulted to the several limitations of this review. The need for multicentered, large sample-sized, randomized, placebo-controlled trials on COVID-19 patients to reach a proper conclusion on the most promising antiviral agent is warranted.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.Recommanded Product: 55981-09-4

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

Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Talaam, Keith Kiplangat;Inaoka, Daniel Ken;Hatta, Takeshi;Tsubokawa, Daigo;Tsuji, Naotoshi;Wada, Minoru;Saimoto, Hiroyuki;Kita, Kiyoshi;Hamano, Shinjiro published 《Mitochondria as a potential target for the development of prophylactic and therapeutic drugs against Schistosoma mansoni infection》. 《Antimicrobial Agents and Chemotherapy》published the findings. The article contains the following contents:

The emergence of parasites resistant to praziquantel, the only therapeutic agent, and its ineffectiveness as a prophylactic agent (inactive against the migratory/juvenile Schistosoma mansoni), make the development of new antischistosomal drugs urgent. The parasite’s mitochondrion is an attractive target for drug development, because this organelle is essential for survival throughout the parasite’s life cycle. We investigated the effects of 116 compounds against Schistosoma mansoni cercaria motility that have been reported to affect mitochondrion-related processes in other organisms. Next, eight compounds plus two controls (mefloquine and praziquantel) were selected and assayed against the motility of schistosomula (in vitro) and adults (ex vivo). Prophylactic and therapeutic assays were performed using infected mouse models. Inhibition of oxygen consumption rate (OCR) was assayed using Seahorse XFe24 analyzer. All selected compounds showed excellent prophylactic activity, reducing the worm burden in the lungs to less than 15% of that obtained in the vehicle control. Notably, ascofuranone showed the highest activity, with a 98% reduction of the worm burden, suggesting the potential for the development of ascofuranone as a prophylactic agent. The worm burden of infected mice with S. mansoni at the adult stage was reduced by more than 50% in mice treated with mefloquine, nitazoxanide, amiodarone, ascofuranone, pyrvinium pamoate, or plumbagin. Moreover, adult mitochondrial OCR was severely inhibited by ascofuranone, atovaquone, and nitazoxanide, while pyrvinium pamoate inhibited both mitochondrial and nonmitochondrial OCRs. These results demonstrate that the mitochondria of S. mansoni are a feasible target for drug development. 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.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《1,3-Thiazolbenzamide Derivatives as Chikungunya Virus nsP2 Protease Inhibitors》 was published in 2021. The authors were Ivanova, Larisa;Rausalu, Kai;Zusinaite, Eva;Tammiku-Taul, Jaana;Merits, Andres;Karelson, Mati, and the article was included in《ACS Omega》. The author mentioned the following in the article:

Chikungunya fever results from an infection with Chikungunya virus (CHIKV, genus Alphavirus) that is prevalent in tropical regions and is spreading fast to temperate climates with documented outbreaks in Europe and the Americas. Currently, there are no available vaccines or antiviral drugs for prevention or treatment of Chikungunya fever. The nonstructural proteins (nsPs) of CHIKV responsible for virus replication are promising targets for the development of new antivirals. This study was attempted to find out new potential inhibitors of CHIKV nsP2 protease using the ligand-based drug design. Two compounds 10 and 10c, identified by mol. docking, showed antiviral activity against CHIKV with IC₅₀ of 13.1 and 8.3μM, resp. Both compounds demonstrated the ability to inhibit the activity of nsP2 in a cell-free assay, and the impact of compound 10 on virus replication was confirmed by western blot. The mol. dynamics study of the interactions of compounds 10 and 10c with CHIKV nsP2 showed that a possible mechanism of action of these compounds is the blocking of the active site and the catalytic dyad of nsP2. 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 cellsSafety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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