Tag: 300-400

Walker, Lauren E.;FitzGerald, Richard;Saunders, Geoffrey;Lyon, Rebecca;Fisher, Michael;Martin, Karen;Eberhart, Izabela;Woods, Christie;Ewings, Sean;Hale, Colin;Rajoli, Rajith K. R.;Else, Laura;Dilly-Penchala, Sujan;Amara, Alieu;Lalloo, David G.;Jacobs, Michael;Pertinez, Henry;Hatchard, Parys;Waugh, Robert;Lawrence, Megan;Johnson, Lucy;Fines, Keira;Reynolds, Helen;Rowland, Timothy;Crook, Rebecca;Okenyi, Emmanuel;Byrne, Kelly;Mozgunov, Pavel;Jaki, Thomas;Khoo, Saye;Owen, Andrew;Griffiths, Gareth;Fletcher, Thomas E.;the AGILE platform published 《An Open Label, Adaptive, Phase 1 Trial of High-Dose Oral Nitazoxanide in Healthy Volunteers: An Antiviral Candidate for SARS-CoV-2》 in 2022. The article was appeared in 《Clinical Pharmacology & Therapeutics (Hoboken, NJ, United States)》. They have made some progress in their research.Product Details of 55981-09-4 The article mentions the following:

Repurposing approved drugs may rapidly establish effective interventions during a public health crisis. This has yielded immunomodulatory treatments for severe coronavirus disease 2019 (COVID-19), but repurposed antivirals have not been successful to date because of redundancy of the target in vivo or suboptimal exposures at studied doses. Nitazoxanide is a US Food and Drug Administration (FDA) approved antiparasitic medicine, that physiol.-based pharmacokinetic (PBPK) modeling has indicated may provide antiviral concentrations across the dosing interval, when repurposed at higher than approved doses. Within the AGILE trial platform (NCT04746183) an open label, adaptive, phase I trial in healthy adult participants was undertaken with high-dose nitazoxanide. Participants received 1500 mg nitazoxanide orally twice-daily with food for 7 days. Primary outcomes were safety, tolerability, optimum dose, and schedule. Intensive pharmacokinetic (PK) sampling was undertaken day 1 and 5 with min. concentration (C_min) sampling on days 3 and 7. Fourteen healthy participants were enrolled between Feb. 18 and May 11, 2021. All 14 doses were completed by 10 of 14 participants. Nitazoxanide was safe and with no significant adverse events. Moderate gastrointestinal disturbance (loose stools or diarrhea) occurred in 8 participants (57.1%), with urine and sclera discoloration in 12 (85.7%) and 9 (64.3%) participants, resp., without clin. significant bilirubin elevation. This was self-limiting and resolved upon drug discontinuation. PBPK predictions were confirmed on day 1 but with underprediction at day 5. Median C_min was above the in vitro target concentration on the first dose and maintained throughout. Nitazoxanide administered at 1,500 mg b.i.d. with food was safe with acceptable tolerability a phase Ib/IIa study is now being initiated in patients with COVID-19.2-((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

DeBoer, Mark D.;Platts-Mills, James A.;Elwood, Sarah E.;Scharf, Rebecca J.;McDermid, Joann M.;Wanjuhi, Anne W.;Jatosh, Samwel;Katengu, Siphael;Parpia, Tarina C.;Rogawski McQuade, Elizabeth T.;Gratz, Jean;Svensen, Erling;Swann, Jonathan R.;Donowitz, Jeffrey R.;Mdoe, Paschal;Kivuyo, Sokoine;Houpt, Eric R.;Mduma, Estomih published 《Effect of scheduled antimicrobial and nicotinamide treatment on linear growth in children in rural Tanzania: A factorial randomized, double-blind, placebo-controlled trial》 in 2021. The article was appeared in 《PLoS Medicine》. They have made some progress in their research.COA of Formula: C12H9N3O5S The article mentions the following:

Background: Stunting among children in low-resource settings is associated with enteric pathogen carriage and micronutrient deficiencies. Our goal was to test whether administration of scheduled antimicrobials and daily nicotinamide improved linear growth in a region with a high prevalence of stunting and enteric pathogen carriage. Methods and findings: We performed a randomized, 2 x 2 factorial, double-blind, placebo-controlled trial in the area around Haydom, Tanzania. Mother-child dyads were enrolled by age 14 days and followed with monthly home visits and every 3-mo anthropometry assessments through 18 mo. Those randomized to the antimicrobial arm received 2 medications (vs. corresponding placebos): azithromycin (single dose of 20 mg/kg) at months 6, 9, 12, and 15 and nitazoxanide (3-day course of 100 mg twice daily) at months 12 and 15. Those randomized to nicotinamide arm received daily nicotinamide to the mother (250 mg pills months 0 to 6) and to the child (100 mg sachets months 6 to 18). Primary outcome was length-for-age z-score (LAZ) at 18 mo in the modified intention-to-treat group. Between Sept. 5, 2017 and August 31, 2018, 1,188 children were randomized, of whom 1,084 (n = 277 placebo/placebo, 273 antimicrobial/placebo, 274 placebo/nicotinamide, and 260 antimicrobial/nicotinamide) were included in the modified intention-to-treat anal. The study was suspended for a 3-mo period by the Tanzanian National Institute for Medical Research (NIMR) because of concerns related to the timing of laboratory testing and the total number of serious adverse events (SAEs); this resulted in some participants receiving their final study assessment late. There was a high prevalence of stunting overall (533/1,084, 49.2%). Mean 18-mo LAZ did not differ between groups for either intervention (mean LAZ with 95% confidence interval [CI]: antimicrobial: -2.05 CI -2.13, -1.96, placebo: -2.05 CI -2.14, -1.97; mean difference: 0.01 CI -0.13, 0.11, p = 0.91; nicotinamide: -2.06 CI -2.13, -1.95, placebo: -2.04 CI -2.14, -1.98, mean difference 0.03 CI -0.15, 0.09, p = 0.66). There was no difference in LAZ for either intervention after adjusting for possible confounders (baseline LAZ, age in days at 18-mo measurement, ward, hospital birth, birth month, years of maternal education, socioeconomic status (SES) quartile category, sex, whether the mother was a member of the Datoga tribe, and mother’s height). Adverse events (AEs) and SAEs were overall similar between treatment groups for both the nicotinamide and antimicrobial interventions. Key limitations include the absence of laboratory measures of pathogen carriage and nicotinamide metabolism to provide context for the neg. findings. Conclusions: In this study, we observed that neither scheduled administration of azithromycin and nitazoxanide nor daily provision of nicotinamide was associated with improved growth in this resource-poor setting with a high force of enteric infections. Further research remains critical to identify interventions toward improved early childhood growth in challenging conditions. Trial registration: ClinicalTrials.gov NCT03268902. 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 cellsCOA of Formula: C12H9N3O5S

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

SDS of cas: 55981-09-4In 2021, Hooshmand, Seyed Aghil;Zarei Ghobadi, Mohadeseh;Hooshmand, Seyyed Emad;Azimzadeh Jamalkandi, Sadegh;Alavi, Seyed Mehdi;Masoudi-Nejad, Ali published 《A multimodal deep learning-based drug repurposing approach for treatment of COVID-19》. 《Molecular Diversity》published the findings. The article contains the following contents:

Abstract: Recently, various computational methods have been proposed to find new therapeutic applications of the existing drugs. The Multimodal Restricted Boltzmann Machine approach (MM-RBM), which has the capability to connect the information about the multiple modalities, can be applied to the problem of drug repurposing. The present study utilized MM-RBM to combine two types of data, including the chem. structures data of small mols. and differentially expressed genes as well as small mols. perturbations. In the proposed method, two sep. RBMs were applied to find out the features and the specific probability distribution of each datum (modality). Besides, RBM was used to integrate the discovered features, resulting in the identification of the probability distribution of the combined data. The results demonstrated the significance of the clusters acquired by our model. These clusters were used to discover the medicines which were remarkably similar to the proposed medications to treat COVID-19. Moreover, the chem. structures of some small mols. as well as dysregulated genes’ effect led us to suggest using these mols. to treat COVID-19. The results also showed that the proposed method might prove useful in detecting the highly promising remedies for COVID-19 with min. side effects. All the source codes are accessible using https://github.com/LBBSoft/Multimodal-Drug-Repurposing.git Graphic abstract: [graphic not available: see fulltext]. 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 cellsSDS of cas: 55981-09-4

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