Month: September 2022

Ahmed, Tasmia;Rahman, S. M. Abdur;Asaduzzaman, Muhammad;Islam, Abul Bashar Mir Khademul Md.;Chowdhury, A. K. Azad published 《Synthesis, in vitro bioassays, and computational study of heteroaryl nitazoxanide analogs》 in 2021. The article was appeared in 《Pharmacology Research & Perspectives》. They have made some progress in their research.COA of Formula: C12H9N3O5S The article mentions the following:

Antiprotozoal drug nitazoxanide (NTZ) has shown diverse pharmacol. properties and has appeared in several clin. trials. Herein we present the synthesis, characterization, in vitro biol. investigation, and in silico study of four hetero aryl amide analogs of NTZ. Among the synthesized mols., compound 2 and compound 4 exhibited promising antibacterial activity against Escherichia coli (E. coli), superior to that displayed by the parent drug nitazoxanide as revealed from the in vitro antibacterial assay. Compound 2 displayed zone of inhibition of 20 mm, twice as large as the parent drug NTZ (10 mm) in their least concentration (12.5 Μg/mL). Compound 1 also showed antibacterial effect similar to that of nitazoxanide. The analogs were also tested for in vitro cytotoxic activity by employing cell counting kit-8 (CCK-8) assay technique in HeLa cell line, and compound 2 was identified as a potential anticancer agent having IC₅₀ value of 172 Μg which proves it to be more potent than nitazoxanide (IC₅₀ = 428 Μg). Furthermore, the compounds were subjected to mol. docking study against various bacterial and cancer signaling proteins. The in vitro test results corroborated with the in silico docking study as compound 2 and compound 4 had comparatively stronger binding affinity against the proteins and showed a higher docking score than nitazoxanide toward human mitogen-activated protein kinase (MAPK9) and fatty acid biosynthesis enzyme (FabH) of E. coli. Moreover, the docking study demonstrated dihydrofolate reductase (DHFR) and thymidylate synthase (TS) as probable new targets for nitazoxanide and its synthetic analogs. Overall, the study suggests that nitazoxanide and its analogs can be a potential lead compound in the 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.COA of Formula: C12H9N3O5S

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

Safety of 6-Nitrobenzo[d]thiazol-2-amineIn 2021, Nath, Rajarshi;Shahar Yar, M.;Pathania, Shelly;Grover, Gourav;Debnath, Biplab;Akhtar, Jawaid Md published 《Synthesis and anticonvulsant evaluation of indoline derivatives of functionalized aryloxadiazole amine and benzothiazole acetamide》. 《Journal of Molecular Structure》published the findings. The article contains the following contents:

A series of I [R = H, 6-Cl, 5-O₂N, etc.] and II [R¹ = H, 4-MeO, 2-O₂N, 4-O₂N; R² = H, 5-Cl, 5-Br] were designed, synthesized and fulfilled structural requirement of pharmacophore and evaluated for anticonvulsant activities using maximal electroshock test (MES), s.c. pentylenetetrazole (scPTZ) seizures and neurotoxicity by motor impairment model in mice. The most active compound I [R = 6-Cl] showed significant anticonvulsant activity against both MES and scPTZ screens and emerged as most effective anticonvulsant compound with median dose of 35.7 mg/kg (MES ED₅₀), 88.15 mg/kg (scPTZ ED₅₀) and toxic dose (TD₅₀) was found to be > 500mg/kg. In-silico studies including mol. docking study were carried out to establish the mol. interaction of potent compound I [R = 6-Cl] in both Na⁺ channel and GABA_A receptors. The prediction of pharmacokinetic parameters and distance mapping of compounds were performed to establish the drug likeness property.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) 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

Pavan Phani Kumar, M.;Anuradha, V.;Subramanyam, Ch.;Hari Babu, V. V. published 《In silico molecular docking study, synthesis and α-amylase inhibitory activity evaluation of phosphorylated derivatives of purine》 in 2021. The article was appeared in 《Phosphorus, Sulfur and Silicon and the Related Elements》. They have made some progress in their research.Reference of 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

A series of phosphorylated derivatives of purine were synthesized in good yields (88-95%) by the reaction of 2-chloro-4-{[(9H-purin-9-yl)methoxy]methyl}-1,3,2-λ⁵-dioxaphospholan-2-one with various heterocyclic amines. In silico mol. docking study was performed for all the designed compounds to assess their potential ability to inhibit the pancreatic α-amylase enzyme. The compounds (6a–6j) with good inhibition toward the target enzyme were prompted for the synthesis. Spectroscopic analyses of all the newly synthesized compounds were performed to confirm their structures. In vitro α-amylase inhibitory activity of the synthesized compounds was also carried out using acarbose as a standard drug. The compounds 2-[(6-chloro-1,3-benzothiazol-2-yl)amino]-4-{[(9H-purin-9-yl)methoxy]methyl}-1,3,2λ⁵-dioxaphospholan-2-one (6j) (IC₅₀, 94.3 ± 0.5μg/mL) and 1-methyl-6-[(2-oxo-4-{[(9H-purin-9-yl)methoxy]methyl}-1,3,2λ⁵-dioxaphospholan-2-yl)amino]-1,2,3,4-tetrahydropyrimidine-2,4-dione (6f) (IC₅₀, 99.0 ± 0.4μg/mL) reported the highest inhibition among the synthesized compounds All the remaining compounds exhibited good to moderate inhibition with IC₅₀ values in the range of 102.9 ± 0.6 to 233.5 ± 0.6μg/mL when compared with the standard drug, acarbose (IC₅₀, 50.47 ± 0.28μg/mL). 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:6285-57-0Reference of 6-Nitrobenzo[d]thiazol-2-amine) 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

Sreedhar, Badvel;Reddy, Thummaluru Veera;Umapriya, Kollu;Raju, Chamarthi Naga;Reddy, Gandi Vidya Sagar published 《Design, synthesis and evaluation of biological activity of amide derivatives of gramine》 in 2018. The article was appeared in 《European Journal of Biomedical and Pharmaceutical Sciences》. They have made some progress in their research.Application of 6285-57-0 The article mentions the following:

A series of new amide derivatives of 3-(3-((dimethylamino)methyl)-1H-indol-1-yl)propanoic acid 2 were synthesized after converting 2 as its acid chloride 3 and reacting 3 with various bioactive amines using 1- methylimidazole as an acid scavenger by Schotten-Baumann reaction. The newly synthesized compounds were characterized by IR, NMR and mass spectral anal. The title compounds were evaluated for their efficacy as antioxidant and antimicrobial agents in vitro. The synthesized amides 4c and 4f exhibited promising antioxidant activity and compounds 4c-g showed high inhibitory activity against both bacteria and fungi.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 of 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

Szala, Marcin;Grzelakowska, Aleksandra;Modrzejewska, Julia;Siarkiewicz, Przemyslaw;Slowinski, Daniel;Swierczynska, Malgorzata;Zielonka, Jacek;Podsiadly, Radoslaw published 《Characterization of the reactivity of luciferin boronate – A probe for inflammatory oxidants with improved stability》. The research results were published in《Dyes and Pigments》 in 2020.Safety of 6-Nitrobenzo[d]thiazol-2-amine The article conveys some information:

Boronate derivatives of luciferin, containing oxidant-activated self-immolative moieties, recently have been developed for bioluminescent detection of hydrogen peroxide in animal models. Here, the authors report the synthesis and characterization of luciferin boronic acid pinacol ester (LBE) as a probe for detection of hydrogen peroxide, hypochlorous acid, and peroxynitrite, with improved stability and response time. HPLC analyses showed that LBE quickly hydrolyzes in phosphate buffer to luciferin boronic acid (LBA). Hydrogen peroxide oxidizes LBA slowly, with the formation of luciferase substrate, luciferin (Luc-OH), as the only product. Hypochlorite also oxidizes LBA to luciferin, but the subsequent reaction of Luc-OH with hypochlorite gives a chlorinated luciferin Luc-OH-Cl, which has a higher fluorescence quantum yield than luciferin at pH 7.4 and is also a substrate for luciferase (Takakura H, et. all. ChemBioChem 2012; 13:1424). Similar to other boronate probes, LBA is oxidized by peroxynitrite in two pathways. Luc-OH is the product of the major pathway, common for all the oxidants tested, whereas the non-fluorescent nitrated derivative, Luc-NO₂, is formed in the minor pathway, specific for peroxynitrite. Formation of luciferin radical intermediate in the minor pathway has been confirmed by EPR spin trapping and mass spectrometric analyses of the spin adducts. LBE shows potential as an improved probe for the detection of inflammatory oxidants in biol. settings. Complementation of the bioluminescence measurements by HPLC or LC-MS-based identification of chlorinated and nitrated luciferin(s) will help identify the oxidants detected. 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 Safety 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

Quality Control of (S)-1-(4-(4Methylthiazol-5-yl)phenyl)ethan-1-amine HCl《Cancer Selective Target Degradation by Folate-Caged PROTACs》 was published in 2021. The authors were Liu, Jing;Chen, He;Liu, Yi;Shen, Yudao;Meng, Fanye;Kaniskan, H. Umit;Jin, Jian;Wei, Wenyi, and the article was included in《Journal of the American Chemical Society》. The author mentioned the following in the article:

PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin-proteasome system. However, potential toxicity of PROTACs in normal cells due to the off-tissue on-target degradation effect limits their clin. applications. Precise control of a PROTAC’s on-target degradation activity in a tissue-selective manner could minimize potential toxicity/side-effects. To this end, we developed a cancer cell selective delivery strategy for PROTACs by conjugating a folate group to a ligand of the VHL E3 ubiquitin ligase, to achieve targeted degradation of proteins of interest (POIs) in cancer cells vs. noncancerous normal cells. We show that our folate-PROTACs, including BRD PROTAC (folate-ARV-771), MEK PROTAC (folate-MS432), and ALK PROTAC (folate-MS99), are capable of degrading BRDs, MEKs, and ALK, resp., in a folate receptor-dependent manner in cancer cells. This design provides a generalizable platform for PROTACs to achieve selective degradation of POIs in cancer cells. To complete the study, the researchers used (S)-1-(4-(4Methylthiazol-5-yl)phenyl)ethan-1-amine HCl (cas: 1948273-01-5) .

Quality Control of (S)-1-(4-(4Methylthiazol-5-yl)phenyl)ethan-1-amine HClVarious laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.

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

Angeles-Arvizu, Adriana;Enriquez-Flores, Sergio;Jimenez-Gutierrez, Alma;Perez-Rangel, Armando;Luna-Arias, Juan Pedro;Castillo-Romero, Araceli;Hernandez, Jose Manuel;Leon-Avila, Gloria published 《MDR1 protein (ABC-C1) Over Expression in Giardia Intestinalis Incubated with Albendazole and Nitazoxanide》. The research results were published in《Acta Parasitologica》 in 2021.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article conveys some information:

Giardia intestinalis is a worldwide parasite. Drugs used for the treatment of giardiasis are metronidazole, albendazole and nitazoxanide. The development of drug resistance is an obstacle to the effective treatment. Resistance mechanisms in some parasites involve the participation of ATP-binding cassette (ABC) transporter superfamily. To find if the ATP-binding cassette genes are overexpressed in trophozoites treated with albendazole or nitazoxanide. A search for ATP-binding cassette genes in Giardia sequence database (GiardiaDB) was done and six genes were selected. Trophozoites treated with albendazole or nitazoxanide and the expression of these six ABC genes was quantitated by real-time RT-PCR. The ABC-C1 gene was selected, and a fragment cloned. The ABC-C1 protein was expressed, and polyclonal antibodies were elicited in mice to detect the protein in treated trophozoites, finally a docking anal. was performed for ABC-C1 and tizoxanide interaction. Bioinformatics anal. showed that the ATP-binding cassette (ABC) topol. is present in the six proteins. The qRT-PCR revealed that the ABC-C1 gene was overexpressed in cells incubated with nitazoxanide or albendazole. Confocal anal. showed that ABC-C1 protein levels increased in trophozoites with both treatments but was higher with nitazoxanide. The mark was detected heavily in the periphery of the cells. Using a docking anal., it was found that the nitazoxanide metabolite, tizoxanide was docked close to the ATP-binding region as well as in the exit tunnel, located in the transmembrane region. These findings in Giardia intestinalis, support the possible role of ABC-C1 in drug efflux. 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.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 acetateIn 2021, Wipperman, Matthew F.;Bhattarai, Shakti K.;Vorkas, Charles Kyriakos;Maringati, Venkata Suhas;Taur, Ying;Mathurin, Laurent;McAulay, Katherine;Vilbrun, Stalz Charles;Francois, Daphie;Bean, James;Walsh, Kathleen F.;Nathan, Carl;Fitzgerald, Daniel W.;Glickman, Michael S.;Bucci, Vanni published 《Gastrointestinal microbiota composition predicts peripheral inflammatory state during treatment of human tuberculosis》. 《Nature Communications》published the findings. The article contains the following contents:

The composition of the gastrointestinal microbiota influences systemic immune responses, but how this affects infectious disease pathogenesis and antibiotic therapy outcome is poorly understood. This question is rarely examined in humans due to the difficulty in dissociating the immunol. effects of antibiotic-induced pathogen clearance and microbiome alteration. Here, we analyze data from two longitudinal studies of tuberculosis (TB) therapy (35 and 20 individuals) and a cross sectional study from 55 healthy controls, in which we collected fecal samples (for microbiome anal.), sputum (for determination of Mycobacterium tuberculosis (Mtb) bacterial load), and peripheral blood (for transcriptomic anal.). We decouple microbiome effects from pathogen sterilization by comparing standard TB therapy with an exptl. TB treatment that did not reduce Mtb bacterial load. Random forest regression to the microbiome-transcriptome-sputum data from the two longitudinal datasets reveals that renormalization of the TB inflammatory state is associated with Mtb pathogen clearance, increased abundance of Clusters IV and XIVa Clostridia, and decreased abundance of Bacilli and Proteobacteria. We find similar associations when applying machine learning to peripheral gene expression and microbiota profiling in the independent cohort of healthy individuals. Our findings indicate that antibiotic-induced reduction in pathogen burden and changes in the microbiome are independently associated with treatment-induced changes of the inflammatory response of active TB, and the response to antibiotic therapy may be a combined effect of pathogen killing and microbiome driven immunomodulation. 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), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Rahman, Sajid Ur;Mi, Rongsheng;Zhou, Shasha;Gong, Haiyan;Ullah, Munib;Huang, Yan;Han, Xiangan;Chen, Zhaoguo published 《Advances in therapeutic and vaccine targets for Cryptosporidium: Challenges and possible mitigation strategies》 in 2022. The article was appeared in 《Acta Tropica》. They have made some progress in their research.Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article mentions the following:

A review. Cryptosporidium is known to be the second most common diarrheal pathogen in children, causing potentially fatal diarrhea and associated with long-term growth stunting and cognitive deficits. The only Food and Drug Administration-approved treatment for cryptosporidiosis is nitazoxanide, but this drug has not shown potentially effective results in susceptible hosts. Therefore, a safe and effective drug for cryptosporidiosis is urgently needed. Cryptosporidium genome sequencing anal. may help develop an effective drug, but both in vitro and in vivo approaches to drug evaluation are not fully standardized. On the other hand, the development of partial immunity after exposure suggests the possibility of a successful and effective vaccine, but protective surrogates are not precise. In this review, we present our current perspectives on novel cryptosporidiosis therapies, vaccine targets and efficacies, as well as potential mitigation plans, recommendations and perceived challenges.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.Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Recommanded Product: 6285-57-0《Synthesis, spectroscopic characterization and biological evaluation of some 6-nitro-benzothiazole-2-yl-hydrazone derivatives》 was published in 2018. The authors were Kolate, S. S.;Waghulde, G. P.;Patil, C. J.;Sarode, C. H., and the article was included in《Journal of Pharmaceutical, Chemical and Biological Sciences》. The author mentioned the following in the article:

A series of 2-[(6-Nitro-benzothiazol-2-yl)-hydrazonomethyl]-substituted-phenol derivatives I [R = 3-MeO, 5-Br, 4-diethylamino, etc.] were synthesized and characterized by using elemental and spectroscopic analyses (FT-IR, UV-Vis, ¹H-NMR, ¹³C-NMR and Mass spectra). The synthesized compounds I were screened for antimicrobial activities against two Gram-pos. bacteria (Bacillus subtilis and Streptomyces griseus) two Gramneg. bacteria (Salmonella typhi and Pseudomonas aeruginosa) and three funguses (Candidi tropicalis, Kluyveromyces marxianus and Saccharomyces cerevisiae). The antioxidant activities of these compounds I were determined by hydrogen peroxide (H₂O₂) scavenging activity. The substitution iodo-group compound I [R = 3,5-diiodo] was more potentially active than other synthesized compounds I in antibacterial and antifungal activities and the most promising antioxidant activity showed by compounds I [3-MeO, 4-MeO]. 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 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