Month: September 2022

Hedvat, Jessica;Salerno, David M.;Kovac, Danielle;Scheffert, Jenna L.;Corbo, Heather;Chen, Justin K.;Choe, Jason Y.;Jennings, Douglas L.;Anamisis, Anastasia;Liu, Esther C.;Lee, Jennifer H.;Shertel, Tara;Lange, Nicholas W. published 《Nitazoxanide treatment for norovirus infection in solid organ transplant recipients》. The research results were published in《Clinical Transplantation》 in 2022.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article conveys some information:

A review. This was an IRB-approved, single-center retrospective study of all SOT recipients with GI PCR pos. for acute NV who either received nitazoxanide for NV or did not receive nitazoxanide between Jan., 2015 and August, 2019. A total of 195S OT recipients with GIPCR pos. for NV infection were screened; 52 patients who received nitazoxanide (nita+) were matched on the basis of transplant type and time post-transplant to 52 patients who had GIPCR pos. NV but did not receive nitazoxanide (nita-). These results suggest that nitazoxanide may improve symptoms from NV infection. 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.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Category: thiazole《Design, synthesis and biological evaluation of some 2-(6-nitrobenzo[d]thiazol-2-ylthio)-N-benzyl-N-(6-nitrobenzo[d]thiazol-2-yl)acetamide derivatives as selective DprE1 inhibitors》 was published in 2019. The authors were Gawad, Jineetkumar;Bonde, Chandrakant, and the article was included in《Synthetic Communications》. The author mentioned the following in the article:

In the present study, pharmacophore model was developed using single ligand by ligand-based drug discovery approach. The key features responsible for DprE1 inhibitory activity were taken into consideration for developing pharmacophore. After the virtual screening, top 1000 hits were further subjected to docking study using GLIDE module, Schrodinger. Docking studies have shown promising interaction with amino residues with better glide score. Ligand-based drug design approach yielded a series of 15, 2-(6-nitrobenzo[d]thiazol-2-ylthio)-N-benzyl-N-(6-nitrobenzo[d]thiazol-2-yl)acetamide derivatives I(R¹ = H, Me, COMe, NH₂, etc.; R² = H, Br, NO₂, Me, etc.). The synthesized compounds were screened for In vitro antitubercular activity against Mycobacterium tuberculosis (H₃₇Rv). Four compounds, I (R¹ = H; R² = OMe) (MIC-1.01 μM); I (R¹ = Cl; R² = H) (MIC-0.91 μM); I (R¹ = R² = H) (MIC-0.82 μM); and I (R¹ = H; R² = Br) (MIC-1.04 μM) have shown promising activity compared to MIC of standard isoniazid (INH) and DprE1 enzyme inhibition was compared to BTZ043. Two halogen-substituted compounds have exhibited drastic enzyme inhibition. 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

Millet, Antoine;Filho, Mauro Safir;Hamouda-Tekaya, Nedra;Cavazza, Elisa;Abbe, Patricia;Ruediger, Johanna;Plaisant, Magali;Mayen, Julie;Rocchi, Stephane;Ronco, Cyril;Benhida, Rachid published 《Development and in vivo evaluation of fused benzazole analogs of anti-melanoma agent HA15》. The research results were published in《Future Medicinal Chemistry》 in 2021.Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine The article conveys some information:

In line with our recent discovery of an efficient anticancer thiazolebenzenesulfonamide framework HA15 (1) based on a remarkable endoplasmic reticulum stress inducement mode of action, we report herein a series of innovative constrained HA15 analogs, featuring four types of bicylic derivatives The structure-activity relationship anal., using a cell line assay, led us to identify a novel version of HA15: a new benzothiazole derivative (10b) exhibiting important anti-melanoma effect against sensitive and resistant melanoma cells. Meanwhile, compound 10b induced a significant tumor growth inhibition in vivo with no apparent signs of toxicity. These results consistently open new directions to improve and develop more powerful anticancer therapeutics harboring this type of fused framework. 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 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