21346-21-4

Usage

InChI:InChI=1/C9H7NO2S2/c11-7-3-1-6(2-4-7)10-8(12)5-14-9(10)13/h1-4,11H,5H2

Upstream product

• 2131-60-4 4-hydroxyphenyl isothiocyanate 
• 68-11-1 mercaptoacetic acid 
• 123-30-8 4-amino-phenol 
• 62812-90-2 triethylamine (4-hydroxyphenyl)carbamodithioate 
• 6326-83-6 bis(carboxymethyl)trithiocarbonate 

Downstream Products

• 15059-00-4 3-(4-hydroxy-phenyl)-2-thioxo-thiazolidine-4,5-dione 5-phenylhydrazone 
• 24044-44-8 3-(4-hydroxyphenyl)-thiazolidine-2,4-dione 
• 306323-46-6 (5Z)-3-(4-hydroxyphenyl)-5-thiophen-2-ylmethylen-2-thioxothiazolidin-4-one 
• 1268494-92-3 3-(4-hydroxyphenyl)-2-thioxo-5-{4-[(1,3,3-trimethyl-1,3-dihydroindol-2-ylidenemethyl)azo]benzylidene}thiazolidin-4-one 

Relevant academic research and scientific papers

Synthesis and Biological Evaluation of Novel Carbazole Hybrids as Promising Antimicrobial Agents

Two series of carbazole analogs of 8-methoxy-N-substituted-9H-carbazole-3-carboxamides (series 1) and carbazolyl substituted rhodanines (series 2) were synthesized through facile synthetic routes. All the final compounds from these two series were evaluated for their preliminary in vitro antifungal and antibacterial activity against four fungal (Candida albicans, Cryptococcus neoformans, Cryptococcus tropicalis and Aspergillus niger) and four bacterial (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) strains, respectively. Among the tested compounds, three compounds of series 1 displayed promising antifungal and antibacterial activity, especially against C. neoformans and S. aureus. In addition, one compound of series 1 displayed notable antimicrobial activity (MIC: 6.25 μg/mL) against clinical isolates of C. albicans and C. neoformans (MIC: 12.5 μg/mL). From the second series, four compounds exhibited significant antifungal and antibacterial activity, especially against C. neoformans and S. aureus. The most active compound of series 2 displayed a prominent antimicrobial activity against C. neoformans (MIC: 3.125 μg/mL) and S. aureus (MIC: 1.56 μg/mL), respectively.

NIFUROXAZIDE ANALOGS AND THERAPEUTIC USES THEREOF

Nifuroxazide analogs, and their pharmaceutically acceptable salts and derivatives are described. Methods and uses are also provided that include the administration of an effective amount of the nifuroxazide analogs, or their pharmaceutically acceptable sa

Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors

Based on the structure of HIV-1 gp41 binding site for small-molecule inhibitors, optimization of lead 2 resulted in the discovery of a new series of 2,5-dimethyl-3-(5-(N-phenylrhodaninyl)methylene)-N-(3-(1H-tetrazol-5-yl)phenyl) pyrrole compounds with improved anti-HIV-1 activity. The most active compounds 13a and 13j exhibited significant potency against gp41 6-HB formation with IC50 values of 4.4 and 4.6 μM and against HIV-1 replication in the MT-2 cells with EC50 values of 3.2 and 2.2 μM, respectively, thus providing a new starting point to develop highly potent small-molecule HIV fusion inhibitors targeting gp41.

Design, synthesis, and biological evaluation of N-carboxyphenylpyrrole derivatives as potent HIV fusion inhibitors targeting gp41

On the basis of the structures of small-molecule hits targeting the HIV-1 gp41, N-(4-carboxy-3-hydroxy)phenyl-2,5-dimethylpyrrole (2, NB-2), and N-(3-carboxy-4-chloro)phenylpyrrole (A1, NB-64), 42 N-carboxyphenylpyrrole derivatives in two categories (A and B series) were designed and synthesized. We found that 11 compounds exhibited promising anti-HIV-1 activity at micromolar level and their antiviral activity was correlated with their inhibitory activity on gp41 six-helix bundle formation, suggesting that these compounds block HIV fusion and entry by disrupting gp41 core formation. The structure-activity relationship and molecular docking analysis revealed that the carboxyl group could interact with either Arg579 or Lys574 to form salt bridges and two methyl groups on the pyrrole ring were favorable for interaction with the residues in gp41 pocket. The most active compound, N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole (A12), partially occupied the deep hydrophobic pocket, suggesting that enlarging the molecular size of A12 could improve its binding affinity and anti-HIV-1 activity for further development as a small-molecule HIV fusion and entry inhibitor.

Simple zwitterionic merocyanines as potential NLO chromophores

A suite of zwitterionic pyridylidene-based merocyanines that contain no interconnecting π-bridge between the donor and acceptor rings has been synthesised and their second-order NLO properties evaluated largely by semi-empirical computational methods (MOP

3-Oxyaryl-2-thionethiazolidones-4 and their choleretic activity

The synthesis of the group of 3-oxyaryl-2-thionethiazolidones-4 is described. The structures of the new compounds are supported by 1H-NMR spectra. These compounds have been tested in vivo for their choleretic activity. The obtained results gave the opportunity to separate the perspective substances as the potential choleretics.