2,6-Disubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent Staphylococcal biofilm inhibitors was written by Cascioferro, Stella;Parrino, Barbara;Petri, Giovanna Li;Cusimano, Maria Grazia;Schillaci, Domenico;Di Sarno, Veronica;Musella, Simona;Giovannetti, Elisa;Cirrincione, Girolamo;Diana, Patrizia. And the article was included in European Journal of Medicinal Chemistry in 2019.COA of Formula: C9H5BrN2 This article mentions the following:
A class of 36 new 2-(6-phenylimidazo[2,-1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, compounds I [R = H, Cl, Br; R1 = H, Me; R2 = H, 3-MeO, 4F, etc.] was efficiently synthesized and evaluated for their anti-biofilm properties against the Gram-pos. bacterial reference strains Staphylococcus aureus ATCC 25923, S. aureus ATCC 6538 and Staphylococcus epidermidis ATCC 12228, and the Gram-neg. strains Pseudomonas aeruginosa ATCC 15442 and Escherichia coli ATCC 25922. Many of these new compounds, were able to inhibit biofilm formation of the tested Staphylococcal strains showing BIC50 lower than 10 μg/mL. In particular, compounds I [R = H, R1 = H, R2 = 2,5-diMeO; R = H, R1 = Me, R2 = 3-MeO] showed remarkable anti-biofilm activity against S. aureus ATCC 25923 with BIC50 values of 0.5 and 0.8 μg/mL, resp., whereas compound I [R = Cl, R1 = H, R2 = 2,5-diMeO] was the most potent against S. aureus ATCC 6538, with a BIC50 of 0.3 μg/mL. Remarkably, these compounds showed effects in the early stages of the biofilm formation without affecting the mature biofilm of the same strains and the viability of the planktonic form. Their ability in counteracting a virulence factor (biofilm formation) without interfering with the bacterial growth in the free life form make them novel valuable anti-virulence agents. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-cyanoindole (cas: 90271-86-6COA of Formula: C9H5BrN2).
5-Bromo-3-cyanoindole (cas: 90271-86-6) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.COA of Formula: C9H5BrN2
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles