In 2022,Pharmaceuticals included an article by Moodley, Rashmika; Mashaba, Chakes; Rakodi, Goitsemodimo H.; Ncube, Nomagugu B.; Maphoru, Mabuatsela V.; Balogun, Mohammed O.; Jordan, Audrey; Warner, Digby F.; Khan, Rene; Tukulula, Matshawandile. Safety of 6-Chlorobenzothiazol-2-ylamine. The article was titled 《New Quinoline-Urea-BenzΞothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling》. The information in the text is summarized as follows:
A series of 25 new benzothiazole-urea-quinoline hybrid compounds, I (X = H, Me, F, NO2, etc.) and II (n = 0, 2, 3, 4, and 6) were synthesized successfully via a three-step synthetic sequence involving an amidation coupling reaction as a critical step. In vitro evaluation of these hybrid compounds for their antitubercular inhibitory activity against the Mycobacterium tuberculosis H37Rv pMSp12::GPF bioreporter strain was undertaken. Of the 25 tested compounds, 17 compounds exhibited promising anti-TB activities of less than 62.5μM (MIC90) and 13 compds showed promising activity with MIC90 values in the range of 1-10μM, while compound I(X = CF3), being the most active, exhibited sub-micromolar activity (0.968μM) in the CAS assay. In addition, minimal cytotoxicity against the HepG2 cell line (cell viability above 75%) in 11 of the 17 compounds, at their resp. MIC90 concentrations, was observed, with compound I(X = CF3), exhibiting 100% cell viability. The hybridization of the quinoline, urea, and benzothiazole scaffolds demonstrated a synergistic relationship because the activities of resultant hybrids were vastly improved compared to the individual entities. In silico ADME predictions showed that the majority of these compounds have drug-like properties and are less likely to potentially cause cardiotoxicity (QPlogHERG > -5).6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Safety of 6-Chlorobenzothiazol-2-ylamine) was used in this study.
6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Safety of 6-Chlorobenzothiazol-2-ylamineThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica