Synthesis, Characterization and Biological Screening of Pyrazole-Conjugated Benzothiazole Analogs

Abstract

Compounds containing electron donating groups show the promising antimicrobial and antioxidant activities, compounds with CH and Cl substitution show excellent anti-TB activity. Synthesized molecules may become potential candidates for the clinical trials.

A Comprehensive Examination of Heterocyclic Scaffold Chemistry for Antitubercular Activity

“…In vitro anti-TB activity, (162d) and (162e) had a minimum inhibitory concentration of 1.6 μg/mL. (Scheme 33) [48] A series of novel nitro furanyl methyl N-heterocycles based on the structure of IIIM-MCD-211 were designed and synthesized by Apeng Wang et al The Structure-activity relation (SAR) of the nitrofuranyl methyl N-heterocycle series was planned to be explored by replacing the piperazine ring of IIIM-MCD-21 with a piperidine moiety and introducing an oxime or aryl group on the piperidine ring, as well as fusion of the Nheterocycle and benzene ring of IIIM-MCD-21. After the development of the novel compounds, they were screened for their anti-tubercular properties.…”

“…In vitro anti‐TB activity, (162d) and (162e) had a minimum inhibitory concentration of 1.6 μg/mL. (Scheme 33) [48] …”

Recent advances in the synthesis of new benzothiazole based anti-tubercular compounds

“…Then 75a–i reacted with POCl 3 under reflux conditions to give pyrazole-conjugated benzothiazoleanalogues 76a–i which further reacted with 2-hydrazinyl benzothiazole 51a and benzothiazole-2-carbohydrazide 77 to furnish the desired compounds 78a–i and 79a–i respectively (Scheme 20, Table 16). 58…”

“…Then 75a-i reacted with POCl 3 under reux conditions to give pyrazole-conjugated benzothiazoleanalogues 76a-i which further reacted with 2-hydrazinyl benzothiazole 51a and benzothiazole-2-carbohydrazide 77 to furnish the desired compounds 78a-i and 79a-i respectively (Scheme 20, Table 16). 58 In vitro screening was done for the anti-tubercular activity of the synthesized compounds 78a-i and 79a-i using Microplate Alamar Blue Assay (MABA) technique. Compared to benzothiazole carbohydrazide derivatives, which had MIC values of 100 to 25 mg mL −1 , benzothiazole hydrazine compounds displayed greater activity (MIC values 25 to 1.6 mg mL −1 ) (Table 16).…”

Untitled

“…The hybrid molecular designing is an effective method in modern medicinal chemistry to get highly active molecules. This hybridization may result in complementary pharmacophoric functions or emerge as a new mechanism of action [10][11] . Benzoyl-benzofuran derivatives possessing piperazine linker shows the anticancer activity against a panel of human tumor cell lines and apoptosis in A549 cell 12 .…”