Synthesis of 3-chloro-4-fluorophenyl-3,4-dichlorophenyl substituted thiocarbamide derivatives as potential antitubercular agents

Abstract

A series of dihalosubstituted thiocarbamide derivatives (5a-e, 6a-e, 7a-e, and 8a-e) were synthesized as antitubercular agents. The structures of dihalosubstituted thiocarbamide derivatives were established on the basis of IR, 1 H, 13 C NMR, and mass spectral data. All the compounds were tested in vitro for antimycobacterial activity against Mycobacterium tuberculosis (ATCC-25177) by well-diffusion method and MIC by serial dilution method. Results of the antitubercular screening revealed that some of the compounds showed moderate to good antitubercular activity. Of all the compounds tested, two derivatives viz., 8d and 8e expressed MIC of 25 lg/ml, and one compound 7e showed MIC of 12.5 lg/ml against M. tuberculosis (ATCC-25177).

Calcium-catalysed synthesis of amines through imine hydrosilylation: an experimental and theoretical study

“…While 2v is a ligand with potential for application in catalysis, 2w has potential for application in medicinal chemistry due to its antifungal properties and also as a precursor of antitubercular agents. 60,61…”

“…While 2v is a ligand with potential for application in catalysis, 2w has potential for application in medicinal chemistry due to its antifungal properties and also as a precursor of antitubercular agents. 60,61 At this stage, we were keen to get insights into the processes involved in the previously described hydrosilylation.…”

“…While 2v represents a potential ligand finding application in catalysis, 2w has potential applications in medicinal chemistry for its antifungal properties and also as a precursor for antitubercular agents. 60,61 At this stage, we were keen to get insights into the processes involved in the previously described hydrosilylation. From a mechanistic point of view, two main hydrosilane activation pathways have been previously proposed (Scheme 1): (i) the Chalk-Harrod and modified Chalk-Harrod mechanism occurring for e. g. with rhodium or platinum catalysts and relying on two-electron oxidative addition and reductive elimination steps (Scheme 1, A); (ii) a ionic mechanism in which a Lewis acidic catalyst enhances the electrophilic character of the silicon center through activation of the Si-H bond (Scheme 1, B).…”

Insights into the Effects of Ligand Binding on Leucyl-tRNA Synthetase Inhibitors for Tuberculosis: In Silico Analysis and Isothermal Titration Calorimetry Validation

“…Incidences of drug-resistant tuberculosis have become common and are rising at an alarming rate. The development of resistance and cross-resistance has always driven researchers to search for novel targets and drugs with new mechanisms to counter the drug resistance problem [ 2 , 3 ]. Aminoacyl t-RNA synthetases are ubiquitously found in all organisms and regulate the transcription process by playing an active role in protein biosynthesis.…”