A series of 30 novel diamino phenyl chloropicolinate fettered carboxamides, urea, and thiourea derivatives were synthesized by coupling of methyl 4-amino-6-(2-aminophenyl)-3-chloropyridine-2-carboxylate with different acid chlorides, urea, and thiourea moieties, respectively. All of these compounds were characterized by 1H and 13C nuclear magnetic resonance spectroscopy, CHN analysis, and high-resolution mass spectra for confirmation of the structures. Two compounds were also characterized by single-crystal X-ray diffraction analysis to confirm the structures obtained by spectral analysis. All these 30 compounds were tested for their in vitro antimycobacterial activity using the microplate alamar blue assay method against Mycobacterium tuberculosis. Five compounds have shown good minimum inhibitory concentration (MIC) values with low cytotoxicity when compared with the reference drugs. Moreover, some of the compounds have high MIC values compared with isoniazid, rifampicin, and so forth and also had shown good reign in the spread of bacteria by the nutrient starvation model. These antimycobacterial activity results have shown a good correlation with molecular docking model analysis with the inhibitors MurB by exhibiting strong interactions. Some of these compounds could be promising candidates against M. tuberculosis for future preclinical agent drug development.

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A couple of series of heterocyclic‐based urea and thiourea derivatives, connected with a hybrid scaffold skeleton containing pyrazole and piperazine ring moieties, were achieved. In this study, a total of fifteen new compounds were synthesized by reacting 1‐(3‐methyl‐1‐phenyl‐1H‐pyrazol‐5‐yl)piperazine hydrochloride with carbamides and thiocarbamides. All the fifteen newly synthesized compound structures were confirmed by 1H & 13C NMR and FTIR spectroscopy, ESI mass spectrometry, CHNS analysis and HPLC chromotograms. Moreover, the structures of N‐allyl‐4‐(3‐methyl‐1‐phenyl‐1H‐pyrazol‐5‐yl)piperazine‐1‐carbothioamide and 4‐(3‐methyl‐1‐phenyl‐1H‐pyrazol‐5‐yl)‐N‐(4‐nitrophenyl)piperazine‐1‐carbothioamide were also confirmed by single‐crystal X‐ray diffraction analysis. Further, as per the objective of this work, all these fifteen newly synthesized compounds were screened for anti‐inflammatory activity. The majority of the compounds displayed moderate‐to‐good anti‐inflammatory activity. The anti‐inflammatory activity study was also correlated with molecular docking studies using the receptor Cyclooxygenase‐2.

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We identified twenty-two new sacubitril derivatives (5a–v) as lead compounds for various biologically active targets.