Synthesis, characterization, and biological evaluation of novel thiazole and pyrazole derivatives of quinoline-4-carboxylic acid as potential antimicrobial agents

Discovery of Novel Thiazol-2-Amines and Their Analogues as Bioactive Molecules: Design, Synthesis, Docking and Biological Evaluation

“…showed excellent inhibition with MIC (zoi) 6.25 (22.5), 25 (21.5) and 25 (18) µg/mL against E. coli, S. typhi and P. aeruginosa respectively as compared to the standard drug. Molecular docking results suggest that compound exhibited inhibitory activity by binding of the title compound within the active sites of the inhibiting Enoyl ACP reductase, Lipid A, Pyridoxal kinase and type I DHQase enzymes.…”

“…They are also useful as anti-allergic [12], anthelmintic [13] agents and as sedative hypnotics [14]. Several methods for the synthesis of thiazole derivatives have been developed [15][16][17], based on the above observations and as a part of our research in the synthesis of novel heterocyclic systems [18,19], a simple facile route has been described for the synthesis of new thiazol-…”

Synthesis and biological evaluation of novel 2‐arylquinoline‐3‐fused thiazolo[2,3‐c]1,2,4‐triazole heterocycles as potential antiproliferative and antimicrobial agents

“…Thiosemicarbazide can be easily cyclized to result various cyclic compounds hence, they are considered as key intermediates in heterocyclic chemistry. Similarly, 2‐phenyl quinoline hydrazenethiazol compounds were found to have a key role in pharmacological applications like antimicrobial [10], antitubercular [11], anticancer [12], antiproliferative [13], anti‐inflammatory [14] and antihypertensive [15] activities. In addition, quinoline‐based fused thiazol[2,3c]1,2,4‐triazole scaffolds exhibits significant biological activities such as antitumor [15], antimicrobial [16] and antitubercular [16].…”

Novel Double [3 + 2 + 1] Heteroannulation for Forming Unprecedented Dipyrazolo-Fused 2,6-Naphthyridines

“…The functionalized fused naphthyridine unit is often found in many natural products of marine origin that have shown a wide range of biological activities such as HIV-1 integrase inhibition and as antitumor agents and selective antagonists of 5-HT4 receptors, . In addition, a variety of synthetic fused 2,6-naphthyridines exhibited various biological properties, including selective human PKD1 inhibitor, protein kinase CK2 inhibitors, and antimicrobial agents . Although many studies on the preparation of fused 2,6-naphthyridine derivatives have been developed, − , these methods suffer multistep syntheses.…”

“…In addition, a variety of synthetic fused 2,6-naphthyridines exhibited various biological properties, including selective human PKD1 inhibitor, protein kinase CK2 inhibitors, and antimicrobial agents . Although many studies on the preparation of fused 2,6-naphthyridine derivatives have been developed, − , these methods suffer multistep syntheses. Thus, the development of general and efficient routes to regioselective synthesis of fused 2,6-naphthyridine is still challenging.…”