Design, synthesis and biological evaluation of 8-aminoquinoline-1,2,3-triazole hybrid derivatives as potential antimicrobial agents

Synthesis, Anticancer Evaluation and Pharmacokinetic Studies of Quinoline‐Triazole Hybrid Derivatives

“…After getting low yield and prolonged reaction time of the reaction of 3‐azidopropyl 4‐methylbenzensulfonate and 5‐aminoquinoline, 1‐azido‐3‐iodopropane was prepared by Finkelstein reaction of the corresponding tosyl derivatives and used without further purification. N ‐(3‐azidopropyl)quinolin‐5‐amine ( 7 ) was obtained in moderate yield (70 %) [13] …”

“…They are also important in other fields like material science and chemical biology [10,11] . Synthesis of the triazole ring through click reaction, using azide and alkyne groups has led to increased incorporation of the triazole moiety in key drug candidates [10,12,13] …”

“…Molecules synthesized by the hybridization methodology are highly desirable and important because of their activity through multiple coming together on a single molecule with lower toxicity [14] . The hybrid molecules bearing quinoline and triazole heterocyclic rings have shown various promising biological activity [13,15,16] . As in the many antimalarial drugs like chloroquinine, pamaquine, primaquine, and tafenoquine [17] structures, in which the quinoline ring is substituted with the amino group from different positions and derivatized as N ‐alkyl, are quite common.…”

Hybrid Azine Derivatives: A Useful Approach for Antimicrobial Therapy

“…In their attempt to obtain new quinoline derivatives with antimicrobial activity, Albayrak et al [ 20 ] synthesized a library of 20 new triazolo-quinoline hybrid derivatives and studied their antimicrobial activities. The reaction pathway involves several steps ( Scheme 13 ), starting from 8-nitroquinoline 53 .…”

Silver-Catalyzed Cascade Cyclization of Amino-NH-1,2,3-Triazoles with 2-Alkynylbenzaldehydes: An Access to Pentacyclic Fused Triazoles

“…Broad attention has been paid to 1,2,3-triazole-containing heterocycles, which have been widely applied in the fields of medicine [ 1 , 2 , 3 , 4 , 5 ], pesticide [ 6 , 7 , 8 , 9 , 10 ], biochemistry [ 11 , 12 , 13 , 14 ], and material science [ 15 , 16 , 17 , 18 , 19 , 20 ] since the ‘Click’ triazole chemistry was founded at the beginning of this century [ 21 , 22 ]. For instance, some of the well-known drugs bearing triazole moiety are presented in Figure 1 , including A (Cefatrizine) and B (Tazobactum) as β -lactam antibiotic [ 1 , 23 , 24 , 25 , 26 , 27 ], C as anti-cancer reagent [ 23 , 28 ], D as potential nonpeptidic angiotensin (II) receptor antagonists [ 29 , 30 ], E as a toll-like receptor [ 29 , 31 ], F as a mental disorders medicine [ 32 ], and G as a wall teichoic acid active antibiotic [ 11 ].…”