In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and antiviral activity of a series of novel quinoline derivatives as anti-RSV or anti-IAV agents, published in 2021-03-15, which mentions a compound: 111-24-0, mainly applied to quinoline preparation antiviral activity antiRSV antiIAV agent; Anti-IAV; Anti-RSV; Quinoline derivatives; Structure-activity relationships; Synthesis, Application of 111-24-0.
The synthesis of a series of novel quinoline derivatives, I [R = pyrrolidin-1-yl, methylamino, morpholin-4-yl, etc; R1 = benzyl, adamantan-1-yl, furan-2-ylmethyl, etc; R2 = H; R1R2 = -(CH2)2O(CH2)2-], II (n = 3, 4, 5) based on the lead compound I (R = pyrrolidin-1-yl; R1 = benzyl; R2 = H) (III), identified from a rRSV-mGFP high-throughput screening assay was reported. The results revealed that target compounds I (R = pyrrolidin-1-yl, R1 = 4-fluorobenzyl, R2 = H; R = pyrrolidin-1-yl, R1 = 4-methoxybenzyl, R2 = H; R = pyrrolidin-1-yl, R1 = 3-methoxybenzyl, R2 = H; R = dimethylamino, R1 = benzyl, R2 = H; R = (S)-3-tert-butoxycarbonylaminopyrrolidin-1-yl, R1 = benzyl, R2 = H) (IC50 = 3.10-6.93μM) had good in vitro activity against RSV, which were better than I (R = pyrrolidin-1-yl, R1 = benzyl, R2 = H) and ribavirin. In addition, it is found that compound I (R = 1-tert-butoxycarbonylpiperazin-4-yl, R1 = benzyl, R2 = H) displayed the lower cytotoxicity (CC50: 2490.33μM) and the highest selective index (SI = 673.06), suggest its promising potential as a candidate for further development. On the other hand, some compounds (IC50: 1.87-14.28μM) were more active against IAV than or comparable to ribavirin (IC50: 15.36 ± 0.93μM). Particularly, the most active compound I (R = (S)-3-tert-butoxycarbonylaminopyrrolidin-1-yl, R1 = benzyl, R2 = H) (IC50: 1.87 ± 0.58μM) was found to be 8.2-fold more potent than the reference drug, which could inhibit the virus transcription and replication cycle at an early stage.
In some applications, this compound(111-24-0)Application of 111-24-0 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.
Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis