312758-85-3Relevant academic research and scientific papers
Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents
Upadhyay, Akanksha,Kushwaha, Pragati,Gupta, Sampa,Dodda, Ranga Prasad,Ramalingam, Karthik,Kant, Ruchir,Goyal, Neena,Sashidhara, Koneni V.
, p. 172 - 181 (2018/05/25)
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2.43 to 45.75 μM) and intracellular amastigotes (IC50 ranging from 7.06 to 34.9 μM) than the control, miltefosine (IC50 = 8.4 μM), with less cytotoxicity in comparison to the standard drugs. Overall results revealed that prototype signify a new structural lead for antileishmanial chemotherapy.
Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors
Kühne, Holger,Obst-Sander, Ulrike,Kuhn, Bernd,Conte, Aurelia,Ceccarelli, Simona M.,Neidhart, Werner,Rudolph, Markus G.,Ottaviani, Giorgio,Gasser, Rodolfo,So, Sung-Sau,Li, Shirley,Zhang, Xiaolei,Gao, Lin,Myers, Michael
, p. 5092 - 5097 (2016/10/05)
Dual inhibition of fatty acid binding proteins 4 and 5 (FABP4 and FABP5) is expected to provide beneficial effects on a number of metabolic parameters such as insulin sensitivity and blood glucose levels and should protect against atherosclerosis. Starting from a FABP4 selective focused screening hit, biostructure information was used to modulate the selectivity profile in the desired way and to design potent dual FABP4/5 inhibitors with good selectivity against FABP3. With very good pharmacokinetic properties and no major safety alerts, compound 12 was identified as a suitable tool compound for further in vivo investigations.
Poly(N-bromo-N-ethylbenzene-1,3-disulfonamide) and N,N,N′,N′-tetrabromobenzene-1,3-disulfonamide as efficient reagents for synthesis of quinolines
Ghorbani-Vaghei, Ramin,Akbari-Dadamahaleh, Somayeh
scheme or table, p. 1055 - 1058 (2009/05/11)
Poly(N-bromo-N-ethylbenzene-1,3-disulfonamide) [PBBS] and N,N,N′,N′-tetrabromobenzene-1,3-disulfonamide [TBBDA] were used as efficient reagents for the synthesis of quinolines in excellent yields from 2-aminoaryl ketones and carbonyl compounds under aqueo
