57641-48-2Relevant academic research and scientific papers
Synthesis and antileishmanial activity of 1,3-bis(aryloxy)propan-2-amines
Lavorato, Stefania N.,Duarte, Mariana C.,Lage, Daniela P.,Tavares, Carlos A. P.,Coelho, Eduardo A. F.,Alves, Ricardo J.
, p. 1052 - 1072 (2017/04/14)
We describe herein the antileishmanial activity of 1,3-bis(aryloxy)propan-2-amines, prepared in four simple steps from epichlorohydrin. Among the evaluated compounds, three (4o, 4q, and 4r) displayed considerable activity against Leishmania amazonensis promastigote forms, with IC50 values below 10 μM. We also analyzed the effects of the nature and the position of ring substituent on activity. Two amines (4m and 4o) showed excellent profiles in the treatment of L. amazonensis-infected macrophages, reducing the parasite burden by more than 95% in tested concentrations.
1,3-Bis(aryloxy)propan-2-ols as potential antileishmanial agents
Lavorato, Stefania N.,Duarte, Mariana C.,Lage, Daniela P.,Tavares, Carlos A. P.,Coelho, Eduardo A. F.,Alves, Ricardo J.
, p. 981 - 986 (2017/10/05)
We describe herein the synthesis and antileishmanial activity of 1,3-bis(aryloxy)propan-2-ols. Five compounds (2, 3, 13, 17, and 18) exhibited an effective antileishmanial activity against stationary promastigote forms of Leishmania amazonensis (IC50??15.0?μm), and an influence of compound lipophilicity on activity was suggested. Most of the compounds were poorly selective, as they showed toxicity toward murine macrophages, except 17 and 18, which presented good selective indexes (SI?≥?10.0). The five more active compounds (2, 3, 13, 17, and 18) were selected for the treatment of infected macrophages, and all of them were able to reduce the number of internalized parasites by more than 80%, as well as the number of infected macrophages by more than 70% in at least one of the tested concentrations. Altogether, these results demonstrate the potential of these compounds as new hits of antileishmanial agents and open future possibilities for them to be tested in in vivo studies.
Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity
Sun, Dianqing,Scherman, Michael S.,Jones, Victoria,Hurdle, Julian G.,Woolhiser, Lisa K.,Knudson, Susan E.,Lenaerts, Anne J.,Slayden, Richard A.,McNeil, Michael R.,Lee, Richard E.
experimental part, p. 3588 - 3594 (2009/10/10)
Direct anti-tuberculosis screening of commercially available compound libraries identified a novel piperidinol with interesting anti-tuberculosis activity and drug like characteristics. To generate a structure activity relationship about this hit a 22 mem
An efficient catalyst-free regio- and stereoselective ring-opening of epoxides with phenoxides using polyethylene glycol as the reaction medium
Das, Biswanath,Krishnaiah, Maddeboina,Thirupathi, Ponnaboina,Laxminarayana, Keetha
, p. 4263 - 4265 (2008/02/12)
A catalyst-free regio- and stereoselective ring-opening of epoxides with phenoxides has been carried out efficiently using polyethylene glycol as the reaction medium to form the corresponding β-aryloxyalcohols in high yields at room temperature.
Highly regioselective ring opening of oxiranes with phenoxides in the presence of β-cyclodextrin in water
Surendra,Krishnaveni, N. Srilakshmi,Nageswar,Rao, K. Rama
, p. 4994 - 4995 (2007/10/03)
Highly regioselective ring opening of oxiranes to β-hydroxy ethers with phenoxides has been achieved in impressive yields in the presence of β-cyclodextrin as catalyst and water as solvent.
Hypocholesterolemic activity of 1,3 bis(substituted phenoxy) 2 propanones
Piantadosi,Hall,Wyrick,Ishaq
, p. 222 - 229 (2007/10/12)
A series of 1,3 bis (substituted phenoxy) 2 propanones was found to be active hypocholesterolemic agents at 10 mg/kg/day. The p chloro and p methyl substituted phenoxy compounds possess the highest activity. These compounds did not possess the estrogenic and antifertility activities of the related previously reported derivatives of the bis (β phenylethyl) ketone series. The 1,3 bis (p methylphenoxy) 2 propanone (7) also lowered serum triglycerides and glycerol which appeared to be due to increased levels of serum lipase and reduced activity of liver lipase. There was reduced incorporation of free fatty acids into complex lipids by the liver. Cholesterol was excreted faster in the treated animals.
