- Aegeline inspired synthesis of novel β3-AR agonist improves insulin sensitivity in vitro and in vivo models of insulin resistance
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Background and Purpose: In our drug discovery program of natural product, earlier we have reported Aegeline that is N-acylated-1-amino-2- alcohol, which was isolated from the leaves of Aeglemarmelos showed anti-hyperlipidemic activity for which the QSAR s
- Rajan, Sujith,Satish, Sabbu,Shankar, Kripa,Pandeti, Sukanya,Varshney, Salil,Srivastava, Ankita,Kumar, Durgesh,Gupta, Abhishek,Gupta, Sanchita,Choudhary, Rakhi,Balaramnavar, Vishal M.,Narender, Tadigoppula,Gaikwad, Anil N.
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- Substituted diaryl compound and preparation method and application thereof
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The invention relates to the field of medicinal chemistry, in particular to a substituted diaryl compound (I). The preparation method comprises the following steps: medicine preparation and medical application thereof. Test results show that the substituted diaryl compound has a good inhibition effect on human lung cancer (A549), human ovarian cancer (SKOV3), human melanoma (A375) and human colon cancer (LOVO) cells. Formula (I):
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Paragraph 0073-0075
(2021/09/15)
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- Improvement and simplification of synthesis of 3-aryloxy-1,2-epoxypropanes using solvent-free conditions and microwave irradiations. Relation with medium effects and reaction mechanism
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Some 3-aryloxy-1,2-epoxypropanes, interesting as potential synthons in β-adrenergic receptor antagonists preparation, were obtained in excellent yields (65-96% within 2-17 min) by microwave activation (monomode system) using solid-liquid solvent-free phase transfer catalysis (PTC). The best results for the O-alkylation of some phenols with epichlorohydrin were obtained using TBAB and NaOH/K2CO3 (1:4 mol/mol) as phase transfer catalyst and more acceptable basic system, respectively. These new procedure is compared with classical methods. Significant specific microwave effect (non-purely thermal) was evidenced in all cases. They were discussed in terms of reaction medium and mechanism, taking into account the variations in polarity of the systems.
- Pchelka, Beata K.,Loupy, Andre,Petit, Alain
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p. 10968 - 10979
(2007/10/03)
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- Resolution of racemic 3-aryloxy-1-nitrooxypropan-2-ols by lipase-catalyzed enantioselective acetylation
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Both (R)- and (S)-enantiomers of 3-aryloxy-1-nitrooxypropan-2-ols (R)-(-)-1, (S)-(+)-2 were prepared in high enantiomeric excess by lipase from Pseudomonas cepacia (Amano PS) or Pseudomonas fluorescens (Amano AK)-catalyzed acetylation of racemic alcohols 1a-g with vinyl acetate in n-hexane at 4 or 22°C. The enantioselectivity of this transformation was dependent on the substitution pattern of the aryl ring with E-values ranging from 31 to 111.
- Pchelka, Beata Krystyna,Loupy, Andre,Plenkiewicz, Jan,Petit, Alain,Blanco, Luis
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p. 2109 - 2119
(2007/10/03)
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- A NEW APPLICATION OF CORRELATION EQUATIONS. INFLUENCE OF SUBSTITUENT ON BASICITY OF A SERIES OF CHLOROPHENYL GLYCIDYL ETHERS
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The relation between the basicity of simple oxiranes and substituent constants was described earlier by the common equation pKb=co+c1?.It has been shown that this equation is not satisfied in the case of chlorophenyl glycidyl ethers, when the pKa values of chlorophenols have been taken as a measure of the inductive effect of chlorophenoxy substituent and pKb have been estimated from infrared measurements.The modification of the equation to the following form: pKb=co+(c1+c2Sk)pKa by considerarion of the conformation factor Sk make a good correlation possible.The possibility of the existence of some chlorophenyl glycidyl ethers rotameres has been also discussed on the above basis.
- Stolarzewicz, Andrzej,Dworak, Andrzej,Jedlinski, Zbigniew
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p. 2517 - 2523
(2007/10/02)
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