94266-06-5Relevant academic research and scientific papers
Manganese(III)-Promoted Double Carbonylation of Anilines Toward α-Ketoamides Synthesis
Chen, Bo,Kuai, Chang-Sheng,Wu, Xiao-Feng,Xu, Jian-Xing
, (2021/12/06)
Employing anilines as nucleophiles in double carbonylation is a longstanding challenge. In this communication, a Mn(III)-promoted double carbonylation of alkylborates or Hantzsch esters with anilines toward the synthesis of α-ketoamides has been developed. By using easily available potassium alkyltrifluoroborates or Hantzsch esters as the starting material, and cheap and non-toxic Mn(OAc)3 ? 2H2O as the promotor, a broad range of alkyl α-ketoamide derivatives were synthesized in moderate to good yields with excellent selectivity. (Figure presented.).
Synthesis and anticonvulsant activity of some 1,4-dihydropyridine derivatives
Begum, Safia,Sirisha, Kalam
, p. 433 - 438 (2021/09/28)
A series of asymmetrical 4-alkyl/aryl-2,6-dimethyl-3-N-(aryl/heteroaryl)-carbamoyl-5-ethoxycarbonyl-1, 4-dihydropyridines 3a-d and symmetrical 4-alkyl/aryl-2,6-dimethyl-3,5-bis-(ethoxycarbonyl)-1,4-dihydropyridines 4a and 4b have been prepared by the condensation of various benzaldehydes, ethylacetoacetate, 2-aminopyridine or p-toludine in ethanol (Hantzch method). The structures of all the synthesized 1,4-dihydropyridine derivatives have been confirmed by spectral data (IR,1H NMR) and elemental analysis. Compounds 3a-c, 4a and 4b (10 mg/kg) have been evaluated for their anticonvulsant effect against pentylenetetrazole- induced convulsions with phenytoin (4 mg/kg) as the standard. The anticonvulsant potential of the newly synthesized compounds have been assessed on the basis of increase in latency (onset time) to induce convulsions; decrease in number of convulsions and increase in latency of death compared to control and standard.
Synthesis of diethyl 4-substituted-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates as a new series of inhibitors against yeast α-glucosidase
Niaz, Huma,Kashtoh, Hamdy,Khan, Jalaluddin A. J.,Khan, Ajmal,Wahab, Atia-Tul,Alam, Muhammad Tanveer,Khan, Khalid Mohammed,Perveen, Shahnaz,Choudhary, M. Iqbal
, p. 199 - 209 (2015/04/14)
1,4-Dihydropyridine-3,5-dicarboxylate derivatives (1-25) were synthesized in high yields via Hantzsch reaction and evaluated for their α-glucosidase inhibitory activity. Compounds 1, 2, 6-8, 11, 13-15, and 23-25 showed a potent inhibitory activity against yeast α-glucosidase with IC50 values in the range of 35.0-273.7 μM, when compared with the standard drug acarbose (IC50 = 937 ± 1.60 μM). Their structures were characterized by different spectroscopic techniques. The kinetics, selectivity, and toxicity studies on these compounds were also carried out. The kinetic studies on most active compounds 14 and 25 determined their modes of inhibition and dissociation constants Ki. Compound 14 was found to be a non-competitive inhibitor with Ki = 25.0 ± 0.06, while compound 25 was identified as a competitive inhibitor with Ki = 66.0 ± 0.07 μM.
Synthesis, anticancer and MRP1 inhibitory activities of 4-alkyl/aryl-3,5-bis(carboethoxy/carbomethoxy)-1,4-dihydro-2,6-dimethylpyridines
Amgoth, Srinivas Nayak,Porika, Mahendar,Abbagani, Sadanandam,Garlapati, Achaiah,Vanga, Malla Reddy
, p. 147 - 155 (2013/03/13)
Fourteen new 4-alkyl/aryl-3,5-bis-(carboethoxy/carbomethoxy)-1,4-dihydro-2, 6-dimethylpyridines (4a-4n) have been prepared by conventional and microwave irradiation (MWI) methods from a three component reaction mixture viz., alkyl acetoacetate (1), appropriate aldehyde (2) and ammonium acetate (3). The compounds prepared have been purified and characterized by their spectral (FTIR, 1H NMR and MS) data. The two synthetic methods employed have been compared in terms of relative yields and reaction times. On comparison, the MWI method has been found to be easy, simple, eco-friendly, rapid and high yielding. The synthesized compounds have been evaluated for their cytotoxic activity against HT-29 (colon cancer) and MDA-MB (breast cancer) cell lines and MRP1 inhibitory activity using the insect cell membrane MRP 1 ATPase assay. Though some of the compounds could exhibit some degree of cytotoxicity it was found to be low in comparison to standard. Among the compounds tested 4g was relatively better in its MRP1 inhibitory action (IC50 = 16 μM) but not comparable to that of benzbromarone (IC50 = 4 μM).
