New poly(azomethine-ether)s PAMEs containing 1-phenethyl-4-piperidone moiety have been synthesized through a solution polymerization of various diformyl-a,w-diphenoxyalkanes,I-IV with 3,5-bis(p-aminobenzylidene)-1-Phe...New poly(azomethine-ether)s PAMEs containing 1-phenethyl-4-piperidone moiety have been synthesized through a solution polymerization of various diformyl-a,w-diphenoxyalkanes,I-IV with 3,5-bis(p-aminobenzylidene)-1-Phenethyl-4-piperidone VI.The structures of these polymers were confirmed using spectroscopic techniques.The inherent viscosities of the resulting polymers were found to range from 0.65 to 0.95 dl/g.The solubility of the PAMEs was estimated,showing good solubility in aprotic solvents.The thermal properties of the PAMEs were also evaluated by DSC technique.Liquid crystalline state of the polymers was observed on polarizing microscope exhibiting nematic phase for most of the synthesized polymers.展开更多
Dengue is a severe mosquito-borne viral infection causing half a million deaths annually. Dengue virus NS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(aryli...Dengue is a severe mosquito-borne viral infection causing half a million deaths annually. Dengue virus NS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(arylidene)-4-piperidones analogues 4a4j were synthesized and screened in silico against DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active sites. Results were validated through an in vitro DENV2 NS2B/NS3 protease assay using a fluorogenic Boc-Gly-Arg-Arg-AMC substrate. Nitro derivatives of 3,5-bis(arylidene)-4-piperidones (4e and 4j) emerged as promising lead molecules for novel protease inhibitors with an IC<sub>50</sub> of 15.22 and 16.23 µmol/L, respectively, compared to the standard, panduratin A, having IC<sub>50</sub> of 57.28 µmol/L.展开更多
基金The experiments were conducted by Amna A.Abayo and writing,paper discussion and revision was contributed by Ismail A.Alkskas,who was the corresponding author.
文摘New poly(azomethine-ether)s PAMEs containing 1-phenethyl-4-piperidone moiety have been synthesized through a solution polymerization of various diformyl-a,w-diphenoxyalkanes,I-IV with 3,5-bis(p-aminobenzylidene)-1-Phenethyl-4-piperidone VI.The structures of these polymers were confirmed using spectroscopic techniques.The inherent viscosities of the resulting polymers were found to range from 0.65 to 0.95 dl/g.The solubility of the PAMEs was estimated,showing good solubility in aprotic solvents.The thermal properties of the PAMEs were also evaluated by DSC technique.Liquid crystalline state of the polymers was observed on polarizing microscope exhibiting nematic phase for most of the synthesized polymers.
基金The Research University Team Grant (RUT/1001/PKIMIA/855006) provided by Universiti Sains Malaysia(USM)
文摘Dengue is a severe mosquito-borne viral infection causing half a million deaths annually. Dengue virus NS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(arylidene)-4-piperidones analogues 4a4j were synthesized and screened in silico against DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active sites. Results were validated through an in vitro DENV2 NS2B/NS3 protease assay using a fluorogenic Boc-Gly-Arg-Arg-AMC substrate. Nitro derivatives of 3,5-bis(arylidene)-4-piperidones (4e and 4j) emerged as promising lead molecules for novel protease inhibitors with an IC<sub>50</sub> of 15.22 and 16.23 µmol/L, respectively, compared to the standard, panduratin A, having IC<sub>50</sub> of 57.28 µmol/L.
