European Journal of Medicinal Chemistry_文献综述【化源网】


Synthesis of highly functionalized barbituric acids and study of their interactions with p-glycoprotein and Mg2+--potential candidates for multi drug resistance modulation. Eur. J. Med. Chem. 45(3) , 1256-62, (2010) 2010-03-01 A number of barbituric acids with appropriate substituent at C-5 position were synthesized and investigated for their interactions with p-gp and Mg(2+). Compounds 5, 6, 8-10, 12-14 and 16 increased the basal activity of p-gp by more than 50% at 0.05 muM conce...
Synthesis, in vitro antibacterial and antifungal evaluations of new alpha-hydroxyphosphonate and new alpha-acetoxyphosphonate derivatives of tetrazolo [1, 5-a] quinoline. Eur. J. Med. Chem. 45 , 1128-32, (2010) 2010-03-01 A series of new alpha-hydroxyphosphonate and alpha-acetoxyphosphonate derivatives have been synthesized for the first time of tetrazolo [1, 5-a] quinoline derivatives. Elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data elucidated the structure...
Synthesis, antibacterial and antiviral properties of curcumin bioconjugates bearing dipeptide, fatty acids and folic acid. Eur. J. Med. Chem. 45 , 1078-86, (2010) 2010-03-01 Curcumin bioconjugates, viz. di-O-tryptophanylphenylalanine curcumin (2), di-O-decanoyl curcumin (3), di-O-pamitoyl curcumin (4), di-O-bis-(gamma,gamma)folyl curcumin (6), C(4)-ethyl-O-gamma-folyl curcumin (8) and 4-O-ethyl-O-gamma-folyl curcumin (10) have be...
A theoretical study of the structure-radical scavenging activity of trans-resveratrol analogues and cis-resveratrol in gas phase and water environment. Eur. J. Med. Chem. 45 , 1015-27, (2010) 2010-03-01 Quantum calculations based on the density functional theory (DFT) have been employed to study the relation between the structure and antioxidant activity of trans-resveratrol (TR), cis-resveratrol (CR), trans-4.4'-dihydroxystilbene (trans-4,4'-DHS), trans-3,4...
5-Substituted [1]pyrindine derivatives with antiproliferative activity. Eur. J. Med. Chem. 45 , 896-901, (2010) 2010-03-01 We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cy...
Synthesis and antimicrobial activities of 3-O-alkyl analogues of (+)-catechin: improvement of stability and proposed action mechanism. Eur. J. Med. Chem. 45 , 1028-33, (2010) 2010-03-01 We report here the synthesis and biological properties of 3-O-alkyl analogues of (+)-catechin (5), which itself is one of the major natural polyphenols found in green tea and has several physiological activities. Starting from 5, a series of 3-O-alkyl-(+)-cat...
New pyrazoles incorporating pyrazolylpyrazole moiety: synthesis, anti-HCV and antitumor activity. Eur. J. Med. Chem. 45 , 1042-50, (2010) 2010-03-01 Three series of novel pyrazole derivatives 2b-d, 4a-d and 6a-d were synthesized via two step procedure that utilizes hydrazonoyl chlorides 1a-d and enaminones 3a-d and 5a-d, respectively as starting materials. The structures of all the newly synthesized produ...
Synthesis of new spiroindolinones incorporating a benzothiazole moiety as antioxidant agents. Eur. J. Med. Chem. 45 , 1068-77, (2010) 2010-03-01 3H-Spiro[1,3-benzothiazole-2,3'-indol]-2'(1'H)-ones 3a-c and 4a-e were synthesized from treating the 5-substituted 1H-indole-2,3-diones with 2-aminothiophenol in ethanol. The structures were confirmed by elemental analyses, spectrometry (IR, (1)H NMR, (13)C N...
Synthesis and antioxidant properties of enone core based dendrimers with carbazole as surface group. Eur. J. Med. Chem. 45 , 1220-4, (2010) 2010-03-01 Synthesis of enone core based dendrimers with carbazole as surface group has been achieved. All the synthesized dendrimers showed excellent antioxidant behavior with commercially available 1,1-diphenyl-2-picryl hydrazyl (DPPH).Copyright (c) 2009 Elsevier Mass...
New 1,3-oxazolo[4,5-c]quinoline derivatives: synthesis and evaluation of antibacterial and antituberculosis properties. Eur. J. Med. Chem. 45 , 957-66, (2010) 2010-03-01 A new class of fused oxazoloquinoline derivatives was synthesized starting from 2-bromo-1-phenylethanones 1a-b through multi-step reactions. The newly synthesized compounds were evaluated for their in vitro antibacterial against Escherichia coli (ATTC-25922),...

Synthesis of highly functionalized barbituric acids and study of their interactions with p-glycoprotein and Mg2+--potential candidates for multi drug resistance modulation.

Eur. J. Med. Chem. 45(3) , 1256-62, (2010)

2010-03-01

A number of barbituric acids with appropriate substituent at C-5 position were synthesized and investigated for their interactions with p-gp and Mg(2+). Compounds 5, 6, 8-10, 12-14 and 16 increased the basal activity of p-gp by more than 50% at 0.05 muM conce...

Synthesis, in vitro antibacterial and antifungal evaluations of new alpha-hydroxyphosphonate and new alpha-acetoxyphosphonate derivatives of tetrazolo [1, 5-a] quinoline.

Eur. J. Med. Chem. 45 , 1128-32, (2010)

2010-03-01

A series of new alpha-hydroxyphosphonate and alpha-acetoxyphosphonate derivatives have been synthesized for the first time of tetrazolo [1, 5-a] quinoline derivatives. Elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data elucidated the structure...

Synthesis, antibacterial and antiviral properties of curcumin bioconjugates bearing dipeptide, fatty acids and folic acid.

Eur. J. Med. Chem. 45 , 1078-86, (2010)

2010-03-01

Curcumin bioconjugates, viz. di-O-tryptophanylphenylalanine curcumin (2), di-O-decanoyl curcumin (3), di-O-pamitoyl curcumin (4), di-O-bis-(gamma,gamma)folyl curcumin (6), C(4)-ethyl-O-gamma-folyl curcumin (8) and 4-O-ethyl-O-gamma-folyl curcumin (10) have be...

A theoretical study of the structure-radical scavenging activity of trans-resveratrol analogues and cis-resveratrol in gas phase and water environment.

Eur. J. Med. Chem. 45 , 1015-27, (2010)

2010-03-01

Quantum calculations based on the density functional theory (DFT) have been employed to study the relation between the structure and antioxidant activity of trans-resveratrol (TR), cis-resveratrol (CR), trans-4.4'-dihydroxystilbene (trans-4,4'-DHS), trans-3,4...

5-Substituted [1]pyrindine derivatives with antiproliferative activity.

Eur. J. Med. Chem. 45 , 896-901, (2010)

2010-03-01

We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cy...

Synthesis and antimicrobial activities of 3-O-alkyl analogues of (+)-catechin: improvement of stability and proposed action mechanism.

Eur. J. Med. Chem. 45 , 1028-33, (2010)

2010-03-01

We report here the synthesis and biological properties of 3-O-alkyl analogues of (+)-catechin (5), which itself is one of the major natural polyphenols found in green tea and has several physiological activities. Starting from 5, a series of 3-O-alkyl-(+)-cat...

New pyrazoles incorporating pyrazolylpyrazole moiety: synthesis, anti-HCV and antitumor activity.

Eur. J. Med. Chem. 45 , 1042-50, (2010)

2010-03-01

Three series of novel pyrazole derivatives 2b-d, 4a-d and 6a-d were synthesized via two step procedure that utilizes hydrazonoyl chlorides 1a-d and enaminones 3a-d and 5a-d, respectively as starting materials. The structures of all the newly synthesized produ...

Synthesis of new spiroindolinones incorporating a benzothiazole moiety as antioxidant agents.

Eur. J. Med. Chem. 45 , 1068-77, (2010)

2010-03-01

3H-Spiro[1,3-benzothiazole-2,3'-indol]-2'(1'H)-ones 3a-c and 4a-e were synthesized from treating the 5-substituted 1H-indole-2,3-diones with 2-aminothiophenol in ethanol. The structures were confirmed by elemental analyses, spectrometry (IR, (1)H NMR, (13)C N...

Synthesis and antioxidant properties of enone core based dendrimers with carbazole as surface group.

Eur. J. Med. Chem. 45 , 1220-4, (2010)

2010-03-01

Synthesis of enone core based dendrimers with carbazole as surface group has been achieved. All the synthesized dendrimers showed excellent antioxidant behavior with commercially available 1,1-diphenyl-2-picryl hydrazyl (DPPH).Copyright (c) 2009 Elsevier Mass...

New 1,3-oxazolo[4,5-c]quinoline derivatives: synthesis and evaluation of antibacterial and antituberculosis properties.

Eur. J. Med. Chem. 45 , 957-66, (2010)

2010-03-01

A new class of fused oxazoloquinoline derivatives was synthesized starting from 2-bromo-1-phenylethanones 1a-b through multi-step reactions. The newly synthesized compounds were evaluated for their in vitro antibacterial against Escherichia coli (ATTC-25922),...