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Comparative in vivo behavior studies of cyclen-based copper-64 complexes: regioselective synthesis, X-ray structure, radiochemistry, log P, and biodistribution : Yoo, Jeongsoo; Reichert, David E.; Welch, Michael J. Journal of Medicinal Chemistry, 2004 , vol. 47, # 26 p. 6625 - 6637 The in vivo behavior of copper (II)-cyclen complexes was modified via substitution of the parent ligand with two different substituents, 4-tert-butylbenzyl and acetate. This was achieved by using same synthetic strategy (regioselective protection/first alkyla...
Biological evaluation of bishydroxymethyl-substituted cage dimeric 1, 4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells : Richter, Martin; Molnar, Josef; Hilgeroth, Andreas Journal of Medicinal Chemistry, 2006 , vol. 49, # 9 p. 2838 - 2840 A series of N-substituted cage dimeric 1, 4-dihydropyridines 3a-e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure-activity relationships (SAR) and cytotoxic properties are discusse...
Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1, 4-dioxa-7-azaspiro [4.5] decanes as potential dopamine agonists : Brubaker; Colley Jr. Journal of Medicinal Chemistry, 1986 , vol. 29, # 8 p. 1528 - 1531 Three 7-methyl-1, 4-dioxa-7-azaspiro [4.5] decanea that contained either the benzyl, 3- indolylmethyl, or Cindolylmethyl group at the 6-position were synthesized via alkylation of the pyrrolidine enamine of the key intermediate, ethyl 3-oxopiperidine-l-carbox...
2-Benzyl-and 2-Phenyl-3, 4-dihydroxyphenyl-alanine1 : Burger,A.B. et al. Journal of Medicinal Chemistry, 1963 , vol. 6, p. 614 - 616 solution-of 0.4 g.(17.5 mmoles) of sddium in 40 ml. of absolute ethanol were added 3.8 g.(17.5 mmoles) of diethyl acetamidomalonate and crude 2-phenylveratryl chloride [prepared from 5.35 g.(2.5 mmoles'i of 3-phenj lveratrole]. Bfter 9 hr. of refluxing and st...
Substituted thiadiazolines as inhibitors of central nervous system carbonic anhydrase : Lukes,J.J.; Nieforth,K.A. Journal of Medicinal Chemistry, 1975 , vol. 18, p. 351 - 354 A series (24-30) of substituted thiadiazolines was synthesized and tested for in c, itro carbonic anhydrase inhibition and for protective ability against pentylenetetrazole-induced convulsions. ED;,)(pentylenetetrazole protection). TD, o, and LD:,, values are...
Synthesis of 3, 4-dihydroxy-5-fluoro-DL-Phenylalanine and 3, 4-Dihydroxy-5-[fluorine-18] fluoro-DL-phenylalanine : Firnau,G. et al. Journal of Medicinal Chemistry, 1973 , vol. 16, p. 416 - 418 F 170 62b aQuantitative. bCalculated from 6. about two-thirds of lesions. Dihydroxyphenylalanine (DOPA) enters healthy, mature brain capillaries where it is decarboxylated to dopamine. Dopamine can be concentrated in the capillaries by an amine oxidase inhibi...
Some amino and ammonio nitrogen mustard analogs : Price,C.C. et al. Journal of Medicinal Chemistry, 1965 , vol. 8, p. 650 - 655 Biological data on these compounds were reported in detail The amino mustards were found to have a single LD5o of 3-8 mg./kg. compared to 3 mg./kg. for HS-2. In suppression of Ehrlich ascites tumor, IIa was the most active compound, being slightly superior to...
Synthesis and hypoglycemic activity of phenylalkyloxiranecarboxylic acid derivatives : Eistetter, Klaus; Wolf, Horst P. O. Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 109 - 113 A series of new 2-(phenylalkyl) oxirane-2-carboxylic acids has been synthesized and studied for its effects on the concentration of blood glucose. Most of the compounds exhibit remarkable blood glucose lowering activities in fasted rats. Structure-activity st...
Synthesis and antitumor evaluation of selected 5, 6-disubstituted 1 (2) H-indazole-4, 7-diones : Conway, Gregory A.; Loeffler, Larry J.; Hall, Iris H. Journal of Medicinal Chemistry, 1983 , vol. 26, # 6 p. 876 - 884 A series of novel aziridinyl-substituted 1 (2) H-indazole-4, 7-diones and related 1 (2) H- indazole-4, 7-diones was synthesized and tested against Ehrlich ascites carcinoma growth in male CF1 mice. Ten of the test compounds, including two aziridinyl-substitut...
Functionalized DL-amino acid derivatives. Potent new agents for the treatment of epilepsy : Conley, Judith D.; Kohn, Harold Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 567 - 574 Structural analogues of the potent known anticonvulsant agent N-acetyl-DL-alanine N- benzylamide (la) have been prepared (16 examples). The pharmacological activities of these products were evaluated in the maximal electroshock seizure (MES), the subcutaneous...

Comparative in vivo behavior studies of cyclen-based copper-64 complexes: regioselective synthesis, X-ray structure, radiochemistry, log P, and biodistribution

: Yoo, Jeongsoo; Reichert, David E.; Welch, Michael J. Journal of Medicinal Chemistry, 2004 , vol. 47, # 26 p. 6625 - 6637

The in vivo behavior of copper (II)-cyclen complexes was modified via substitution of the parent ligand with two different substituents, 4-tert-butylbenzyl and acetate. This was achieved by using same synthetic strategy (regioselective protection/first alkyla...

Biological evaluation of bishydroxymethyl-substituted cage dimeric 1, 4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells

: Richter, Martin; Molnar, Josef; Hilgeroth, Andreas Journal of Medicinal Chemistry, 2006 , vol. 49, # 9 p. 2838 - 2840

A series of N-substituted cage dimeric 1, 4-dihydropyridines 3a-e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure-activity relationships (SAR) and cytotoxic properties are discusse...

Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1, 4-dioxa-7-azaspiro [4.5] decanes as potential dopamine agonists

: Brubaker; Colley Jr. Journal of Medicinal Chemistry, 1986 , vol. 29, # 8 p. 1528 - 1531

Three 7-methyl-1, 4-dioxa-7-azaspiro [4.5] decanea that contained either the benzyl, 3- indolylmethyl, or Cindolylmethyl group at the 6-position were synthesized via alkylation of the pyrrolidine enamine of the key intermediate, ethyl 3-oxopiperidine-l-carbox...

2-Benzyl-and 2-Phenyl-3, 4-dihydroxyphenyl-alanine1

: Burger,A.B. et al. Journal of Medicinal Chemistry, 1963 , vol. 6, p. 614 - 616

solution-of 0.4 g.(17.5 mmoles) of sddium in 40 ml. of absolute ethanol were added 3.8 g.(17.5 mmoles) of diethyl acetamidomalonate and crude 2-phenylveratryl chloride [prepared from 5.35 g.(2.5 mmoles'i of 3-phenj lveratrole]. Bfter 9 hr. of refluxing and st...

Substituted thiadiazolines as inhibitors of central nervous system carbonic anhydrase

: Lukes,J.J.; Nieforth,K.A. Journal of Medicinal Chemistry, 1975 , vol. 18, p. 351 - 354

A series (24-30) of substituted thiadiazolines was synthesized and tested for in c, itro carbonic anhydrase inhibition and for protective ability against pentylenetetrazole-induced convulsions. ED;,)(pentylenetetrazole protection). TD, o, and LD:,, values are...

Synthesis of 3, 4-dihydroxy-5-fluoro-DL-Phenylalanine and 3, 4-Dihydroxy-5-[fluorine-18] fluoro-DL-phenylalanine

: Firnau,G. et al. Journal of Medicinal Chemistry, 1973 , vol. 16, p. 416 - 418

F 170 62b aQuantitative. bCalculated from 6. about two-thirds of lesions. Dihydroxyphenylalanine (DOPA) enters healthy, mature brain capillaries where it is decarboxylated to dopamine. Dopamine can be concentrated in the capillaries by an amine oxidase inhibi...

Some amino and ammonio nitrogen mustard analogs

: Price,C.C. et al. Journal of Medicinal Chemistry, 1965 , vol. 8, p. 650 - 655

Biological data on these compounds were reported in detail The amino mustards were found to have a single LD5o of 3-8 mg./kg. compared to 3 mg./kg. for HS-2. In suppression of Ehrlich ascites tumor, IIa was the most active compound, being slightly superior to...

Synthesis and hypoglycemic activity of phenylalkyloxiranecarboxylic acid derivatives

: Eistetter, Klaus; Wolf, Horst P. O. Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 109 - 113

A series of new 2-(phenylalkyl) oxirane-2-carboxylic acids has been synthesized and studied for its effects on the concentration of blood glucose. Most of the compounds exhibit remarkable blood glucose lowering activities in fasted rats. Structure-activity st...

Synthesis and antitumor evaluation of selected 5, 6-disubstituted 1 (2) H-indazole-4, 7-diones

: Conway, Gregory A.; Loeffler, Larry J.; Hall, Iris H. Journal of Medicinal Chemistry, 1983 , vol. 26, # 6 p. 876 - 884

A series of novel aziridinyl-substituted 1 (2) H-indazole-4, 7-diones and related 1 (2) H- indazole-4, 7-diones was synthesized and tested against Ehrlich ascites carcinoma growth in male CF1 mice. Ten of the test compounds, including two aziridinyl-substitut...

Functionalized DL-amino acid derivatives. Potent new agents for the treatment of epilepsy

: Conley, Judith D.; Kohn, Harold Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 567 - 574

Structural analogues of the potent known anticonvulsant agent N-acetyl-DL-alanine N- benzylamide (la) have been prepared (16 examples). The pharmacological activities of these products were evaluated in the maximal electroshock seizure (MES), the subcutaneous...