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Showing 1 to 12 of 850 entries
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Molecular dynamics: new advances in drug discovery.

European journal of medicinal chemistry

Milardi D, Pappalardo M.
PMID: 25466447
Eur J Med Chem. 2015 Feb 16;91:1-3. doi: 10.1016/j.ejmech.2014.10.078. Epub 2014 Nov 01.

No abstract available.

Synthesis of oxypropanolamine derivatives of 3,4-dihydro-2H-1,4-benzoxazine, beta-adrenergic affinity, inotropic, chronotropic and coronary vasodilating activities.

European journal of medicinal chemistry

Iakovou K, Kazanis M, Vavayannis A, Bruni G, Romeo MR, Massarelli P, Teramoto S, Fujiki H, Mori T.
PMID: 10889316
Eur J Med Chem. 1999 Nov 01;34(11):903-917. doi: 10.1016/s0223-5234(99)00109-9.

Aseries of oxypropanolamine derivatives of 3,4-dihydro-2H-1,4-benzoxazine were synthesized and evaluated for inotropic, chronotropic and coronary vasodilating activities in the canine heart, affinity to beta(1)-adrenergic receptor in turkey erythrocytes and affinity to the beta(2)-adrenergic receptor in the rat lung. Among...

Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT(4) receptor agonists.

European journal of medicinal chemistry

Itoh K, Kanzaki K, Ikebe T, Kuroita T, Tomozane H, Sonda S, Sato N, Haga K, Kawakita T.
PMID: 10889321
Eur J Med Chem. 1999 Nov 01;34(11):977-989. doi: 10.1016/s0223-5234(99)00158-0.

A number of new carboxamide derivatives were synthesized. The affinity of these compounds for the serotoninergic 5-HT(4) receptor was evaluated by use of radioligand-binding techniques. The agonistic activity was evaluated as the contractile effect of the ascending colon isolated...

Synthesis and anti-inflammatory activity of N-substituted 2-oxo-2H-1-benzopyran-3-carboxamides and their 2-iminoanalogues.

European journal of medicinal chemistry

Bylov IE, Vasylyev MV, Bilokin YV.
PMID: 10889323
Eur J Med Chem. 1999 Nov 01;34(11):997-1001. doi: 10.1016/s0223-5234(99)00119-1.

Aseries of N-arylsubstituted 2-imino-2H-1-benzopyran-3-carboxamides 3a and b and 2-oxo-2H-1-benzopyran-3-carboxamides 4a-h were synthesized and evaluated for their anti-inflammatory activity in carrageenan-induced rat paw oedema assays and in acetic acid-induced peritonitis tests in albino rats. The resulting products were found to...

Synthesis, antibacterial activity evaluation and QSAR studies of novel dispiropyrrolidines.

European journal of medicinal chemistry

Karthikeyan K, Sivakumar PM, Doble M, Perumal PT.
PMID: 20580853
Eur J Med Chem. 2010 May 06; doi: 10.1016/j.ejmech.2010.04.035. Epub 2010 May 06.

A series of novel dispiropyrrolidines have been synthesized through 1,3-dipolar cycloaddition of an azomethine ylide generated from sarcosine and isatin with the dipolarophile 3-benzylidene-1-methyl-pyrrolidine-2,5-dione. Their antibacterial activity was evaluated against Bacillus subtilis NCIM 2718, Staphylococcus aureus NCIM5021, Salmonella typhi...

WITHDRAWN: Discovery of 5-benzylidene(thio) barbiturates as a new class of mushroom tyrosinase inhibitors.

European journal of medicinal chemistry

Cao R, Yan Q, Shi B, Bai Z, Ren Z.
PMID: 21349609
Eur J Med Chem. 2011 Feb 03; doi: 10.1016/j.ejmech.2011.01.058. Epub 2011 Feb 03.

This article has been withdrawn at the request of the authors. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy.

Spiranes 6. Ring A homologues of N-benzyloxy-2-azaspiro[4.4]nonane-1,3-dione. Synthesis, X-ray analysis and anticonvulsant evaluation.

European journal of medicinal chemistry

Alexander M, Stables J, Ciechanowicz-Rutkowska M, Hursthouse M, Hibbs D, Edafiogho I, Farrar V, Moore J, Scott K.
PMID: 22026934
Eur J Med Chem. 1996;31(10):787-95. doi: 10.1016/0223-5234(96)83972-9.

A series of spirosuccinimides was synthesized and evaluated for anticonvulsant activity. The study was designed to determine the effect of varying the carbocyclic (ring A) nucleus, while maintaining the heterocyclic ring constant, on anticonvulsant activity. Results indicate that maximum...

Stereospecificity of myofibrillar calcium sensitivity and PDE inhibition in cardiotonic thiadiazinones.

European journal of medicinal chemistry

Nadler G, Delimoge I, Lahouratate P, Leger I, Morvan M, Zimmermann R.
PMID: 22026936
Eur J Med Chem. 1996;31(10):805-12. doi: 10.1016/0223-5234(96)83974-2.

In pyridazinone or thiadiazinone cardiotonic agents with one chiral centre, the PDE inhibitory action resides mainly in one enantiomer and the myofibrillar calcium sensitization mainly in the other. This phenomenon is observed when the chiral centre is located on...

Synthesis and anticonvulsant activity of some 4-nitro-N-phenylbenzamides.

European journal of medicinal chemistry

Bailleux V, Vallée L, Nuyts J, Hamoir G, Poupaert J, Stables J, Vamecq J.
PMID: 22625428
Eur J Med Chem. 1995;30(5):439-44. doi: 10.1016/0223-5234(96)88254-7.

A short series of 4-nitro-N-phenylbenzamides was synthesized and evaluated for anticonvulsant properties and neurotoxicity. In mice dosed intraperitoneally, three of the four 4-nitro-N-phenylbenzamides were efficient in the maximal electroshock-induced seizure (MES) test, especially N-(2,6-dimethylphenyl)-4-nitrobenzamide (ED(50) value in the MES...

Synthesis of dicationic diaryltriazines nucleic acid binding agents.

European journal of medicinal chemistry

Spychala J, Boykin D, Wilson W, Zhao M, Tidwell R, Dykstra C, Hall J, Jones S, Schinazi R.
PMID: 21556310
Eur J Med Chem. 1994;29(5):363-367. doi: 10.1016/0223-5234(94)90061-2.

- The synthesis of 2,4-bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-1,3,5-triazine 6a and 2,4-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-1,3,5-triazine 6b in 3 steps from either 4-bromobenzamidine or 4-(carbamoyl)benzamidine is reported. The synthesis of 4,6-bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-2-dimethylamino-1,3,5-triazine 9a and 4,6-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-2-dimethylamino-1,3,5-triazine 9b in 2 steps from 1,4-dicyanobenzene is also described. The compounds 6b and...

Multifunctional compounds: smart molecules for multifactorial diseases.

European journal of medicinal chemistry

Bansal Y, Silakari O.
PMID: 24565571
Eur J Med Chem. 2014 Apr 09;76:31-42. doi: 10.1016/j.ejmech.2014.01.060. Epub 2014 Jan 31.

Multifunctional compounds (MFCs) are designed broadly as hybrid or conjugated drugs or as chimeric drugs from two or more pharmacophores/drugs having specific pharmacological activities. These are capable of eliciting multiple pharmacological actions and have emerged as magic bullets in...

Corrigendum to "Novel natural compounds from endophytic fungi with anticancer activity" [EJMECH 156, (2018) 316-343].

European journal of medicinal chemistry

Li SJ, Zhang X, Wang XH, Zhao CQ.
PMID: 30165343
Eur J Med Chem. 2018 Sep 05;157:960-961. doi: 10.1016/j.ejmech.2018.08.041. Epub 2018 Aug 27.

No abstract available.

Showing 1 to 12 of 850 entries