Dihydropyridine, eine neue Gruppe stark wirksamer Coronartherapeutika

Bossert, F.; Vater, W.

doi:10.1007/bf00598745

Cited by 129 publications

(17 citation statements)

References 1 publication

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“…While the R enantiomer was found to be an agonist, the Senantiomer was found to be antagonist, S-enantiomer is 50-fold more active than R-enantiomer in respect to receptor binding [59]. H 160/51 is an analog of calcium antagonist felodipine.…”

Section: Structure-activity Relationshipsmentioning

confidence: 98%

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Fused 1,4-Dihydropyridines as Potential Calcium Modulatory Compounds

Şafak¹,

Şimşek²

2006

MRMC

118

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1,4-Dihydropyridine (1,4-DHP) derivatives nifedipine of which the prototype, are the most popular drugs having calcium antagonistic activity. Fused 1,4-dihydropyridines (DHPs) have also exhibit calcium modulatory activities. In this article, we emphasize calcium channels and fused 1,4-DHP derivatives affecting calcium channels. In addition, the basic considerations of synthesis, metabolism, structure-activity relationships and the latest developments on fused 1,4-DHP derivatives will be reviewed. This review also has extended examples of fused 1,4-DHP derivatives having cited activities synthesized by our group.

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Section: Structure-activity Relationshipsmentioning

confidence: 98%

“…This reaction is still widely used for 1,4-DHP synthesis [58]. Bossert and Vater starting with condensed pyrane derivative and proceeding via quinoline [59].…”

Section: Calcium Channel Modulatory Compoundsmentioning

confidence: 99%

Fused 1,4-Dihydropyridines as Potential Calcium Modulatory Compounds

Şafak¹,

Şimşek²

2006

MRMC

118

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“…The Vater, 1971). The heart has remained the focus of microsphere method allows regional blood flow to attention, even though it is now well known that these many vascular beds to be measured at the same time drugs have effects on other parts of the circulation (Heymann, Payne, Hoffman & Rudolph, 1977).…”

Section: Introductionmentioning

confidence: 99%

Calcium antagonist and the peripheral circulation: differences and similarities between PY 108–068, nicardipine, verapamil and diltiazem

Hof

1983

British J Pharmacology

128

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1 The effects of two dihydropyridines, PY 108-068 (PY) and nicardipine (N), and two other calcium antagonists, verapamil (V) and diltiazem (D), on regional blood flow were measured in open-chest cats, anaesthetized with chloralose-urethane. 2 Each substance was infused at 3 different dose rates, each for 10 min. The total doses given were 5 plus 10 plus 35 (total of 50) jig/kg for PY, 10 plus 20 plus 70 (total of 100) jug/kg for N and 100 plus 200 plus 700 (total of 1000) Ag/kg for V and D.3 All substances lowered blood pressure and increased total peripheral conductance. Heart rate was lowered only by V, D and PY. Cardiac output was markedly increased only by the diyhydroypridine derivatives; D had small and V almost no effects. 4 AU substances increased coronary flow and redistributed it in favour of the subepicardial layer. All substances also increased blood flow to the brain. The effects of verapamil were comparatively small. 5 Skeletal muscle flow was increased strongly by the two dihydropyridine derivatives. D and V had negligible effects. 6 Blood flow to stomach and small intestine was only slightly increased. Flow to the kidneys increased slightly in diltiazem-treated animals but did not change with all other treatments. Flow to the liver, the adrenals, and the spleen remained unchanged or showed a tendency to decrease. 7 The organ conductances which reflect the active changes in vascular tone better than blood flow values, showed that there was a tendency towards vasodilatation even in most organs where blood flow tended to decrease.8 Results obtained in an earlier series of experiments with nifedipine were very similar to those described here for N, except that nifedipine was about twice as potent. 9 Calcium antagonists were thus neither general peripheral vasodilators nor did they show a uniform pattern of preferential sites of action. The most important common features were increases in coronary and cerebral blood flow and the most important differences the divergent effects of the dihydropyridines on one side and V and D on the other side on skeletal muscle flow. The size of this vascular bed may help to explain why dihydropyridines appear to be particularly potent as peripheral vasodilators.

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“…Chiral 1,4-dihydropyridines [26][27][28] have been employed as synthetic intermediates for a wide variety of compounds such as natural products [29], calcium channel blockers [30], and NADH models [31]. Because of the importance of C-4 chirality with respect to the pharmacological activity of 4-aryl-1,4-dihydropyridines, various studies have been devoted to the preparation of unsymmetrical 1,4-dihydropyidine-3,5-diesters, such as nitrendipine [32], felodipine [33,34], and also to the preparation of unsymmetrical 1,4-dihydropyridines, in which an alkoxycarbonyl (ester) group and an alkanoyl (keto) group are located on the 3-and 5-positions, respectively [35][36][37][38].…”

Section: Introductionmentioning

confidence: 99%

Photosensitized oxidation of unsymmetrical 1,4-dihydropyridines

Memarian

Abdoli‐Senejani

Tangestaninejad

2006

JICS

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Photosensitized oxidation of unsymmetrically substituted 1,4-dihydropyridines using dye sensitizers methylene blue, rose bengal and tetraphenylporphyrin by taking visible light source resulted in the aromatization of dihydropyridine ring and formation of the corresponding pyridine derivatives. Comparison of the results obtained under photosensitized reaction with those obtained by direct photo-oxidation indicated a very fast and smooth reaction of these compounds and formation of pyridine derivatives using theses dyestuffs.

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Dihydropyridine, eine neue Gruppe stark wirksamer Coronartherapeutika

Cited by 129 publications

References 1 publication

Fused 1,4-Dihydropyridines as Potential Calcium Modulatory Compounds

Fused 1,4-Dihydropyridines as Potential Calcium Modulatory Compounds

Calcium antagonist and the peripheral circulation: differences and similarities between PY 108–068, nicardipine, verapamil and diltiazem

Photosensitized oxidation of unsymmetrical 1,4-dihydropyridines

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