Výsledky vyhledávání - "Robert M. DeMarinis"

Arylazide photoaffinity probe for α2-adrenoceptors

Autor: Robert J. Lefkowitz, Robert M. DeMarinis, John W. Regan

Publikováno v: Biochemical Pharmacology. 34:3667-3672

An arylazide photoaffinity probe for alpha 2-adrenoceptors has been developed and characterized. The compound, 3-methyl-6-chloro-9-azido-1H-2,3,4,5-tetrahydro-3-benzazepine (SKF 102229), had a Ki for the human platelet alpha 2-adrenoceptor of approxi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7658c5ac0ca10148c86beacfd9c61075
https://doi.org/10.1016/0006-2952(85)90228-x

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Biological and chemotherapeutic studies on three semisynthetic cephamycins

Autor: Jerry A. Weisbach, Joseph R. Guarini, Paul Actor, Joseph V. Uri, Donald Pitkin, Lillian Phillips, Robert M. DeMarinis

Publikováno v: The Journal of Antibiotics. 31:82-91

Three semisynthetic cephamycin antibiotics (7alpha-methoxy-cephalosporins), SK&F 73678, SK&F 83088 (CS-1170) and cefoxitin, have been found to possess favorable biological and chemotherapeutic properties. All three cephamycins are active in vitro aga

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b680287ff0f6fbc4a4d6e62f6b021c8
https://doi.org/10.7164/antibiotics.31.82

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Nuclear analogs of β-lactam antibiotics 8. Stereospecific synthesis of a C-3 methoxylated monocyclic s-lactam

Autor: William M. Bryan, Robert M. DeMarinis

Publikováno v: Tetrahedron Letters. 23:731-734

Methoxylation of 1 (R = PhOCH2CO) occurred stereospecifically from the α-face as determined by x-ray crystallography to provide 2 which was converted to 4 whose in vitro antimicrobial activity was determined.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e3e73f2e111310c2bb703bd997502b8a
https://doi.org/10.1016/s0040-4039(00)86933-6

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alpha.-Adrenergic agents. 1. Direct-acting .alpha.1 agonists related to methoxamine

Autor: J. P. Hieble, D H Shah, Robert M. DeMarinis, Robert G. Pendleton, W. M. Bryan

Publikováno v: Journal of Medicinal Chemistry. 24:1432-1437

A series of phenylethylamines related to methoxamine has been prepared and evaluated for direct alpha 1-receptor agonist activity. It has been observed that for open-chain compounds such as methoxamine, in which the amine-containing portion is free t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c3df075a0eb8aa885e3be54b0431810
https://doi.org/10.1021/jm00144a012

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Dopamine receptor agonists: 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol and a series of related 3-benzazepines

Autor: H. M. Sarau, M. Brenner, R. G. Franz, Stephen T. Ross, James W. Wilson, Hieble Jp, Robert M. DeMarinis

Publikováno v: Journal of Medicinal Chemistry. 29:733-740

The N-allyl derivative (SK&F 85174) of 6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-dio l (SK&F 82526) not only retains the exceptional D-1 agonist potency of its parent but also displays reasonably potent D-2 agonist activity

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2543607ee759466503cdb4f07a8ba3a
https://doi.org/10.1021/jm00155a024

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alpha.-Adrenergic agents. 2. Synthesis and .alpha.1-agonist activity of 2-aminotetralins

Autor: D H Shah, R. F. Hall, Robert G. Pendleton, J. P. Hieble, Robert M. DeMarinis

Publikováno v: Journal of Medicinal Chemistry. 25:136-141

Substituted 2-aminotetralins are potent, selective, direct-acting agonists at postjunctional alpha 1 receptors. Within this series, substituent alterations on the ring, as well as on the nitrogen, change the potency of compounds by over three orders

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::930087c970f546ad621bba5c050fba04
https://doi.org/10.1021/jm00344a009

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N-[2-hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide. A potent agonist which releases intracellular calcium by activation of .alpha.1-adrenoceptors

Autor: Robert M. DeMarinis, K. F. Jim, W. D. Matthews, J. P. Hieble, P. G. Lavanchy

Publikováno v: Journal of Medicinal Chemistry. 28:245-248

N-[2-Hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide (SK&F 102652) has been prepared and characterized pharmacologically. It is a potent agonist with an EC50 of 25 nM at alpha 1-adrenoceptors as determined in the isolated perfused rabbit ea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99b0f540220b2b225aa452185a5cfc21
https://doi.org/10.1021/jm00380a017

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Dopamine agonists related to 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol, 6-position modifications

Autor: R. G. Franz, Stephen T. Ross, James W. Wilson, Gregory Gallagher, Robert M. DeMarinis, Henry M. Sarau, J. P. Hieble, M. Brenner

Publikováno v: Journal of Medicinal Chemistry. 30:35-40

The N-allyl derivative (SKF 85174) of 6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol (SKF 82526) retains the DA-1 agonist potency of the latter compound but unlike the parent also shows substantial DA-2 agonist activity. In

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e4642f4069ac4c44a607c0a3edbc28b
https://doi.org/10.1021/jm00384a006

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