Ulrich Rose - Academia.edu (original) (raw)
Papers by Ulrich Rose
Planta Medica, Aug 24, 2006
ChemInform, Aug 22, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
PubMed, Nov 1, 1991
In the course of investigations on structure-activity relationships of fostedil-and sulmazole-ana... more In the course of investigations on structure-activity relationships of fostedil-and sulmazole-analogously fused 5-membered heterocycles, 1,3-benzimidazoles were obtained by simple cyclisation. In vitro experiments on isolated organs demonstrate markedly positive inotropic effects of some derivatives, whereas others exert both relaxing activity on smooth musculature in vitro and antihypertensive effects in vivo. Moreover they exhibit fungicide properties in vitro.
PubMed, 1991
The symmetrically substituted dihydropyridine-dicarboxylate 3 exerts only weak calcium antagonist... more The symmetrically substituted dihydropyridine-dicarboxylate 3 exerts only weak calcium antagonistic activity on smooth muscles compared with the standard nifedipine. On electrically stimulated, left guinea pig-atria and particularly on electrically stimulated papillary muscles marked positive inotropic effects are registered. They can be attributed to release of catecholamines from intracellular stores.
PubMed, Apr 1, 1986
The nucleophilic substitution of one chlorine atom in 2,4-dichloro-6-(dihexylamino)-1,3,5-triazin... more The nucleophilic substitution of one chlorine atom in 2,4-dichloro-6-(dihexylamino)-1,3,5-triazine (1) by primary (2a-b) or secondary (2c) amines leads to the aliphatically substituted chloro-dihexylamino-1,3,5-triazines (3a-c) Structures of type 3 may be characterized by the spectroscopic data. In the mass spectra, the complete degradation of the alkyl groupings is striking and manifested in a series of consecutive peaks with differences of 14 between each other. Antiviral activity is exhibited by 3a through an inhibitory effect towards vaccinia virus and by 3b as interferon inductor towards encephalomyocarditis virus. Moreover, 3a and 3b exhibit a strong activity towards Trichomonas vaginalis. Additionally, 3a is capable of exerting temperature lowering and anthelminthic effects.
PubMed, Mar 1, 1991
Hexahydroquinolinones of type 6 are accessible from Hantzsch-like cyclization of 1,3-cyclohexaned... more Hexahydroquinolinones of type 6 are accessible from Hantzsch-like cyclization of 1,3-cyclohexanedione with aromatic aldehydes and different beta-aminocrotonates and acetoacetates/ammonia, respectively. Reaction with pyridiniumbromideperbromide leads to the octahydrofuro[3,4-b] guinoline-diones 6h and 6i. 6j was obtained by N-alkylation. Positive inotropic effects were observed on electrically stimulated left atria of guinea pigs whereas BaCl2-induced contractions of the ileum were inhibited in a dose dependent manner. On electrically stimulated guinea pig papillary muscle 6h exhibits contractility promoting effects which can be attributed to calcium agonism.
PubMed, Nov 1, 1989
The anellated dihydropyridines 4a-l can be gained by Hantzsch-like synthesis from 5,5-dimethylcyc... more The anellated dihydropyridines 4a-l can be gained by Hantzsch-like synthesis from 5,5-dimethylcyclohexanedione (1), the aromatic aldehydes 2a-l and methyl-beta-aminocrotonate (3). Cyclisation of the side chains with bromosuccinimide or pyridiniumbromideperbromide leads to the octahydrofuro[3,4-b]chinoline-diones 4m-p. Structures of type 4 are characterized by the spectroscopic data. Positive inotropic effects, caused by calcium agonism, are exerted by the tested substances at the isolated, electrically stimulated left guinea pig atrium, 4j being the most potent with an intrinsic activity of 0.79, compared with ethyl 4-[2-(difluoromethoxy)phenyl]-1, 4,5,7-tetrahydro-2-methyl-5-oxo-furo[3,4-b]pyridine-3-carboxylate. BaCl2-induced contractions at the guinea pig ileum are suppressed dose-dependently.
Journal of Medicinal Chemistry, Jun 1, 1992
Enantiomerically pure hexahydroquinolinones of the structural type 9 were prepared by a variation... more Enantiomerically pure hexahydroquinolinones of the structural type 9 were prepared by a variation of the Hantzsch synthesis in which an optically active acetoacetate served as a chiral auxiliary reagent. Determinations of the de and ee values are described. The absolute configurations of the optically pure products were characterized by single-crystal X-ray analysis. The antipodes 9a and 9b exhibited calcium antagonistic activities on smooth musculature; the (S)-(-)-enantiomer 9b was the more potent compound with regard to the EC50 values which differed by a factor of 100; the intrinsic activity of 9b was 1.2, compared with a value of 0.54 for 9a. On the other hand, R-(+)-9a exerted positive inotropic effects on electrically stimulated atria. The cause of these effects is discussed.
ChemInform, Dec 1, 1987
ChemInform Abstract Die gemäss dem Formelschema synthetisierten 2-Cyan-aminopyrimidine (III) zeic... more ChemInform Abstract Die gemäss dem Formelschema synthetisierten 2-Cyan-aminopyrimidine (III) zeichnen sich durch trichomonazide, antivirale und antimykotische Wirkung aus. (1 H-, 1 3C-NMR-, IR-, MS-Daten).
ChemInform, Mar 31, 1987
ChemInform Abstract The title compounds (III) are obtained by reacting the triazine (I) with one ... more ChemInform Abstract The title compounds (III) are obtained by reacting the triazine (I) with one or two equivalents of the aryl mercaptans (II). (IR-, 1H-NMR-, MS-data, MS-discussion).
ChemInform, Oct 16, 1990
ChemInform Abstract The cyclohexanedione (I) is coupled with the aromatic aldehydes (II) to give ... more ChemInform Abstract The cyclohexanedione (I) is coupled with the aromatic aldehydes (II) to give arylmethylenecyclohexanediones which react in situ with the aminocrotonate (III) to yield the hexahydroquinolinones (IV). These have positive inotropic effects at electrically stimulated left guinea pig atrium. BaCl2-induced contractions of guinea pig ileum are supressed depending on the dose.
Chemischer Informationsdienst, Jun 25, 1985
ChemInform Abstract Die nach bekannten Verfahren hergestellten Triazine (III) sind herbizid und a... more ChemInform Abstract Die nach bekannten Verfahren hergestellten Triazine (III) sind herbizid und algizid wirksam. (IR-, NMR-, MS-Daten).
ChemInform, Aug 21, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
ChemInform, Aug 22, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Chemischer Informationsdienst, Jul 8, 1986
ChemInform Abstract Durch Umsetzung der Aniline (II) mit dem 2,4-Dichlor-6-(dicyclohexylamino)-tr... more ChemInform Abstract Durch Umsetzung der Aniline (II) mit dem 2,4-Dichlor-6-(dicyclohexylamino)-triazin (I) werden die Triazin-Derivate (III) hergestellt. Umfassend diskutiert werden die Massenspektren. Es werden herbizide und antidiabetische Wirkungen angegeben. (IR-, MS-, 1H-NMR-Daten).
Chemischer Informationsdienst, 1986
ChemInform Abstract Aus dem Dichlor-amino-triazin (I) werden mit den sekundären Aminen (II) die u... more ChemInform Abstract Aus dem Dichlor-amino-triazin (I) werden mit den sekundären Aminen (II) die unsymmetrischen 1,3-Diamino-5-chlor-s-triazine (III) erhalten, die antidiabetische, trichomonazide, antivirale und anthelmintische Wirkung zeigen. (IR-, NMR-, MS-Daten).
Planta Medica, Aug 24, 2006
ChemInform, Aug 22, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
PubMed, Nov 1, 1991
In the course of investigations on structure-activity relationships of fostedil-and sulmazole-ana... more In the course of investigations on structure-activity relationships of fostedil-and sulmazole-analogously fused 5-membered heterocycles, 1,3-benzimidazoles were obtained by simple cyclisation. In vitro experiments on isolated organs demonstrate markedly positive inotropic effects of some derivatives, whereas others exert both relaxing activity on smooth musculature in vitro and antihypertensive effects in vivo. Moreover they exhibit fungicide properties in vitro.
PubMed, 1991
The symmetrically substituted dihydropyridine-dicarboxylate 3 exerts only weak calcium antagonist... more The symmetrically substituted dihydropyridine-dicarboxylate 3 exerts only weak calcium antagonistic activity on smooth muscles compared with the standard nifedipine. On electrically stimulated, left guinea pig-atria and particularly on electrically stimulated papillary muscles marked positive inotropic effects are registered. They can be attributed to release of catecholamines from intracellular stores.
PubMed, Apr 1, 1986
The nucleophilic substitution of one chlorine atom in 2,4-dichloro-6-(dihexylamino)-1,3,5-triazin... more The nucleophilic substitution of one chlorine atom in 2,4-dichloro-6-(dihexylamino)-1,3,5-triazine (1) by primary (2a-b) or secondary (2c) amines leads to the aliphatically substituted chloro-dihexylamino-1,3,5-triazines (3a-c) Structures of type 3 may be characterized by the spectroscopic data. In the mass spectra, the complete degradation of the alkyl groupings is striking and manifested in a series of consecutive peaks with differences of 14 between each other. Antiviral activity is exhibited by 3a through an inhibitory effect towards vaccinia virus and by 3b as interferon inductor towards encephalomyocarditis virus. Moreover, 3a and 3b exhibit a strong activity towards Trichomonas vaginalis. Additionally, 3a is capable of exerting temperature lowering and anthelminthic effects.
PubMed, Mar 1, 1991
Hexahydroquinolinones of type 6 are accessible from Hantzsch-like cyclization of 1,3-cyclohexaned... more Hexahydroquinolinones of type 6 are accessible from Hantzsch-like cyclization of 1,3-cyclohexanedione with aromatic aldehydes and different beta-aminocrotonates and acetoacetates/ammonia, respectively. Reaction with pyridiniumbromideperbromide leads to the octahydrofuro[3,4-b] guinoline-diones 6h and 6i. 6j was obtained by N-alkylation. Positive inotropic effects were observed on electrically stimulated left atria of guinea pigs whereas BaCl2-induced contractions of the ileum were inhibited in a dose dependent manner. On electrically stimulated guinea pig papillary muscle 6h exhibits contractility promoting effects which can be attributed to calcium agonism.
PubMed, Nov 1, 1989
The anellated dihydropyridines 4a-l can be gained by Hantzsch-like synthesis from 5,5-dimethylcyc... more The anellated dihydropyridines 4a-l can be gained by Hantzsch-like synthesis from 5,5-dimethylcyclohexanedione (1), the aromatic aldehydes 2a-l and methyl-beta-aminocrotonate (3). Cyclisation of the side chains with bromosuccinimide or pyridiniumbromideperbromide leads to the octahydrofuro[3,4-b]chinoline-diones 4m-p. Structures of type 4 are characterized by the spectroscopic data. Positive inotropic effects, caused by calcium agonism, are exerted by the tested substances at the isolated, electrically stimulated left guinea pig atrium, 4j being the most potent with an intrinsic activity of 0.79, compared with ethyl 4-[2-(difluoromethoxy)phenyl]-1, 4,5,7-tetrahydro-2-methyl-5-oxo-furo[3,4-b]pyridine-3-carboxylate. BaCl2-induced contractions at the guinea pig ileum are suppressed dose-dependently.
Journal of Medicinal Chemistry, Jun 1, 1992
Enantiomerically pure hexahydroquinolinones of the structural type 9 were prepared by a variation... more Enantiomerically pure hexahydroquinolinones of the structural type 9 were prepared by a variation of the Hantzsch synthesis in which an optically active acetoacetate served as a chiral auxiliary reagent. Determinations of the de and ee values are described. The absolute configurations of the optically pure products were characterized by single-crystal X-ray analysis. The antipodes 9a and 9b exhibited calcium antagonistic activities on smooth musculature; the (S)-(-)-enantiomer 9b was the more potent compound with regard to the EC50 values which differed by a factor of 100; the intrinsic activity of 9b was 1.2, compared with a value of 0.54 for 9a. On the other hand, R-(+)-9a exerted positive inotropic effects on electrically stimulated atria. The cause of these effects is discussed.
ChemInform, Dec 1, 1987
ChemInform Abstract Die gemäss dem Formelschema synthetisierten 2-Cyan-aminopyrimidine (III) zeic... more ChemInform Abstract Die gemäss dem Formelschema synthetisierten 2-Cyan-aminopyrimidine (III) zeichnen sich durch trichomonazide, antivirale und antimykotische Wirkung aus. (1 H-, 1 3C-NMR-, IR-, MS-Daten).
ChemInform, Mar 31, 1987
ChemInform Abstract The title compounds (III) are obtained by reacting the triazine (I) with one ... more ChemInform Abstract The title compounds (III) are obtained by reacting the triazine (I) with one or two equivalents of the aryl mercaptans (II). (IR-, 1H-NMR-, MS-data, MS-discussion).
ChemInform, Oct 16, 1990
ChemInform Abstract The cyclohexanedione (I) is coupled with the aromatic aldehydes (II) to give ... more ChemInform Abstract The cyclohexanedione (I) is coupled with the aromatic aldehydes (II) to give arylmethylenecyclohexanediones which react in situ with the aminocrotonate (III) to yield the hexahydroquinolinones (IV). These have positive inotropic effects at electrically stimulated left guinea pig atrium. BaCl2-induced contractions of guinea pig ileum are supressed depending on the dose.
Chemischer Informationsdienst, Jun 25, 1985
ChemInform Abstract Die nach bekannten Verfahren hergestellten Triazine (III) sind herbizid und a... more ChemInform Abstract Die nach bekannten Verfahren hergestellten Triazine (III) sind herbizid und algizid wirksam. (IR-, NMR-, MS-Daten).
ChemInform, Aug 21, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
ChemInform, Aug 22, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Chemischer Informationsdienst, Jul 8, 1986
ChemInform Abstract Durch Umsetzung der Aniline (II) mit dem 2,4-Dichlor-6-(dicyclohexylamino)-tr... more ChemInform Abstract Durch Umsetzung der Aniline (II) mit dem 2,4-Dichlor-6-(dicyclohexylamino)-triazin (I) werden die Triazin-Derivate (III) hergestellt. Umfassend diskutiert werden die Massenspektren. Es werden herbizide und antidiabetische Wirkungen angegeben. (IR-, MS-, 1H-NMR-Daten).
Chemischer Informationsdienst, 1986
ChemInform Abstract Aus dem Dichlor-amino-triazin (I) werden mit den sekundären Aminen (II) die u... more ChemInform Abstract Aus dem Dichlor-amino-triazin (I) werden mit den sekundären Aminen (II) die unsymmetrischen 1,3-Diamino-5-chlor-s-triazine (III) erhalten, die antidiabetische, trichomonazide, antivirale und anthelmintische Wirkung zeigen. (IR-, NMR-, MS-Daten).