Theophylline derivatives as potential histamine H-3-receptor antagonists
Previous results of histamine H-3-receptors investigations allowed to formulate a general structure of H-3-receptor antagonists. According to this model a series of compounds were obtained. As heterocycles they contained a theophylline moiety connected with a polar group (amine, ester, amide, and th...
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Published in | Pharmazie Vol. 53; no. 8; pp. 518 - 521 |
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Main Authors | , |
Format | Journal Article |
Language | English |
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Govi-Verlag Pharmazeutischer Verlag Gmbh
01.08.1998
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Abstract | Previous results of histamine H-3-receptors investigations allowed to formulate a general structure of H-3-receptor antagonists. According to this model a series of compounds were obtained. As heterocycles they contained a theophylline moiety connected with a polar group (amine, ester, amide, and thiourea function) via an alkyl chain linked by a spacer to a lipophilic residue. The common distance between xanthine moiety and lipophilic rest was a six-link-chain. Selected compounds did not show significant H-3-receptor antagonist activity and were weak antagonists at histamine H-1-receptors. |
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AbstractList | Previous results of histamine H-3-receptors investigations allowed to formulate a general structure of H-3-receptor antagonists. According to this model a series of compounds were obtained. As heterocycles they contained a theophylline moiety connected with a polar group (amine, ester, amide, and thiourea function) via an alkyl chain linked by a spacer to a lipophilic residue. The common distance between xanthine moiety and lipophilic rest was a six-link-chain. Selected compounds did not show significant H-3-receptor antagonist activity and were weak antagonists at histamine H-1-receptors. |
Author | Kiec-Kononowicz, K Cegla, MT |
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Keywords | H-3 RECEPTOR ANTAGONISTS |
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References | SCHLICKER, E (WOS:A1994PH43400053) 1994; 113 POIZOT, A (WOS:A1986A963200017) 1986; 36-1 Huls, A (WOS:A1996VN93600001) 1996; 329 Stark, H (WOS:A1997XN60800003) 1997; 52 LIPP R (WOS:000075458900003.11) 1992; 16 SCHWARTZ, JC (WOS:A1990DC16000003) 1990; 30 LIGNEAU, X (WOS:A1994PN49000059) 1994; 271 VANROSSUM, JM (WOS:A19635501A00026) 1963; 143 ONO, N (WOS:A1978FL95700043) 1978; 51 Stark, Holger (BCI:BCI199699107678) 1996; 21 Leurs, R (MEDLINE:8545536) 1995; 45 ECKSTEIN, MARIAN (BCI:BCI19654600070719) 1964; 16 ARRANG, JM (WOS:A1983QM85800080) 1983; 302 PASCAL, JC (WOS:A1985AFX8900019) 1985; 28 ECKSTEIN M (WOS:000075458900003.4) 1971; 6 ECKSTEIN M (WOS:000075458900003.5) 1962; 14 ZELNIK, R (WOS:A1959WM53800097) 1959 KAMINSKI, ZJ (WOS:A1987K276800018) 1987 LENNARTZ, HG (WOS:A1978FE30400005) 1978; 13 ABOUGHARBIA, M (WOS:A1995RY25500018) 1995; 38 STARK, H (WOS:A1994PK81700007) 1994; 29 |
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ADDITION NUCLEOPHILE DE LA THEOPHYLLINE ET DE LA THEOBROMINE AUX COMPOSES ETHYLENIQUES - APPLICATION A LALCOYLATION AU MOYEN DE BASES DE MANNICH publication-title: BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE contributor: fullname: ZELNIK, R – volume: 45 start-page: 107 year: 1995 ident: MEDLINE:8545536 article-title: The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor. publication-title: Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques contributor: fullname: Leurs, R – volume: 52 start-page: 495 year: 1997 ident: WOS:A1997XN60800003 article-title: Search for novel leads for histamine H-3-receptor antagonists: oxygen-containing derivatives publication-title: PHARMAZIE contributor: fullname: Stark, H – volume: 38 start-page: 4026 year: 1995 ident: WOS:A1995RY25500018 article-title: NEW ANTIHISTAMINES - SUBSTITUTED PIPERAZINE AND PIPERIDINE-DERIVATIVES AS NOVEL H-1-ANTAGONISTS publication-title: JOURNAL OF MEDICINAL CHEMISTRY contributor: fullname: ABOUGHARBIA, M – start-page: 917 year: 1987 ident: WOS:A1987K276800018 article-title: 2-CHLORO-4,6-DIMETHOXY-1,3,5-TRIAZINE - A NEW COUPLING REAGENT FOR PEPTIDE-SYNTHESIS publication-title: SYNTHESIS-STUTTGART contributor: fullname: KAMINSKI, ZJ – volume: 14 start-page: 41 year: 1962 ident: WOS:000075458900003.5 publication-title: DISSERTATIONES PHARM contributor: fullname: ECKSTEIN M – volume: 29 start-page: 695 year: 1994 ident: WOS:A1994PK81700007 article-title: ACYLATED AND ALKYLATED HISTAMINE DERIVATIVES AS NEW HISTAMINE H-3 RECEPTOR ANTAGONISTS publication-title: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY contributor: fullname: STARK, H – volume: 329 start-page: 379 year: 1996 ident: WOS:A1996VN93600001 article-title: Novel histamine H-3-receptor antagonists with benzyl ether structure or related moieties: Synthesis and structure-activity relationships publication-title: ARCHIV DER PHARMAZIE contributor: fullname: Huls, A – volume: 51 start-page: 2401 year: 1978 ident: WOS:A1978FL95700043 article-title: CONVENIENT PROCEDURE FOR ESTERIFICATION OF CARBOXYLIC-ACIDS publication-title: BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN contributor: fullname: ONO, N – volume: 21 start-page: 507 year: 1996 ident: BCI:BCI199699107678 article-title: Developments of histamine H-3-receptor antagonists publication-title: Drugs of the Future contributor: fullname: Stark, Holger |
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Snippet | Previous results of histamine H-3-receptors investigations allowed to formulate a general structure of H-3-receptor antagonists. According to this model a... |
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SubjectTerms | Chemistry Chemistry, Medicinal Chemistry, Multidisciplinary Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology |
Title | Theophylline derivatives as potential histamine H-3-receptor antagonists |
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