摘要:

AbstractA number of novel pyridazinomorphinans have been synthesized by the inverse electron demand Diels‐Alder reaction of various 3,6‐disubstituted 1,2,4,5‐tetrazines with enamines derived from dihydrocodeinone and with codeinone. Reduction of some of the pyridazinomorphinans did not furnish the expected pyrroloepoxymorphinans; in all cases investigated reductive cleavage of the epoxybridge was observed to yield dihydropyridazino‐ or pyrrolomorphinans. The structures of all new compounds were assigned by the spectral data, that of the cycloadduct of codeinone was additionally verified by X‐ray crystallography. Compounds5a, 8, 11a, and16have been evaluated for their affinity at μ and κ opioid receptors in radioligand binding assays. Their ability to inhibit [3H]DAMGO binding at μ and [3H]U 69.593 binding at κ receptors, respectively as compared to codeine has been foun

ISSN:0365-6233    

DOI:10.1002/ardp.19973300602

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractA series of amidrazones was prepared and characterized by1H NMR and mass spectroscopy. The substances were tested againstM. tuberculosis, M. avium, M. intracellulare, andM. lufu.Compounds11–13exhibit a satisfactory inhibition of mycobacteri

ISSN:0365-6233    

DOI:10.1002/ardp.19973300603

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractThe interaction of organometallic compounds with biological systems, generally called bioorganometallic chemistry, is receiving increasing interest. We present the first part of our studies concerning the biological activity of organometallic compounds. Several alkyne‐cobalt carbonyl complexes inhibited the growth of human melanoma and lung carcinoma cell lines. They are more active than uncomplexed dicobalt octacarbonyl, cobalt chloride, or the free ligand. A significant difference in potency towards the lung carcinoma cell line was observed among the cobalt complexes, indicating that the complexed ligand may influence cytotoxic activity. These results suggest that further exploratory work with such cobalt‐alkyne complexes is warran

ISSN:0365-6233    

DOI:10.1002/ardp.19973300604

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractThe α1‐adrenergic and 5‐HT1Aserotonergic receptor affinities of a series of 1‐arylpiperazines are presented. The role of the spacer and the influence of the terminal substituents on the α1‐adrenoreceptor affinity and the 5‐HT1A/α1 receptor selectivity a

ISSN:0365-6233    

DOI:10.1002/ardp.19973300605

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractIn the present study we synthesized aza‐analogs of 8‐styrylxanthines, in which the ethenyl bridge is replaced by an imine, amide, or azo function, in order to investigate structure‐activity relationships of the 8‐substituent of A2A‐selective xanthine derivatives. Thus, various 8‐substituents were combined with theophylline or caffeine, respectively, and affinities of the novel compounds for adenosine A1‐ and A2A‐receptors were determined and compared with those of analogous 8‐styrylxanthine derivatives. 8‐(Benzylideneamino)caffeine derivatives exhibited high affinity and selectivity for A2A‐adenosine receptors, but were unstable in aqueous buffer solution at physiological pH values. 8‐(Phenylazo)caffeine derivatives were less potent than corresponding 8‐styrylcaffeine derivatives at adenosine receptors. The most potent azo compound of the present series was 8‐(m‐chlorophenylazo)caffeine (14b) exhibiting a Kivalue of 400 nM at A2A‐adenosine receptors and 20‐fold selectivity versus A1‐receptors. Due to the facile synthetic access to 8‐(phenylazo)xanthine derivatives, which are obtained by coupling of 8‐unsubstituted xanthines with phenyldiazonium salts,14bmay be an interesting new lead compound for the development of more potent and selec

ISSN:0365-6233    

DOI:10.1002/ardp.19973300606

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

Abstract(+)−Vincamine (1) and (+)−vinpocetine (2) were chlorosulfonylated and the resulting sulfonyl chloride isomers (3–6) were transformed into sulfonamides (7–10). The ester group of sulfonamides was modified by selective hydrolysis and transesterification. Apovincaminol derivatives (14–16) were also prepared by reduction. In addition to the known cerebrovascular effects of the unsubstituted compounds (1,2), sulfonamides also show a significant peripheral vasodilat

ISSN:0365-6233    

DOI:10.1002/ardp.19973300607

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19973300601

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY