ISSN:0365-6233    

DOI:10.1002/ardp.19973300702

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractThe synthesis of 3‐substituted 2‐phenyl‐2,3‐dihydro‐4H‐1,3,2‐benzoxazaphosphorin‐4‐one 2‐sulfide derivatives is described. The action of a series 2‐oxide (1–6) and 2‐sulfide (7–12) derivatives on the central nervous system has been evaluated. Compounds1–4, 6, 7–10exhibit neuroleptic activity. Derivatives of sulfide series

ISSN:0365-6233    

DOI:10.1002/ardp.19973300703

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractStarting from amino(di)azines and 2‐chloro‐6‐methyliso(thio)cyanate a series of aryl‐substituted urea and thiourea derivatives was prepared and screened as potential antiepileptics. Among the new derivatives tested, only2band3cexhibited adequate anticonvulsant effects, whereas3dand4dwere found to be convulsant

ISSN:0365-6233    

DOI:10.1002/ardp.19973300704

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractThe key step in the synthesis of the pharmacologically interesting 1‐phenyltetrahydro‐3‐benzazepine skeleton is the Michael addition of (2‐lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals5a,bwithn‐butyllithium, to β‐nitrostyrene (6). The reductive ring closure of the nitro acetals7a,bsucceeded with zinc dust and hydrochloric acid to give the 3‐benzazepines11a,bin good yields. The unsubstituted 3‐benzazepine11ashowed a considerable affinity for the phencyclidine binding site of the NMDA receptor (Ki= 6.41 μM), whereas donor substituents in the aryl moiety (11b,c) reduce the affinity for

ISSN:0365-6233    

DOI:10.1002/ardp.19973300705

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractA range of 18 derivatives of flavone‐8‐acetic acid (FAA) with substituents on the 2‐phenyl group have been prepared and their anti‐tumour activity evaluatedin vitroagainst a panel of human and murine tumour cell lines andin vivoagainst MAC 15A. There was no clear‐cut relationship betweenin vitroandin vivoactivity but the activity in each situation was found to be very sensitive to the precise substitution pattern with closely related isomers giving widely different activities. Some of the compounds, notably10b,cj, andr, were activein vivoand these require further studies in order to evaluate their potential for de

ISSN:0365-6233    

DOI:10.1002/ardp.19973300706

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractA series of the derivatives of 1‐[2‐hydroxy‐3‐(4‐phenyl‐1‐piperazinyl)propyl]‐pyrrolidin‐2‐one (MG‐1) was synthesized and tested for electrocardiographic, antiarrhythmic, and antihypertensive activity as well as for α1‐ and α2‐ adrenoceptors binding affinities. Some of the compounds of this series slightly decreased the heart rate, prolonged P‐Q, Q‐T intervals and QRS complex. Only compound7(1‐[2‐hydroxy‐3‐(4‐phenyl‐1‐piperazinyl)propyl]‐pyrrolidine) possesses potent antiarrhythmic and a slight hypotensive properties, and affinity for α1‐ and α2‐ adrenoceptor. The results suggest that the antiarrhythmic and hypotensive effect of compound7andMG‐1is related to their adrenolytic properties, and that those propert

ISSN:0365-6233    

DOI:10.1002/ardp.19973300707

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

摘要:

AbstractA topological modification of ipriflavone1, a recent antiosteoporotic drug, is described. The flavone moiety of1has been replaced by a xanthone one. Among the new derivatives, the 3,6‐diisopropoxyxanthone (2a) has shown significant bone resorption inhibition inin vitroandin vivotest

ISSN:0365-6233    

DOI:10.1002/ardp.19973300708

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19973300701

出版商:WILEY‐VCH Verlag    

年代:1997

数据来源: WILEY