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Il Farmaco; edizione scientifica最新文献

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Synthesis, binding affinities for alpha-adrenoceptor and eudismic analysis of chiral benzodioxane derivatives and their chiral opened analogues. 手性苯并二氧杂环衍生物及其手性开放类似物的合成、与肾上腺素受体的结合亲和性及流行病学分析。
Il Farmaco; edizione scientifica Pub Date : 1988-12-01
V Ferri, M Pallavicini, D Piccini, E Valoti, L Villa, N Brunello, G Racagni
{"title":"Synthesis, binding affinities for alpha-adrenoceptor and eudismic analysis of chiral benzodioxane derivatives and their chiral opened analogues.","authors":"V Ferri, M Pallavicini, D Piccini, E Valoti, L Villa, N Brunello, G Racagni","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 12 Suppl","pages":"1153-63"},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13990646","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Prolyl derivatives of enalapril as potential angiotensin converting enzyme inhibitors. 依那普利脯氨酸衍生物作为潜在的血管紧张素转换酶抑制剂。
Il Farmaco; edizione scientifica Pub Date : 1988-12-01
R Ciabatti, G Tarzia, F Battaglia, D Barone, E Baldoli
{"title":"Prolyl derivatives of enalapril as potential angiotensin converting enzyme inhibitors.","authors":"R Ciabatti,&nbsp;G Tarzia,&nbsp;F Battaglia,&nbsp;D Barone,&nbsp;E Baldoli","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of a new class of potential angiotensin converting enzyme (ACE) inhibitors, analogs of enalapril, is reported. In these molecules the C-terminal amino acidic sequence Ala-Pro of enalapril was replaced by the sequence Pro-Pro. The compounds were tested both in vitro and in vivo. They showed no in vivo activity but only a week in vitro inhibitory activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 12","pages":"989-1003"},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13992420","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Amidinosemicarbazido derivatives of pyrazole: synthesis and inhibitory effect on blood coagulation and platelet aggregation. 吡唑氨基氨基脲基衍生物的合成及其对凝血和血小板聚集的抑制作用。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01 DOI: 10.1002/CHIN.198923166
R. Ferroni, L. Milani, D. Simoni, P. Orlandini, T. Poli, M. Guarneri, U. Taddeo
{"title":"Amidinosemicarbazido derivatives of pyrazole: synthesis and inhibitory effect on blood coagulation and platelet aggregation.","authors":"R. Ferroni, L. Milani, D. Simoni, P. Orlandini, T. Poli, M. Guarneri, U. Taddeo","doi":"10.1002/CHIN.198923166","DOIUrl":"https://doi.org/10.1002/CHIN.198923166","url":null,"abstract":"Amidinosemicarbazido derivatives of pyrazole having various substituents on pyrazole ring were prepared and their effect on platelet function and blood coagulation was determined in vitro. Platelet aggregation and serotonin release induced by ADP, collagen, arachidonic acid and thrombin were markedly inhibited by pyrazole derivatives at mM concentrations. Compounds with a hydrophobic nucleus at position 1 of the pyrazole ring showed the most potent antiplatelet activity. On the contrary, their effect on blood coagulation was faintly inhibitory.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"21 1","pages":"891-9"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81386337","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Amidinosemicarbazido derivatives of pyrazole: synthesis and inhibitory effect on blood coagulation and platelet aggregation. 吡唑氨基氨基脲基衍生物的合成及其对凝血和血小板聚集的抑制作用。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01
R Ferroni, L Milani, D Simoni, P Orlandini, T Poli, M Guarneri, U Taddeo
{"title":"Amidinosemicarbazido derivatives of pyrazole: synthesis and inhibitory effect on blood coagulation and platelet aggregation.","authors":"R Ferroni,&nbsp;L Milani,&nbsp;D Simoni,&nbsp;P Orlandini,&nbsp;T Poli,&nbsp;M Guarneri,&nbsp;U Taddeo","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Amidinosemicarbazido derivatives of pyrazole having various substituents on pyrazole ring were prepared and their effect on platelet function and blood coagulation was determined in vitro. Platelet aggregation and serotonin release induced by ADP, collagen, arachidonic acid and thrombin were markedly inhibited by pyrazole derivatives at mM concentrations. Compounds with a hydrophobic nucleus at position 1 of the pyrazole ring showed the most potent antiplatelet activity. On the contrary, their effect on blood coagulation was faintly inhibitory.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 11","pages":"891-9"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14381852","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Benzodiazepine receptor ligands. Synthesis and pharmacological evaluation of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines. 苯二氮卓类受体配体。6-芳基-3,8-二取代-1,2,4-三唑[3,4-a]酞嗪的合成及药理评价。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01 DOI: 10.1002/chin.198923193
G. Tarzia, E. Occelli, D. Barone
{"title":"Benzodiazepine receptor ligands. Synthesis and pharmacological evaluation of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines.","authors":"G. Tarzia, E. Occelli, D. Barone","doi":"10.1002/chin.198923193","DOIUrl":"https://doi.org/10.1002/chin.198923193","url":null,"abstract":"A series of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines was synthesised starting from suitable o-benzoylbenzoic acids. The compounds were tested in vitro for inhibition of the specific binding of 3H-Diazepam to benzodiazepine receptors in preparations of membranes from rat brain synaptosomes. None of the compounds was notably active in this test.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"35 1","pages":"921-33"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91188618","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Synthesis and anti-ulcer activity of some new compounds with arylthiomethyl-pyridine structure]. [一些芳基硫甲基吡啶结构新化合物的合成及其抗溃疡活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01 DOI: 10.1002/CHIN.198923176
S. Evangelista, M. Ghelardoni, A. Meli, V. Pestellini, G. Viti
{"title":"[Synthesis and anti-ulcer activity of some new compounds with arylthiomethyl-pyridine structure].","authors":"S. Evangelista, M. Ghelardoni, A. Meli, V. Pestellini, G. Viti","doi":"10.1002/CHIN.198923176","DOIUrl":"https://doi.org/10.1002/CHIN.198923176","url":null,"abstract":"We report the results of the antiulcer activity of some arylthiomethylpyridine compounds. Some of these showed gastroprotective activity against 96% ethanol-induced gastric lesions greater than Omeprazole. However they possess antiulcer properties lower than the reference compound against Indomethacin-induced gastric ulcers.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"26 1","pages":"901-8"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83289094","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Nonsteroidal antiinflammatory agents. XVIII - Stereomeric optically active halogenophenyl-biphenylyl-hydroxypropionic acids. 非甾体类抗炎药。立体旋光性卤代苯基-联苯基-羟基丙酸。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01
L Varoli, S Burnelli, A Guarnieri, N Ghedini, G Scapini, S Ferri, E Cavicchini
{"title":"Nonsteroidal antiinflammatory agents. XVIII - Stereomeric optically active halogenophenyl-biphenylyl-hydroxypropionic acids.","authors":"L Varoli,&nbsp;S Burnelli,&nbsp;A Guarnieri,&nbsp;N Ghedini,&nbsp;G Scapini,&nbsp;S Ferri,&nbsp;E Cavicchini","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The optically active stereomers of some 3-(fluoro-, chloro-, bromophenyl)-2-biphenylyl-3-hydroxypropionic acids were prepared and tested for antiinflammatory activity. Surprisingly, the four bromo-isomers were the most active ones, particularly in the threo configuration.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 11","pages":"909-19"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14381854","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
N,N-disubstituted 4-amino-(6-methoxy)-3-phenyl-2H-naphtho [1,2-b]pyran-2-ones with antiarrhythmic, platelet antiaggregating and local anesthetic activities. 具有抗心律失常、抗血小板聚集和局部麻醉活性的N,N-二取代4-氨基-(6-甲氧基)-3-苯基- 2h -萘[1,2-b]吡喃-2- 1。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01 DOI: 10.1002/chin.198923181
A. Bargagna, M. Longobardi, E. Mariani, P. Schenone, S. Russo, S. Vilagliano, V. de Novellis, E. Marmo
{"title":"N,N-disubstituted 4-amino-(6-methoxy)-3-phenyl-2H-naphtho [1,2-b]pyran-2-ones with antiarrhythmic, platelet antiaggregating and local anesthetic activities.","authors":"A. Bargagna, M. Longobardi, E. Mariani, P. Schenone, S. Russo, S. Vilagliano, V. de Novellis, E. Marmo","doi":"10.1002/chin.198923181","DOIUrl":"https://doi.org/10.1002/chin.198923181","url":null,"abstract":"The synthesis of title compounds (VI) by 1,4-cycloaddition of phenylchloroketene to N,N-disubstituted (E)-2-aminomethylene-3,4-dihydro-(6-methoxy)-1(2H)naphthalenones, followed by dehydrochlorination with DBN and dehydrogenation with Pd/C of the resulting cycloadducts, is described. Some compounds (VI) showed antiarrhythmic activity in rats higher or like that of quinidine and platelet antiaggregating activity in vitro like that of acetylsalycilic acid, as well as moderate infiltration anesthesia in mice and weak hypotensive, bradicardic and antiinflammatory activities in rats.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"319 1","pages":"857-77"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80196687","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Aminoethers of 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6-h ydroxy imine with antiarrhythmic activity. 具有抗心律失常活性的1,3,3-三甲基-5-(苯基亚甲基)-2-氧沙比环辛烷-6-h羟基亚胺的氨基醚。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01
E Mariani, A Bargagna, M Longobardi, P Schenone, S Russo, W Filippelli, L Molinario, E Marmo
{"title":"Aminoethers of 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6-h ydroxy imine with antiarrhythmic activity.","authors":"E Mariani,&nbsp;A Bargagna,&nbsp;M Longobardi,&nbsp;P Schenone,&nbsp;S Russo,&nbsp;W Filippelli,&nbsp;L Molinario,&nbsp;E Marmo","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of beta-dialkylaminoethyl ethers (III a-f) and gamma-dialkylaminopropyl ethers (III g-l) starting from 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6- hydroxyimine (II) is described. beta-Diisopropylaminoethyl ether (III b) and gamma-piperidinopropyl ether (III i) showed an antiarrhythmic activity in rats similar to that of quinidine. Moreover, a number of ethers (III) showed weak hypotensive and bradycardic activity in rats and moderate infiltration anesthesia in mice.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 11","pages":"879-86"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14381851","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[New heterocyclic derivatives of benzimidazole with germicidal activity. V. Synthesis and activity of new derivatives of di-2-benzimidazolyl-2,5-furan]. 新的具有杀菌活性的苯并咪唑杂环衍生物。二-2-苯并咪唑-2,5-呋喃新衍生物的合成及活性研究[j]。
Il Farmaco; edizione scientifica Pub Date : 1988-11-01
M Pedini, G Alunni Bistocchi, G De Meo, A Ricci, L Bastianini, T Sposini, P Jacquignon
{"title":"[New heterocyclic derivatives of benzimidazole with germicidal activity. V. Synthesis and activity of new derivatives of di-2-benzimidazolyl-2,5-furan].","authors":"M Pedini,&nbsp;G Alunni Bistocchi,&nbsp;G De Meo,&nbsp;A Ricci,&nbsp;L Bastianini,&nbsp;T Sposini,&nbsp;P Jacquignon","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In continuation of the research in the field of germicidal and antimycotic agents, the synthesis of 14 new derivatives of di-2-benzimidazolyl-2,5-furan is described. These derivatives are differently substituted (R not equal to R') in the position 5 of the two benzene rings. These new compounds showed no germicidal or fungicidal activity, when tested on different cultures. New compounds are under investigation.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 11","pages":"935-42"},"PeriodicalIF":0.0,"publicationDate":"1988-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14381855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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