Il Farmaco; edizione scientifica最新文献

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[Synthesis and antiparasitic activity of arylproprenones in the nitro-5-imidazole series]. [硝基-5-咪唑系列芳基丙烯酮的合成及抗寄生活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
L Ouattara, M Debaert, R Cavier
{"title":"[Synthesis and antiparasitic activity of arylproprenones in the nitro-5-imidazole series].","authors":"L Ouattara,&nbsp;M Debaert,&nbsp;R Cavier","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of new arylpropenones derived from 1-methyl-5-nitro imidazole is described. The investigation of some antiprotozoal properties has shown that compounds with the groups 4-hydroxyphenyl, 4-chlorophenyl or thiophenyl have trichomonacidal activity similar to that of metronidazole.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"389-93"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14039625","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
[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole. Analgesic activity and effect on conditioned avoidance response]. [2-(4'R')苄基- 5r -苯并咪唑的制备及其药理活性。]镇痛活性及其对条件回避反应的影响[j]。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
G Paglietti, M A Pirisi, M Loriga, G E Grella, F Sparatore, M Satta, P Manca, A Peana
{"title":"[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole. Analgesic activity and effect on conditioned avoidance response].","authors":"G Paglietti,&nbsp;M A Pirisi,&nbsp;M Loriga,&nbsp;G E Grella,&nbsp;F Sparatore,&nbsp;M Satta,&nbsp;P Manca,&nbsp;A Peana","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Several derivatives of 2-benzylbenzimidazole (dibazole) bearing substituents on positions 5 and 4' were prepared and tested, together with dibazole, for their activity on the acquisition of a conditioned avoidance response and for analgesic activity. Chlorpromazine and acetylsalicylic acid were used as standards. Analgesic activity was found for all these compounds, most of which proved more active than A.S.A. As regards the acquisition of a C.A.R., the 5-chloroderivatives exhibit a strong inhibitory activity, that for compound (VIII) is equal to that of chloropromazine, while dibazole and the 5-trifluormethylderivatives stimulate the acquisition.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"203-14"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14542544","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
[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole and 2-(4'-pyridinyl)-5R-benzimidazoles. Analgesic activity and effect on conditioned avoidance response]. [2-(4' r ')苄基- 5r -苯并咪唑和2-(4'-吡啶基)- 5r -苯并咪唑的制备及药理活性。]镇痛活性及其对条件回避反应的影响[j]。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
G Paglietti, M A Pirisi, M Loriga, G E Grella, F Sparatore, M Satta, P Manca
{"title":"[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole and 2-(4'-pyridinyl)-5R-benzimidazoles. Analgesic activity and effect on conditioned avoidance response].","authors":"G Paglietti,&nbsp;M A Pirisi,&nbsp;M Loriga,&nbsp;G E Grella,&nbsp;F Sparatore,&nbsp;M Satta,&nbsp;P Manca","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Sixteen 2-(4'R')phenyl-5R-benzimidazoles and two 2-(4'-pyridinyl)-5R-benzimidazoles were prepared and tested, together with 2-phenylbenzimidazole, for their activity on the acquisition of a conditioned avoidance response in rats and for analgesic activity in mice, and compared with chlorpromazine and acetylsalicylic acid. Several compounds inhibit strongly the acquisition of a C.A.R., with 2-(4'-alkoxy)phenylbenzimidazoles (XVI) and (XVII) clearly exceeding chlorpromazine. Analgesic activity is also generally present in the examined compounds; those bearing in the position 5 a trifluoromethyl or an acetyl group exhibit an activity higher than that of acetylsalicylic acid. Deconditioning and analgesic activities are not correlated with each other.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"215-26"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14541018","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
Electroencephalographic and autonomic effects of centrally administered neurotensin in the rabbit. 中枢给药神经紧张素对家兔的脑电图和自主神经的影响。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
E Marchioni, M Maurelli, A Tartara
{"title":"Electroencephalographic and autonomic effects of centrally administered neurotensin in the rabbit.","authors":"E Marchioni,&nbsp;M Maurelli,&nbsp;A Tartara","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Neurotensin perfusion into the third ventricle of the unanesthetized rabbit induces an increase of the total power density spectrum of the cortex, without modifying the electrical activity of the cornu Ammonis dorsale. This evidence suggests a direct action of the peptide on the cortical neurons and seems to exclude the involvement of the brainstem reticular formation in inducing the electroencephalographic pattern. Simultaneously Neurotensin produces an evident behavioural excitation and a moderate thermolytic effect. The electroneurophysiologic, autonomic and behavioural changes are independent from one another and seem to depend on an action exerted by Neurotensin at various levels in the CNS.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"267-76"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14541025","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 antitumor activity of aminoacid derivatives of the antimetastatic agent DM-COOK. 抗转移剂DM-COOK氨基酸衍生物的合成及抗肿瘤活性研究。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
L Lassiani, M M de Nardo, C Nisi, A Varnavas
{"title":"Synthesis and antitumor activity of aminoacid derivatives of the antimetastatic agent DM-COOK.","authors":"L Lassiani,&nbsp;M M de Nardo,&nbsp;C Nisi,&nbsp;A Varnavas","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Esters and amides of N-(3,3-dimethyl-1-triazeno)benzoylamino acids have been synthesized as inhibitors of cell surface neutral proteases. Preliminary data on activity against P-388 lymphocytic leukemia are also reported.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"227-38"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14541020","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
Different effect of glucagon on gastric acid secretion in vivo and in vitro. 胰高血糖素对体内、体外胃酸分泌的不同影响。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
G Coruzzi, M T Noci, G Bertaccini, E Corsanini
{"title":"Different effect of glucagon on gastric acid secretion in vivo and in vitro.","authors":"G Coruzzi,&nbsp;M T Noci,&nbsp;G Bertaccini,&nbsp;E Corsanini","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effect of glucagon on gastric acid secretion was evaluated in conscious cats with gastric fistula and in the isolated gastric fundus from immature rats. Glucagon (10-25 micrograms/kg/h) caused a slight inhibitory effect on pentagastrin-induced acid secretion; in contrast it was ineffective against dimaprit. At these doses glucagon induced a marked increase in glucose plasma levels. In the isolated rat gastric fundus glucagon (10(-7) M-3 x 10(-6) M) induced a concentration-dependent increase in acid output, being approximately 100 times as potent as histamine. Conversely from histamine, glucagon was not affected by pretreatment with phosphodiesterase inhibitors, thus an involvement of cAMP seems to be unlikely.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"293-300"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14541026","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
Studies on isoquinoline derivatives. IV. Synthesis and evaluation of the antimicrobial and antifungal activities of N2-arylidene-substituted 3-carbazoyl-isoquinolines. 异喹啉衍生物的研究。四、n2 -芳基取代3-咔唑基异喹啉类化合物的合成及抑菌活性评价。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
F Vittorio, M S Pappalardo, G Ronsisvalle, G Blandino
{"title":"Studies on isoquinoline derivatives. IV. Synthesis and evaluation of the antimicrobial and antifungal activities of N2-arylidene-substituted 3-carbazoyl-isoquinolines.","authors":"F Vittorio,&nbsp;M S Pappalardo,&nbsp;G Ronsisvalle,&nbsp;G Blandino","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>2,4-Dimethyl-1-oxo-1,2-dihydro-3-carbazoyl-isoquinoline (II), 1-chloro-, 1-methoxy-3-carbazoyl-4-methylisoquinoline (VI, X) and a series of their hydrazonic derivatives have been synthesized and tested in vitro for antibacterial and antifungal activities. 1-(1-Chloro-4-methyl-3-isoquinolinoyl)-2-(5-nitro-2-furfurylide ne) hydrazine (VII h) proved to be the most effective in the series (MIC 0.78 micrograms/ml) and was more potent than furazolidone against several strains of S.aureus; the same compound also showed a moderate antifungal activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"239-50"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14541022","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
[The anti-H1-histaminic and antimuscarinic effect of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds]. [2-和4-[苄基-(2-二甲氨基乙基)氨基]嘧啶化合物的抗h1组胺和抗毒蕈碱作用]。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
C Maggiali, G Morini, F Mossini, G Morini, E Barocelli, M Impicciatore
{"title":"[The anti-H1-histaminic and antimuscarinic effect of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds].","authors":"C Maggiali,&nbsp;G Morini,&nbsp;F Mossini,&nbsp;G Morini,&nbsp;E Barocelli,&nbsp;M Impicciatore","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>This paper reports the synthesis of 2- and 4- [benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and the evaluation of their inhibitory properties against histamine (H1), acetylcholine and barium chloride, on guinea pig isolated ileum. 4-[p.Methoxybenzyl-(2-dimethylaminoethyl)amino]-2-methoxy-pyrimidine (VIII) is shown to possess H1 receptor antagonist activity, with a potency similar to that observed for Tonzylamine. By contrast, a specific, although weak, antimuscarinic effect is displayed by 4-[benzyl-(2-dimethylaminoethyl)amino]-2-methoxy-5-methylthio-pyrimidine (XII).</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"277-91"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14038195","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
[Nonsteroidal anti-inflammatory agents. V. Synthesis of 1-aryl-5-(1-pyrryl)-pyrazolyl-4-acetic acids with potential anti-inflammatory action]. 非甾体类抗炎药。5 .具有潜在抗炎作用的1-芳基-5-(1-吡啶基)-吡唑基-4-乙酸的合成。
Il Farmaco; edizione scientifica Pub Date : 1988-03-01
F Corelli, S Massa, G Stefancich, R Silvestri, M Artico, G C Pantaleoni, G Palumbo, D Fanini, R Giorgi
{"title":"[Nonsteroidal anti-inflammatory agents. V. Synthesis of 1-aryl-5-(1-pyrryl)-pyrazolyl-4-acetic acids with potential anti-inflammatory action].","authors":"F Corelli,&nbsp;S Massa,&nbsp;G Stefancich,&nbsp;R Silvestri,&nbsp;M Artico,&nbsp;G C Pantaleoni,&nbsp;G Palumbo,&nbsp;D Fanini,&nbsp;R Giorgi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of 1-aryl-5-(1-pyrryl)pyrazoles bearing at position 4 an acetic or alpha-propionic chain is described. The new compounds can be structurally related to lonazolac and its analogues with analgesic-antiinflammatory activities. When tested pharmacologically in comparison with tolmetin and indomethacin none of the above derivatives showed any appreciable activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 3","pages":"251-65"},"PeriodicalIF":0.0,"publicationDate":"1988-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14541024","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
Central extra-endocrine effects of vasopressin and oxytocin in the rabbit. 加压素和催产素对家兔中枢外内分泌的影响。
Il Farmaco; edizione scientifica Pub Date : 1988-02-01
M Maurelli, E Marchioni, A Tartara
{"title":"Central extra-endocrine effects of vasopressin and oxytocin in the rabbit.","authors":"M Maurelli,&nbsp;E Marchioni,&nbsp;A Tartara","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effect of vasopressin and oxytocin on cerebral electrical activity, somatic behavior, heart rate and rectal temperature of non-anesthetized rabbits was studied. Both peptides induced EEG and behavioral activation and proved to be active in modifying heart rate and rectal temperature. EEG and behavioral changes, as well as autonomic effects seemed to be independent of one another, thus suggesting different points of attack of the peptides at CNS level.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 2","pages":"161-8"},"PeriodicalIF":0.0,"publicationDate":"1988-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14517776","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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