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Some photochemical and photobiological properties of 8,8-desmethylxanthyletine (homopsoralen), a potential photochemotherapeutic agent. 8,8-去甲基黄叶碱(同补骨脂素)的光化学和光生物学性质。
Il Farmaco; edizione scientifica Pub Date : 1988-05-01
D Vedaldi, F Dall'Acqua, D Averbeck, E Cundari
{"title":"Some photochemical and photobiological properties of 8,8-desmethylxanthyletine (homopsoralen), a potential photochemotherapeutic agent.","authors":"D Vedaldi,&nbsp;F Dall'Acqua,&nbsp;D Averbeck,&nbsp;E Cundari","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In this paper the photochemical and photobiological properties of 8,8-desmethyl-xanthyletine (homopsoralen) have been studied. This drug forms a molecular complex with DNA undergoing intercalation between two base pairs of the macromolecule. By subsequent irradiation (365 nm) the compound photobinds covalently to the macromolecule showing an initial DNA-photobinding rate higher than that of 8-methoxypsoralen. In the photoreaction with DNA the drug effectively forms inter-strand cross-linkages. Its ability to generate singlet oxygen when irradiated with ultraviolet light is markedly higher than that of 8-MOP. Homopsoralen when irradiated in water solution undergoes effective photolysis. The drug shows a lower antiproliferative activity on diploid yeast (D 7) than 8-MOP and an almost parallel mutagenic activity. Also the gene convertogenic activity, determined on the same yeast strain, is lower than that of 8-MOP. Homopsoralen does not show any skin phototoxicity on guinea-pig skin. Taking into account its DNA-photobinding capacity, its antiproliferative activity, its reduced genotoxicity and lack of skin-phototoxicity homopsoralen may deserve further studies for evaluating its photochemotherapeutic activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 5","pages":"395-407"},"PeriodicalIF":0.0,"publicationDate":"1988-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14197370","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
Effects of antimuscarinic agents, H2-blockers and omeprazole on rat chronic gastric ulcer after long- and short-term administration. 抗毒蕈碱类药物、h2阻滞剂和奥美拉唑对大鼠慢性胃溃疡长期和短期治疗的影响。
Il Farmaco; edizione scientifica Pub Date : 1988-05-01
M Chiavarini, G Morini, E Barocelli, M Impicciatore, F Bordi
{"title":"Effects of antimuscarinic agents, H2-blockers and omeprazole on rat chronic gastric ulcer after long- and short-term administration.","authors":"M Chiavarini,&nbsp;G Morini,&nbsp;E Barocelli,&nbsp;M Impicciatore,&nbsp;F Bordi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Two series of experiments were performed on rat chronic ulcer in order to assess the possible curative and mucosal protective properties of 2 week treatments, or the preventive properties of 4 week treatments with antisecretory agents, acting with different mechanisms of action. At the end of the treatments the gastric secretory and motor responsiveness to a gastrin-like stimulus was simultaneously evaluated. The results support the view that antimuscarinic agents as well as H2-blockers cannot be defined as protective and that after a 4 week treatment they can induce modifications of gastric functions.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 5","pages":"479-87"},"PeriodicalIF":0.0,"publicationDate":"1988-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14042879","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 ring systems--V synthesis and pharmacological activity of 6H-1,3,4-thiadiazolo [3',2':1,2]-5-oxopyrimido [5,4-b] indole derivatives and of 1-phenyl-6H-1,2,4-triazolo [1',5':1,2]-5-oxopyrimido[5,4-b] indole. 新的杂环体系——6h -1,3,4-噻二唑[3′，2′:1,2]-5-氧嘧啶[5,4-b]吲哚衍生物和1-苯基- 6h -1,2,4-三唑[1′，5′:1,2]-5-氧嘧啶[5,4-b]吲哚的合成和药理活性。
Il Farmaco; edizione scientifica Pub Date : 1988-05-01
F Russo, S Guccione, N A Santagati, A Santagati, A Caruso, M G Leone, A Felice, G Attaguile, M Amico Roxas
{"title":"New heterocyclic ring systems--V synthesis and pharmacological activity of 6H-1,3,4-thiadiazolo [3',2':1,2]-5-oxopyrimido [5,4-b] indole derivatives and of 1-phenyl-6H-1,2,4-triazolo [1',5':1,2]-5-oxopyrimido[5,4-b] indole.","authors":"F Russo,&nbsp;S Guccione,&nbsp;N A Santagati,&nbsp;A Santagati,&nbsp;A Caruso,&nbsp;M G Leone,&nbsp;A Felice,&nbsp;G Attaguile,&nbsp;M Amico Roxas","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>As a part of a study on analgesic and antiinflammatory active condensed heterocyclic compounds containing the pyrimidinic ring, a number of 6H-1,3,4-thiadiazolo [3',2':1,2]-5-oxopyrimido [5,4-b]indole and 1-phenyl-6H-1,2,4-triazolo [1',5':1,2]-5-oxopyrimido [5,4-b] indole were synthesized and tested. The results of pharmacological assays are reported and discussed.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 5","pages":"409-20"},"PeriodicalIF":0.0,"publicationDate":"1988-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14394379","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 antifungal activity of new derivatives of 5-(4-halobenzoyl)-4-amino-3-(2-dialkylaminoethylthio)thieno [2,3-c] and [3,2-d] isothiazole]. [5-(4-卤代苯甲酰)-4-氨基-3-(2-二烷基氨基乙基硫)噻唑[2,3-c]和[3,2-d]异噻唑新衍生物的合成及抗真菌活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-05-01
G Romeo, E Bousquet, M S Pappalardo, G Ronsisvalle, S Oliveri, E Cammarata
{"title":"[Synthesis and antifungal activity of new derivatives of 5-(4-halobenzoyl)-4-amino-3-(2-dialkylaminoethylthio)thieno [2,3-c] and [3,2-d] isothiazole].","authors":"G Romeo,&nbsp;E Bousquet,&nbsp;M S Pappalardo,&nbsp;G Ronsisvalle,&nbsp;S Oliveri,&nbsp;E Cammarata","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A new series of 5-(4-halobenzoyl)-4-amino-3-(2-dialkylamino-ethylthio)thieno [2,3-c] and [3,2-d] isothiazole derivatives has been synthetized. The compounds were evaluated for antifungal activity on yeast and dermatophytes. The compound (VI b) resulted about thirty times less potent than miconazole on dermatophytes.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 5","pages":"457-67"},"PeriodicalIF":0.0,"publicationDate":"1988-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14351047","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 physicochemical properties of uracil derivatives with potential biological activity. 具有潜在生物活性的尿嘧啶衍生物的制备及其理化性质。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
P Pecorari, G Vampa, A Albasini, M Rinaldi, M Melegari, M P Costi
{"title":"Preparation and physicochemical properties of uracil derivatives with potential biological activity.","authors":"P Pecorari,&nbsp;G Vampa,&nbsp;A Albasini,&nbsp;M Rinaldi,&nbsp;M Melegari,&nbsp;M P Costi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The characterization of mono- and dimethylated 5-substituted uracils was re-examined. Analysis of their physicochemical properties (pKa, U.V., delta 1H-N.M.R.) affords insight into the structural characteristics of 5-substituted uracil alkylated at the ring nitrogens.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"311-8"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14332958","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
Experimental study on central effects of carboxyethyl-gamma-aminobutyric acid (CEGABA). 羧乙基- γ -氨基丁酸(CEGABA)中枢效应的实验研究。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
P Bo, C Camana, M Curti, F Fussi, A Giorgetti, F Savoldi
{"title":"Experimental study on central effects of carboxyethyl-gamma-aminobutyric acid (CEGABA).","authors":"P Bo,&nbsp;C Camana,&nbsp;M Curti,&nbsp;F Fussi,&nbsp;A Giorgetti,&nbsp;F Savoldi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The central effects of carboxyethyl-gamma-aminobutyric acid (CEGABA) have been studied both in rabbits and in the guinea pig myoclonus model. This drug caused EEG synchronization and behavioural sedation both after intravenous (i.v.) and intracerebroventricular (i.c.v.) administration in a dose-dependent manner, in rabbits. CEGABA showed a protective action against myoclonus induced by means of L-5-HTP in young guinea pigs. These data substantiate the hypothesis that CEGABA is a drug active on the central nervous system and probably exerts its action by strengthening cortical inhibition and/or directly acting on lower brainstem.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"363-72"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14391425","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
Khellin, a naturally occurring furochromone, used for the photochemotherapy of skin diseases: mechanism of action. 一种自然产生的荧光素，用于皮肤病的光化学疗法:作用机制。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
D Vedaldi, S Caffieri, F Dall'Acqua, L Andreassi, L Bovalini, P Martelli
{"title":"Khellin, a naturally occurring furochromone, used for the photochemotherapy of skin diseases: mechanism of action.","authors":"D Vedaldi,&nbsp;S Caffieri,&nbsp;F Dall'Acqua,&nbsp;L Andreassi,&nbsp;L Bovalini,&nbsp;P Martelli","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Khellin, a naturally occurring furochromone, used in the past as a coronary vasodilator, has recently been used in the photochemotherapeutic treatment of vitiligo and psoriasis. With the aim of elucidating its mechanism of action, the interactions both in ground and excited states between the drug and DNA were studied in vitro. Khellin forms in the dark a molecular complex with DNA. By subsequent irradiation (365 nm) the drug photoconjugates covalently with the macromolecule, although the rate of photobinding is rather low. The in vivo photobinding of khellin to the DNA of Ehrlich ascites tumor cells is also low. In photoaddition with the macromolecule the drug forms inter-strand cross-links, although again in small amounts. The furan side monoadduct between khellin and thymine, formed in the photoreaction between the drug and DNA, was isolated and characterized, and shows a cis-syn configuration.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"333-46"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14332959","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 antimicrobial activity of some pyrrole derivatives. II: 2-(2'-acylhydrazino)-3-ethoxycarbonyl-5-aryl (or alkyl)- pyrrole derivatives. 吡咯衍生物的合成及其抑菌活性研究。2-(2′-酰基肼)-3-乙氧羰基-5-芳基(或烷基)-吡咯衍生物。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
M T Cocco, C Congiu, A Maccioni, M L Schivo, G Palmieri
{"title":"Synthesis and antimicrobial activity of some pyrrole derivatives. II: 2-(2'-acylhydrazino)-3-ethoxycarbonyl-5-aryl (or alkyl)- pyrrole derivatives.","authors":"M T Cocco,&nbsp;C Congiu,&nbsp;A Maccioni,&nbsp;M L Schivo,&nbsp;G Palmieri","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of 2-(2'-acylhydrazino)-3-ethoxycarbonyl-3-aryl (or alkyl)-pyrrole derivatives was synthesized and submitted to in vitro microbiological screening. Most derivatives showed considerable antibacterial and antifungal activities.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"319-31"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14192724","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
Acute experimental allergic encephalitis. Treatment with fungal polysaccharides. 急性实验性过敏性脑炎。真菌多糖处理。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
M Ceroni, C Camana, D M Franciotta, F Savoldi, R Scelsi, M Fumagalli
{"title":"Acute experimental allergic encephalitis. Treatment with fungal polysaccharides.","authors":"M Ceroni,&nbsp;C Camana,&nbsp;D M Franciotta,&nbsp;F Savoldi,&nbsp;R Scelsi,&nbsp;M Fumagalli","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>This report describes the effects of a fungal polysaccharide mixture on the Experimental Allergic Encephalitis (EAE) in guinea pigs. The clinical, histopathological and IgG intrathecal synthesis related studies in the EAE sensitized group was compared with that observed in EAE sensitized groups treated with fungal polysaccharides. The results indicate that the fungal polysaccharide mixture is capable of inducing a more localized and milder inflammatory reaction in the guinea pig with EAE. We hypothesize that the fungal polysaccharides can activate complement by the alternative pathway, subtracting it to the specific immune response to EAE.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"381-7"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14332961","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
3,3'-Di[1,3-thiazolidine-4-one]system. IV. Synthesis and pharmacological properties of 3,3'(1,2-ethanediyl)bis [2-aryl-1,3-thiazolidine-4-one 1,1-dioxide] derivatives. 3, 3 ' di (1, 3-thiazolidine-4-one)系统。3,3'(1,2-乙二基)双[2-芳基-1,3-噻唑烷-4- 1,1-二氧基]衍生物的合成和药理学性质。
Il Farmaco; edizione scientifica Pub Date : 1988-04-01
M G Vigorita, T Previtera, M Basile, G Fenech, R Costa de Pasquale, F Occhiuto, C Circosta
{"title":"3,3'-Di[1,3-thiazolidine-4-one]system. IV. Synthesis and pharmacological properties of 3,3'(1,2-ethanediyl)bis [2-aryl-1,3-thiazolidine-4-one 1,1-dioxide] derivatives.","authors":"M G Vigorita,&nbsp;T Previtera,&nbsp;M Basile,&nbsp;G Fenech,&nbsp;R Costa de Pasquale,&nbsp;F Occhiuto,&nbsp;C Circosta","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The 1,1' disulfones obtained by oxidation of the corresponding dl and meso 3,3'(1,2-ethanediyl)bis [2-aryl-4-thiazolidinone] compounds previously investigated, were evaluated as anti-histamine, anti-inflammatory, analgesic and anti-pyretic agents. All 2,2' fluorophenyl compounds were found to be significantly active in inhibiting carrageenin-induced edema, whereas only para-substituted derivatives were active on the histamine-induced bronchospasm in the guinea-pig. They also showed analgesic effects that reached and sometimes exceeded those of indomethacin and phenylbutazone used as reference drugs.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 4","pages":"373-9"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14391426","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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