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Acetic acids bearing the 1-phenyl-1H-indazole nucleus with analgesic and antiinflammatory activity. 具有镇痛和抗炎活性的1-苯基- 1h -吲哚唑核的醋酸。
Il Farmaco; edizione scientifica Pub Date : 1988-10-01
L Mosti, G Menozzi, P Schenone, L Molinario, F Conte, C Montanario, E Marmoe
{"title":"Acetic acids bearing the 1-phenyl-1H-indazole nucleus with analgesic and antiinflammatory activity.","authors":"L Mosti,&nbsp;G Menozzi,&nbsp;P Schenone,&nbsp;L Molinario,&nbsp;F Conte,&nbsp;C Montanario,&nbsp;E Marmoe","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of [(1-phenyl-1H-indazol-4-yl)oxy]acetic acid (IV), (1-phenyl-1H-indazol-4-yl)acetic acid (IX) and (1,5,6,7)tetrahydro-1-phenyl-4H-indazol-4-iminooxy)acetic acid (XIII) starting from 1,5,6,7-tetrahydro-1-phenyl-4H-indazol-4-one (I) is described. These compounds showed a good antiinflammatory activity in rats, and an analgesic activity in mice similar or comparable to that of indomethacin.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 10","pages":"763-74"},"PeriodicalIF":0.0,"publicationDate":"1988-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14395185","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 pharmacologic activity of 3-quinolizidine-1'-yl-5-R-indoles]. [3-喹啉吡啶-1′-酰基-5- r -吲哚的合成及药理活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-10-01
C Boido-Canu, V Boido, F Sparatore, A Sparatore
{"title":"[Synthesis and pharmacologic activity of 3-quinolizidine-1'-yl-5-R-indoles].","authors":"C Boido-Canu,&nbsp;V Boido,&nbsp;F Sparatore,&nbsp;A Sparatore","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>By acid action on the mixture of homolupinal diethylacetal and arylhydrazines several 3-quinolizidin-1'-yl-5-R-indoles (III a - III e) were prepared. The homolupinal diethylacetal, whose hydrolysis gives rise to the unknown aldehyde, was obtained through the action of lupinylmagnesium chloride on diethylphenylorthoformate. Compounds (III) were subjected to wide pharmacological screening; all of them exhibited calcium blocking, negative cardioinotropic and diuretic activities, while single compounds showed antiinflammatory (III d), anticonvulsant and hypoglycemic (III e) activities.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 10","pages":"801-17"},"PeriodicalIF":0.0,"publicationDate":"1988-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14370557","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
Compounds with potential antitumor activity. VI--2-Alkyl-3-[2-(1,3,4-thiadiazolyl)]-4-thiazolidinones. 具有潜在抗肿瘤活性的化合物。六世——2-Alkyl-3 - [2 - (1,3, 4-thiadiazolyl)] 4-thiazolidinones。
Il Farmaco; edizione scientifica Pub Date : 1988-10-01
S Grasso, A Chimirri, P Monforte, G Fenech, M Zappalà, A M Monforte
{"title":"Compounds with potential antitumor activity. VI--2-Alkyl-3-[2-(1,3,4-thiadiazolyl)]-4-thiazolidinones.","authors":"S Grasso,&nbsp;A Chimirri,&nbsp;P Monforte,&nbsp;G Fenech,&nbsp;M Zappalà,&nbsp;A M Monforte","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The antitumor activity of a series of 2-alkyl-3-[2-(1,3,4-thiadiazolyl)]-4-thiazolidinones was tested against the leukemic P 388 tumor system in mice. Only compounds (V-VII) showed significant activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 10","pages":"851-6"},"PeriodicalIF":0.0,"publicationDate":"1988-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14370558","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
[Derivatives of phenoxyacetamide and antimycotic activity]. [苯氧乙酰胺衍生物及抗真菌活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01
G Daidone, D Raffa, M L Bajardi, S Plescia, M Milici
{"title":"[Derivatives of phenoxyacetamide and antimycotic activity].","authors":"G Daidone,&nbsp;D Raffa,&nbsp;M L Bajardi,&nbsp;S Plescia,&nbsp;M Milici","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Novel N-(3-methyl-4-R-isoxazol-5-yl)-2-R1-4-R2-phenoxyacetamides and N-(3-methyl-4-R-isoxazol-5-yl)-2-(2-R1-4-R2-phenoxyacetamido) benzamides were prepared and tested against Candida albicans and Cryptococcus neoformans. The results of the antimicrobial assay showed that the presence of two amidic groups usually enhances antimycotic activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 9","pages":"753-61"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14200592","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
Researches on antibacterial and antifungal agents. IX--Pyrrole analogues of bifonazole with potent antifungal activities. 抗菌和抗真菌药物的研究。联苯唑的吡咯类似物具有有效的抗真菌活性。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01
S Massa, G Stefancich, F Corelli, R Silvestri, S Panico, M Artico, N Simonetti
{"title":"Researches on antibacterial and antifungal agents. IX--Pyrrole analogues of bifonazole with potent antifungal activities.","authors":"S Massa,&nbsp;G Stefancich,&nbsp;F Corelli,&nbsp;R Silvestri,&nbsp;S Panico,&nbsp;M Artico,&nbsp;N Simonetti","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis and antifungal activities of pyrrole analogues of bifonazole are reported. Reduction of 4-nitrobenzophenone to the corresponding alcohol, reaction with phosphorus tribromide of the latter compound and condensation of the bromonitroderivative with imidazole led to 1-[alpha-(4-nitrophenyl)-4'-benzyl]-1H-imidazole. Hydrogenation of the nitro group to amino and reaction with 2,5-dimethoxytetrahydrofuran according to the Clauson-Kaas procedure afforded the pyrrole analogue of bifonazole. This compound and the related chloroderivative were also prepared by a similar pathway starting from 4-(1H-pyrrol-1-yl)benzophenone and its 4'-chloroderivative. Microbiological screening against Candida albicans and Candida spp showed 1-(alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)-1H-imidazole to be the most active compound among the tested derivatives.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 9","pages":"693-704"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14359855","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
3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities. 3, 5-Diphenyl-1H-pyrazole衍生品。1-(2-羟乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物的酯类和n -取代氨基甲酸酯类，具有抑制、抗心律失常、镇痛等活性。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01 DOI: 10.1002/CHIN.198912181
F. Bondavalli, O. Bruno, A. Ranise, P. Schenone, P. Addonizio, V. de Novellis, A. Loffreda, E. Marmo
{"title":"3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.","authors":"F. Bondavalli, O. Bruno, A. Ranise, P. Schenone, P. Addonizio, V. de Novellis, A. Loffreda, E. Marmo","doi":"10.1002/CHIN.198912181","DOIUrl":"https://doi.org/10.1002/CHIN.198912181","url":null,"abstract":"The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"81 1","pages":"725-43"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80503453","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
Potential CNS active agents. II--Studies of 4(3H)-quinazolinones. 潜在的中枢神经系统活性剂。4(3H)-喹唑啉酮的研究。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01
R Lakhan, R L Singh
{"title":"Potential CNS active agents. II--Studies of 4(3H)-quinazolinones.","authors":"R Lakhan,&nbsp;R L Singh","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Some new 2-carbamoylmethylthio- and 2-(omega-dimethylamino-alkyl)thio-3-aryl-7-chloro-4(3H)-quinazolinones have been prepared from 2-thio-3-aryl-7-chloro-4(3H)-quinazolinones as the key intermediate. Five of the synthetic compounds were screened for their CNS activities on mice and found to be either CNS depressants or stimulants.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 9","pages":"745-51"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14359857","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
Potential CNS active agents. II--Studies of 4(3H)-quinazolinones. 潜在的中枢神经系统活性剂。4(3H)-喹唑啉酮的研究。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01 DOI: 10.1002/CHIN.198912209
R. Lakhan, R. L. Singh
{"title":"Potential CNS active agents. II--Studies of 4(3H)-quinazolinones.","authors":"R. Lakhan, R. L. Singh","doi":"10.1002/CHIN.198912209","DOIUrl":"https://doi.org/10.1002/CHIN.198912209","url":null,"abstract":"Some new 2-carbamoylmethylthio- and 2-(omega-dimethylamino-alkyl)thio-3-aryl-7-chloro-4(3H)-quinazolinones have been prepared from 2-thio-3-aryl-7-chloro-4(3H)-quinazolinones as the key intermediate. Five of the synthetic compounds were screened for their CNS activities on mice and found to be either CNS depressants or stimulants.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"20 1","pages":"745-51"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81514589","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
3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities. 3, 5-Diphenyl-1H-pyrazole衍生品。1-(2-羟乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物的酯类和n -取代氨基甲酸酯类，具有抑制、抗心律失常、镇痛等活性。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01
F Bondavalli, O Bruno, A Ranise, P Schenone, P Addonizio, V De Novellis, A Loffreda, E Marmo
{"title":"3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.","authors":"F Bondavalli,&nbsp;O Bruno,&nbsp;A Ranise,&nbsp;P Schenone,&nbsp;P Addonizio,&nbsp;V De Novellis,&nbsp;A Loffreda,&nbsp;E Marmo","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 9","pages":"725-43"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14359858","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
[A substance with antibacterial and antifungal activity. V. Synthesis and microbiological activity of new derivatives of 1,5-diarylpyrrole]. 具有抗菌和抗真菌活性的物质。5 . 1,5-二芳基吡咯新衍生物的合成及微生物活性研究。
Il Farmaco; edizione scientifica Pub Date : 1988-09-01
M Scalzo, G C Porretta, F Chimenti, A Bolasco, M C Casanova, N Simonetti, A Villa
{"title":"[A substance with antibacterial and antifungal activity. V. Synthesis and microbiological activity of new derivatives of 1,5-diarylpyrrole].","authors":"M Scalzo,&nbsp;G C Porretta,&nbsp;F Chimenti,&nbsp;A Bolasco,&nbsp;M C Casanova,&nbsp;N Simonetti,&nbsp;A Villa","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis and antifungal activities of new 1,5-diarylpyrrole derivatives are reported. The N-methylpiperazinyl substituent must be regarded as fundamental to activity. Furthermore the presence of substituents on the para position of the two phenyl rings and the presence of halogen atoms can be considered strengthening factors to microbiological activity. The results obtained are discussed on the basis of structure-activity relationship.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 9","pages":"677-91"},"PeriodicalIF":0.0,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14357103","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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