A. Almerico, G. Cirrincione, E. Aiello, G. Dattolo
{"title":"3-diazopyrroles: key intermediates in the synthesis of antineoplastic agents.","authors":"A. Almerico, G. Cirrincione, E. Aiello, G. Dattolo","doi":"10.1002/CHIN.198929326","DOIUrl":"https://doi.org/10.1002/CHIN.198929326","url":null,"abstract":"","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82895980","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}
{"title":"3-diazopyrroles: key intermediates in the synthesis of antineoplastic agents.","authors":"A M Almerico, G Cirrincione, E Aiello, G Dattolo","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14374677","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}
{"title":"The chemistry of trazodone.","authors":"L Baiocchi","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14206638","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}
F Bondavalli, O Bruno, A Ranise, P Schenone, S Russo, A Loffreda, V De Novellis, C Lo Sasso, E Marmo
The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.
{"title":"3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities.","authors":"F Bondavalli, O Bruno, A Ranise, P Schenone, S Russo, A Loffreda, V De Novellis, C Lo Sasso, E Marmo","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14376784","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}
A Cometti, G G Gallo, J Kettenring, G B Panzone, G Tuan, L F Zerilli
Teicoplanin is a complex formed by five closely related glycopeptides and by a small amount of a hydrolysis product. Minor quantities of related substances are also present. Two of them (named RS-1 and RS-2) were isolated and purified starting from the tailing fractions of a teicoplanin batch. Preparative reversed-phase liquid chromatography on large low-pressure and medium high-pressure scales, concentration, desalting, and freeze-drying steps were applied. 300 mg of RS-1 and 900 mg of RS-2 were obtained in a purity grade (about 90%) sufficient for structural investigation. Starting from considerations on the HPLC retentivity and on biosynthesis, the structures were assigned on the basis of 1H-N.M.R. spectra and homonuclear CO-SY 2D experiments, FAB-MS spectrometry, and GC-MS of the esters of the fatty acids obtained by hydrolysis. RS-1 and RS-2 are teicoplanins having 10-methyl-undecanoic acid and n-dodecanoic acid, respectively as fatty acid chains. No major difference in the in vitro activity of these teicoplanins emerged in comparison with teicoplanin complex.
{"title":"Isolation and structure determination of the main related substances of teicoplanin, a glycopeptide antibiotic.","authors":"A Cometti, G G Gallo, J Kettenring, G B Panzone, G Tuan, L F Zerilli","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Teicoplanin is a complex formed by five closely related glycopeptides and by a small amount of a hydrolysis product. Minor quantities of related substances are also present. Two of them (named RS-1 and RS-2) were isolated and purified starting from the tailing fractions of a teicoplanin batch. Preparative reversed-phase liquid chromatography on large low-pressure and medium high-pressure scales, concentration, desalting, and freeze-drying steps were applied. 300 mg of RS-1 and 900 mg of RS-2 were obtained in a purity grade (about 90%) sufficient for structural investigation. Starting from considerations on the HPLC retentivity and on biosynthesis, the structures were assigned on the basis of 1H-N.M.R. spectra and homonuclear CO-SY 2D experiments, FAB-MS spectrometry, and GC-MS of the esters of the fatty acids obtained by hydrolysis. RS-1 and RS-2 are teicoplanins having 10-methyl-undecanoic acid and n-dodecanoic acid, respectively as fatty acid chains. No major difference in the in vitro activity of these teicoplanins emerged in comparison with teicoplanin complex.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14113479","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}
{"title":"Penems: conception and evolution of a new class of beta-lactam antibiotics.","authors":"E Perrone","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14206640","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}
The results herein described point out that the efforts devoted to the preparation of significant molecules can not be separated from those devoted to the discovery of new synthetic methodologies and to the solution of fundamental chemical problems. The border between basic and applied research vanishes very frequently.
{"title":"How medicinal chemistry triggers fundamental research in heterocyclic chemistry. The chemistry of 4-hydroxy-2-pyrones and a new imidazole antifungal agent.","authors":"M. Moreno‐Mañas","doi":"10.1002/CHIN.198929334","DOIUrl":"https://doi.org/10.1002/CHIN.198929334","url":null,"abstract":"The results herein described point out that the efforts devoted to the preparation of significant molecules can not be separated from those devoted to the discovery of new synthetic methodologies and to the solution of fundamental chemical problems. The border between basic and applied research vanishes very frequently.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79882480","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}
C Rubat, P Coudert, J Couquelet, P Bastide, J Bastide
By addition of methylisocyanate to 5-arylidene 2-aminoalkyl 3-pyridazinones a series of derivatives substituted in the 2-position by an ureidoalkyl moiety was obtained in good yields. Gastric antisecretory and anti-ulcer activities of these new compounds were evaluated. The influence of the substituents attached to the pyridazine ring was discussed.
{"title":"[Synthesis, antisecretory, and anti-ulcer activity of new 5-arylidene-2-ureidoalkyl-3-pyridazinones].","authors":"C Rubat, P Coudert, J Couquelet, P Bastide, J Bastide","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>By addition of methylisocyanate to 5-arylidene 2-aminoalkyl 3-pyridazinones a series of derivatives substituted in the 2-position by an ureidoalkyl moiety was obtained in good yields. Gastric antisecretory and anti-ulcer activities of these new compounds were evaluated. The influence of the substituents attached to the pyridazine ring was discussed.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14376785","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}
J L Delarbre, L Maury, J Rambaud, B Pauvert, M S de Buochberg
Cefadroxil and cefalexine were characterized by thermal and spectral analysis. A vibrational study by infrared and Raman spectroscopies was made to connect the structural data with the antibacterial activity.
{"title":"[Spectral and thermal characterization of cephalosporins. I. Cefadroxil and cefalexin].","authors":"J L Delarbre, L Maury, J Rambaud, B Pauvert, M S de Buochberg","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Cefadroxil and cefalexine were characterized by thermal and spectral analysis. A vibrational study by infrared and Raman spectroscopies was made to connect the structural data with the antibacterial activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14376787","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}
{"title":"Penems: conception and evolution of a new class of beta-lactam antibiotics.","authors":"E. Perrone","doi":"10.1002/CHIN.198929328","DOIUrl":"https://doi.org/10.1002/CHIN.198929328","url":null,"abstract":"","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1988-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78254328","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}
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