{"title":"Synthesis and antimicrobial properties of 3-sulfonyl-1,2,3,4-tetrahydropyrimido [4,5-d] pyrimidines.","authors":"Jerzy Cieplik, Janusz Pluta, Olaf Gubrynowicz","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The paper presents the synthesis of sulfonyl tetrahydropyrimido[4,5-d]pyrimidine derivatives as well as the antimicrobial activity of the obtained compounds. The investigations showed that the obtained sulfonyl derivatives of pyrimido[4,5-d]pyrimidines and especially the compounds with free amino group reveal interesting antibacterial and antifungal activity.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 9","pages":"321-8"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25099048","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":"Synthesis and anticonvulsant activity of some piperazine derivatives.","authors":"H Marona, R Korona, E Szneler","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Various 1,4-substituted derivatives of piperazine (I-XII) were synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (ScMet)--induced seizures and for neurotoxicity (TOX) in the rotorod test in mice and rats. The most promising compounds seem to be 1-[(2,4,6-trimethyl)-phenoxyethyl]-4-(2-hydroxyethyl)-piperazine dihydrochloride (II) and 1,4-bis-[(4-chloro-3-methyl)-phenoxyethyl]-piperazine dihydrochloride (X) which displayed anti-MES activity with their protective index (PI) higher than that for valproate II (rats), X(mice)).</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 9","pages":"329-35"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25099050","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}
U Mandal, Prashant Musmade, Mita Chakraborty, D Senthil Rajan, M Chakravarti, T K Pal, T K Chattaraj
{"title":"Bioequivalence study of sildenafil citrate tablets in healthy human volunteers.","authors":"U Mandal, Prashant Musmade, Mita Chakraborty, D Senthil Rajan, M Chakravarti, T K Pal, T K Chattaraj","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Newly developed sildenafil citrate (SC), a selective inhibitor of cyclic guanosine monophosphate (c-GMP) specific phosphodiesterase type 5 (PDE 5) in the corpus cavernosum is used for the oral treatment of erectile dysfunction. A convenient, sensitive and simple method for the determination of sildenafil in human plasma is presented. The analytical technique was based on reversed-phase high-performance liquid chromatography coupled with UV detector set at 295 nm. Rofecoxib was used as internal standard (I.S). Liquid-liquid extraction using diethyl ether was performed to recover sildenafil and rofecoxib. The retention time of I.S and sildenafil were 5.5 minutes and 7.2 minutes respectively. The method was validated over a linear range of 10 to 1000 ng/ml from plasma. Separate stability study showed that sildenafil is stable under conditions of analysis. The extraction efficiency from plasma varied from 79.69% to 81.13 %. The minimum quantifiable concentration was set at 10 ng/ml. (%o CV<12.5%). The method was used for Bioequivalence Study of Two Brands of Sildenafil citrate 50 mg tablets in healthy human volunteers. All pharmacokinetic parameter were calculated along with statistical evaluation.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 9","pages":"345-9"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25099569","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":"Synthesis and biological evaluation of novel naphthoquinone derivatives as potential anticancer and antimicrobial agents.","authors":"Nargues S Habib, Mona A Mahran","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Four novel series of 1,4-naphthoquinone derivatives namely 2,3-disubstiuted 4-[(benzothiazol-2-yl)hydrazono]-1,4-dihydronaphthalen-1-one 4a-c, N1-(2,3-disubstituted-4-oxo-1,4-dihydronaphthalen-1-ylidene)-N2-(benzotriazol-1-yl)acetic acid hydrazide 5a-c, 2,3-disubstituted 4-[(5-aryl-2,3-dihyrothiazol-2-ylidene)hydrazono]-1,4-dihydronaphthalen-1-one 7a-c, and 3-methyl-2-substituted carbamoyl or thiocarbamoyl-hydrazinocarbonylmethylthio-1,4-dihydronaphthalene-1,4-dione 9a-c were synthesized. Three of the new compounds were chosen by NCI to be evaluated as anticancer agents and they showed promising activity. All the prepared compounds were tested as antimicrobial agents.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 8","pages":"299-307"},"PeriodicalIF":0.0,"publicationDate":"2004-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25274627","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":"Effect of 5-substituted benzylideneaminosalicylic acid on carrageenan-induced ulcerative colitis.","authors":"P Jaysekhar, S B Rao, G Santhakumari","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Mesalazine, a drug of choice in the management of ulcerative colitis, was chemically modified as 5-(E)-substituted benzylideneaminosalicylic acid by condensing 5-aminosalicylic acid with selected aryl aldehydes with an intention to improve its pharmacological profile. The tests were performed to study their anti-inflammatory effect on carrageenan-induced ulcerative colitis in albino rats. The histopathological findings, serum transaminase level and lipid peroxide content in the intestine and liver were taken as indices of pharmacological activity. The azomethine derivative formed from salicylaldehyde (5-ASASB3) was found to have maximum activity and it reversed the disease symptoms in experimental animals The azomethine derivative markedly reduces the ulcerative colitis when compared with parent molecule, mesalazine.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 8","pages":"309-13"},"PeriodicalIF":0.0,"publicationDate":"2004-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25274628","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":"Behavior of cinnamoyl-isothiocyanate towards carbon, nitrogen and oxygen reagents.","authors":"N H Ouf, S El-Bahaie, M G Assy, E El-Shaikh","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Cyclization of cinnamoyl isothiocyanate with nucleophilic reagents either spontaneously or with added a reagents is reported.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 8","pages":"291-7"},"PeriodicalIF":0.0,"publicationDate":"2004-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25274626","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}
D Senthil Rajan, Uttam Kr Mandal, K Veeran Gowda, A Bose, M Ganesan, T K Pal
{"title":"Oral delivery system of insulin microspheres: effect on relative hypoglycemia of diabetic albino rats.","authors":"D Senthil Rajan, Uttam Kr Mandal, K Veeran Gowda, A Bose, M Ganesan, T K Pal","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of the present work was to investigate the effectiveness of a dosage form approach for monitoring both the inactivation and the absorption process by targeting insulin delivery to the upper region of small intestine. The dosage form is based on the incorporation of insulin with protease inhibitor and absorption enhancer into polyacrylic polymer Eudragit L-100. Insulin microspheres were prepared by solvent evaporation technique. And also study the effect of these microspheres upon the relative hypoglycemia (RH) effect in white diabetic albino rats has been studied in comparison to that produced after subcutaneous injection of bovine insulin solution. The oral administration of formulation with aprotinin and bile salts gave significant (p< 0.01) hypoglycemia when compared with formulation with insulin alone and with insulin and bile salts. However, the duration, course and the intensity of effect were different for each formulation. It was interesting to observe that the co-administration of aprotinin and bile salts produce prolonged and significant reduction of blood glucose level. A reduction of 4.47-36.81% in plasma glucose levels and RH of about 11.7% relative to subcutaneous injection of soluble insulin solution can be achieved by encapsulation along with protease inhibitor and bile salts.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 8","pages":"315-8"},"PeriodicalIF":0.0,"publicationDate":"2004-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25274629","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":"Synthesis of new triazolopyrimidines and substituted pyrimidines.","authors":"N H Ouf","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Hydrazinopyrimidine 3 was prepared and transformed into 4, 5 by the reaction with Ar-Cl and POCl3, respectively. Also 3 transformed into 6, 7 by the reaction with ArCHO and FeCl3 respectively. Compound 8 was prepared and transformed into 9, 10, 11 by the reaction with DDC, ethyl bromoacetate and Sodium ethoxide respectively.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 7","pages":"275-9"},"PeriodicalIF":0.0,"publicationDate":"2004-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25099044","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}
Tadeusz Librowski, Ryszard Czarnecki, Magdalena Jastrzebska-Wiesek, Wlodzimierz Opoka, Henryk Marona
{"title":"The influence of some aminoalkanolic xanthone derivatives on central nervous and cardiovascular systems in rodents.","authors":"Tadeusz Librowski, Ryszard Czarnecki, Magdalena Jastrzebska-Wiesek, Wlodzimierz Opoka, Henryk Marona","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of appropriate aminoalkanolic derivatives 2- or 4-methylxanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scPtz) assays, and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (R,S)-2N-(6-chloro-2-xanthonemethyl-2N-methylamino-1-propanol hydrochloride (II, which displayed anti-MES and anti-scPtz activity. Some of the obtained compounds (I - IV and V - VII) were also tested for their effect on the circulatory system (the effect on normal electrocardiogram, protection against adrenaline-, barium-, calcium- and/or strophanthine-induced arrhythmias, the effect on the arterial blood pressure and respiratory movements) and acute toxicity.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 7","pages":"267-74"},"PeriodicalIF":0.0,"publicationDate":"2004-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25099043","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":"Assessment of pharmacy patients' compliance in Bulgaria (2001--2002).","authors":"V Petkova, M Dimitrov","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The goal of this issue is to assess the level of compliance, respectively of non-compliance among pharmacY patients between the years 2001 and 2002 in Sofia, Bulgaria. The authors study and emphasize on the factors that influence the non-compliance of the patients and also try to find different ways to increase the rate of compliance in Bulgaria. Two types of standard individual questionnaires are applied for assessment of the state of compliance and non-compliance among the pharmacy patients. The obtained results show that the main reasons, influencing the non-adherence of the patients are: the high average price of the drugs, the overload daily regimen, inattention, distrust to the treatment and others. The drug form appears to be one of the main factors that cause non-compliance, especially when the patients receive more than one drug in different drug forms few times a day and especially if elderly patients are addressed. Despite the presented comparatively high level of compliance among the patients (from 53% for 2001, to 82% for 2002), there are strategies to enhance compliance that have to be initiated. They incorporate communication tactics, patient's education, and proper dosage of the drugs and scheduling of the drug application. The results of the analysis of the received data show an increase in the level of compliance for the pharmacy patients in Bulgaria. For 2001 it was 53%, while for 2002 it has increased to 82%. This fact shows the influence of strategies for improvement of compliance.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 7","pages":"263-6"},"PeriodicalIF":0.0,"publicationDate":"2004-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25100249","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}