Two simple assay procedures for quantitation of dothiepin HCl has been developed using dothiepin-selective electrode. The first (electrode I) was based on drug, falvianic acid ion pair complex, Bis(2-ethylhexyl-phthalate) and poly vinylchroride (PVC) matrix, second electrode (electrode Ⅱ) based on drug, tungstosilicic acid, Bis(2-ethylhexyl sebactate) as plastisizer and polyvinyl chloride matrix. The elctrolodes showed a near-nernsation response in the range of (10^(-2) to 10^(-4)) and (10^(-1) to 10^(-4)) dothiepin over the pH range of 5 to 8 for the two electrods. The selectivity of the electrode to a number of interferences was investigated. This assay was applied to determine dothiepin HCl in capsules and results compared with those obtained by official method.
{"title":"Quantitative analysis of dothiepin HCl by ion selective electrode","authors":"M. Hosny","doi":"10.7019/CPJ.200702.0025","DOIUrl":"https://doi.org/10.7019/CPJ.200702.0025","url":null,"abstract":"Two simple assay procedures for quantitation of dothiepin HCl has been developed using dothiepin-selective electrode. The first (electrode I) was based on drug, falvianic acid ion pair complex, Bis(2-ethylhexyl-phthalate) and poly vinylchroride (PVC) matrix, second electrode (electrode Ⅱ) based on drug, tungstosilicic acid, Bis(2-ethylhexyl sebactate) as plastisizer and polyvinyl chloride matrix. The elctrolodes showed a near-nernsation response in the range of (10^(-2) to 10^(-4)) and (10^(-1) to 10^(-4)) dothiepin over the pH range of 5 to 8 for the two electrods. The selectivity of the electrode to a number of interferences was investigated. This assay was applied to determine dothiepin HCl in capsules and results compared with those obtained by official method.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"75 1","pages":"25-30"},"PeriodicalIF":0.0,"publicationDate":"2007-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85779385","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}
Microparticulate systems of nimesulide (NIM) were prepared by modified solvent evaporation method using different variables such as polymer: drug (NIM) ratios (ethyl cellulose, EC: nimesulide, NIM) (1:9, 1:6 and 1:3), agitation speeds (500-1000 rpm) and stirring time (5-15 min). The effects of processing variables were evaluated by microparticle size and entrapment efficiency. The average microparticle size increases from 65.53±1.02 to 97.3±2.06 μm with increase in the polymer concentration while reduces with increase in agitation speed and stirring time; but at the too higher speed gives irregular shape of particles. The highest entrapment efficiency (75.17±0.44%), size uniformity, free flowability, i.e., angle of repose (27.5±0.3°) and compressibility index (16.1±1.1%), of microparticles were found with 1:6 (polymer: drug ratio), at 800 rpm and 10 min stirring time among all prepared microparticles (p≤0.05). The in-vitro drug release study of microparticles with optimized processing variables (agitation speed and time) were carried out and compared with conventional and marketed SR tablets. The conventional and SR tablet releases maximum drug within 4 and 8 h while microparticulate system releases more than 14 h. All formulations followed first order release kinetic and diffusion controlled drug release (Higuchi model). These microparticles are stable at room temperature (25±1℃) but agglomerate at elevated temperature (50±1℃) by softening and fusion of the polymer observed under SEM study.
{"title":"Effect of Processing Variables on Micro Particulate System of Nimesulide","authors":"K. Dashora, S. Saraf, S. Saraf","doi":"10.7019/CPJ.200604.0067","DOIUrl":"https://doi.org/10.7019/CPJ.200604.0067","url":null,"abstract":"Microparticulate systems of nimesulide (NIM) were prepared by modified solvent evaporation method using different variables such as polymer: drug (NIM) ratios (ethyl cellulose, EC: nimesulide, NIM) (1:9, 1:6 and 1:3), agitation speeds (500-1000 rpm) and stirring time (5-15 min). The effects of processing variables were evaluated by microparticle size and entrapment efficiency. The average microparticle size increases from 65.53±1.02 to 97.3±2.06 μm with increase in the polymer concentration while reduces with increase in agitation speed and stirring time; but at the too higher speed gives irregular shape of particles. The highest entrapment efficiency (75.17±0.44%), size uniformity, free flowability, i.e., angle of repose (27.5±0.3°) and compressibility index (16.1±1.1%), of microparticles were found with 1:6 (polymer: drug ratio), at 800 rpm and 10 min stirring time among all prepared microparticles (p≤0.05). The in-vitro drug release study of microparticles with optimized processing variables (agitation speed and time) were carried out and compared with conventional and marketed SR tablets. The conventional and SR tablet releases maximum drug within 4 and 8 h while microparticulate system releases more than 14 h. All formulations followed first order release kinetic and diffusion controlled drug release (Higuchi model). These microparticles are stable at room temperature (25±1℃) but agglomerate at elevated temperature (50±1℃) by softening and fusion of the polymer observed under SEM study.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"47 1","pages":"67-74"},"PeriodicalIF":0.0,"publicationDate":"2006-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78405911","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}
R. M. Youssef, E. Khamis, A. Gazy, H. Mahgoub, M. Elsayed
A simple kinetic method was developed for the determination of Buspirone hydrochloride (BUS) in pharmaceutical preparation. The method is based on kinetic investigation of the oxidation reaction of the drug with alkaline potassium permanganate at room temperature for a fixed time of 20 min. The absorbance of the green coloured manganate ion produced was measured at 610 nm. Alternatively, the decrease in the absorbance of permanganate ion after addition of the drug was measured at 525 nm. Calibration graphs in both procedures were linear over the concentration range 10-40 μg/mL. The different experimental parameters affecting the development and stability of the colours were carefully studied and optimized. The determination of BUS by rate constant method, fixed concentration method and fixed time method was also feasible with calibration equations obtained but the latter method was found to be more applicable.
{"title":"Assay of Buspirone Hydrochloride in Tablets Using Kinetic Spectrophotometry","authors":"R. M. Youssef, E. Khamis, A. Gazy, H. Mahgoub, M. Elsayed","doi":"10.7019/CPJ.200604.0085","DOIUrl":"https://doi.org/10.7019/CPJ.200604.0085","url":null,"abstract":"A simple kinetic method was developed for the determination of Buspirone hydrochloride (BUS) in pharmaceutical preparation. The method is based on kinetic investigation of the oxidation reaction of the drug with alkaline potassium permanganate at room temperature for a fixed time of 20 min. The absorbance of the green coloured manganate ion produced was measured at 610 nm. Alternatively, the decrease in the absorbance of permanganate ion after addition of the drug was measured at 525 nm. Calibration graphs in both procedures were linear over the concentration range 10-40 μg/mL. The different experimental parameters affecting the development and stability of the colours were carefully studied and optimized. The determination of BUS by rate constant method, fixed concentration method and fixed time method was also feasible with calibration equations obtained but the latter method was found to be more applicable.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"21 1","pages":"85-94"},"PeriodicalIF":0.0,"publicationDate":"2006-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82027785","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}
Chien-Ming Huang, Liansheng Su, Wen‐Hsin Huang, A. Lee
A practically facile microwave-enhanced synthesis of polyfunctionalized benzopyrans is described. The respective aromatic aldehyde and trimethoxyphenol with malononitrile in the presence of phase transfer agent (10 mol%, tetramethylammonium bromide or benzyltriethylammonium chloride) in water by microwave irradiation-assisted Knoevenagel and Pinner condensations provided novel polyfunctionalized 4-aryl-4H-benzopyrans, substituted 2-amino-4-aryl-4H-5,6,7-trimethoxy-chromene-3-carbonitriles (1-12), in high yields. The title benzopyrans had been primarily examined the cytotoxicity for MCF-7 (breast cancer cell), NCI-H460 (lung cancer cell) and SF268 cells (glioblastoma cell) by sulforhodamine B (SRB) assay.
{"title":"An Expedient One-pot Synthesis of Polyfunctionalized 4-Aryl-4H-benzo[b]pyrans as Potential Cytotoxic Agents","authors":"Chien-Ming Huang, Liansheng Su, Wen‐Hsin Huang, A. Lee","doi":"10.7019/CPJ.200502.0001","DOIUrl":"https://doi.org/10.7019/CPJ.200502.0001","url":null,"abstract":"A practically facile microwave-enhanced synthesis of polyfunctionalized benzopyrans is described. The respective aromatic aldehyde and trimethoxyphenol with malononitrile in the presence of phase transfer agent (10 mol%, tetramethylammonium bromide or benzyltriethylammonium chloride) in water by microwave irradiation-assisted Knoevenagel and Pinner condensations provided novel polyfunctionalized 4-aryl-4H-benzopyrans, substituted 2-amino-4-aryl-4H-5,6,7-trimethoxy-chromene-3-carbonitriles (1-12), in high yields. The title benzopyrans had been primarily examined the cytotoxicity for MCF-7 (breast cancer cell), NCI-H460 (lung cancer cell) and SF268 cells (glioblastoma cell) by sulforhodamine B (SRB) assay.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"12 1","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2005-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89568619","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}
API-ionspray MS and tandem MS/MS techniques were utilized to elucidate the structures of ten flavonoids consisting of five flavonols-morin, and one O-methyl and three acetyl derivatives, and five flavanones-desmethoxymatteucinol, and one acetyl and three O-methyl analogs. Morin and desmethoxymatteucinol were isolated and identified previously from the barks of Vanieria cochinchinesis Lour. (Moraceae) and the flowers of Eugenia javanica Lam. (Myrtaceae), respectively, based on the UV, IR, NMR, EI-MS and derivatization data. In this investigation, apparent protonated molecular (MH^+), MNH4^+, MNa^+ and MK^+ ions in the Q1 Scan MS spectra, and prominent as well as diagnostic product ions for structural elucidation in the tandem MS/MS spectra were observed for all investigated flavonoids each in nanogram quantities.
{"title":"Structural Characterization of Flavonols and Flavanones in Nanogram Quantities by API-ionspray Tandem Mass Spectrometry","authors":"W. Wu, Chong-Heng Huang","doi":"10.7019/CPJ.200502.0007","DOIUrl":"https://doi.org/10.7019/CPJ.200502.0007","url":null,"abstract":"API-ionspray MS and tandem MS/MS techniques were utilized to elucidate the structures of ten flavonoids consisting of five flavonols-morin, and one O-methyl and three acetyl derivatives, and five flavanones-desmethoxymatteucinol, and one acetyl and three O-methyl analogs. Morin and desmethoxymatteucinol were isolated and identified previously from the barks of Vanieria cochinchinesis Lour. (Moraceae) and the flowers of Eugenia javanica Lam. (Myrtaceae), respectively, based on the UV, IR, NMR, EI-MS and derivatization data. In this investigation, apparent protonated molecular (MH^+), MNH4^+, MNa^+ and MK^+ ions in the Q1 Scan MS spectra, and prominent as well as diagnostic product ions for structural elucidation in the tandem MS/MS spectra were observed for all investigated flavonoids each in nanogram quantities.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"9 1","pages":"7-15"},"PeriodicalIF":0.0,"publicationDate":"2005-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85790372","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}
API-ionspray MS and tandem MS/MS techniques were utilized to elucidate the structures of eight natural products consisting of lithospermoside and its two acetates, syringin and its two acetates, and two triterpenes-acetyloleanolic acid and methyloleanoate. Lithospermoside, syringin, and oleanolic acid were isolated and identified previously from Thalictrum rugosum (Ranuncularceae), Magnolia grandiflora (Magnoliaceae), and Eugenia javanica Lam. (Myrtaceae), respectively, on the basis of UV, IR ,NMR,MS (EI, CI) and CD data. In this investigation, apparent protonated molecular (MH^+), ammonium-adducted molecular (MNH4^+), and alkali-metal-adducted molecular (MNa^+ and MK^+) ions in the Q1 Scan MS spectra, and prominent as well as diagnostic product ions for structural elucidation in the tandem MS/MS spectra were observed for all investigated natural products each in nanogram quantities of material.
{"title":"Structural elucidation of glucosides and triterpenes by API-ionspray MS and tandem MS/MS spectrometry","authors":"W. Wu, Chong-Heng Huang","doi":"10.7019/CPJ.200502.0017","DOIUrl":"https://doi.org/10.7019/CPJ.200502.0017","url":null,"abstract":"API-ionspray MS and tandem MS/MS techniques were utilized to elucidate the structures of eight natural products consisting of lithospermoside and its two acetates, syringin and its two acetates, and two triterpenes-acetyloleanolic acid and methyloleanoate. Lithospermoside, syringin, and oleanolic acid were isolated and identified previously from Thalictrum rugosum (Ranuncularceae), Magnolia grandiflora (Magnoliaceae), and Eugenia javanica Lam. (Myrtaceae), respectively, on the basis of UV, IR ,NMR,MS (EI, CI) and CD data. In this investigation, apparent protonated molecular (MH^+), ammonium-adducted molecular (MNH4^+), and alkali-metal-adducted molecular (MNa^+ and MK^+) ions in the Q1 Scan MS spectra, and prominent as well as diagnostic product ions for structural elucidation in the tandem MS/MS spectra were observed for all investigated natural products each in nanogram quantities of material.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"12 1","pages":"17-27"},"PeriodicalIF":0.0,"publicationDate":"2005-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75374990","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}
Two methods have been developed for the determination of terazosin in pure form and in dosage forms- one based on a potentiometric sensor and the other a voltammetric technique. Terazosin-silicotungstic acid ion-association is developed as an ionophore in the fabrication of the potentiometric sensor. The optimum concentration range of the developed method was 7 x 10^(-2) to 8 X 10^(-4) M of the drug. The system gave a perfectly Nernstian slope (59.3 mV per decade) in the pH 4.2 with hardly any interference from the common cations and anions. The cyclic and linear sweep voltammetric studies of the drug on a glassy carbon electrode in the potential range -100 to +100 mV with a switching potential of 800 mV have also been carried out. The drug gave a well-defined irreversible anodic peak at 774 mV when sodium hydroxide was used as the supporting electrolyte. Influence of scan rate and concentration on current were studied and based on this, a voltammetric method has also been developed for the quantitative determination of the drug. Both the methods have been applied for the determination of the drug in two commercially available tablets and the results are highly precise and accurate.
{"title":"Electrochemical Determination of Terazosin in Pure Form and in Dosage Forms","authors":"K. G. Kumar, S. John, R. Poduval, P. Augustine","doi":"10.7019/CPJ.200502.0029","DOIUrl":"https://doi.org/10.7019/CPJ.200502.0029","url":null,"abstract":"Two methods have been developed for the determination of terazosin in pure form and in dosage forms- one based on a potentiometric sensor and the other a voltammetric technique. Terazosin-silicotungstic acid ion-association is developed as an ionophore in the fabrication of the potentiometric sensor. The optimum concentration range of the developed method was 7 x 10^(-2) to 8 X 10^(-4) M of the drug. The system gave a perfectly Nernstian slope (59.3 mV per decade) in the pH 4.2 with hardly any interference from the common cations and anions. The cyclic and linear sweep voltammetric studies of the drug on a glassy carbon electrode in the potential range -100 to +100 mV with a switching potential of 800 mV have also been carried out. The drug gave a well-defined irreversible anodic peak at 774 mV when sodium hydroxide was used as the supporting electrolyte. Influence of scan rate and concentration on current were studied and based on this, a voltammetric method has also been developed for the quantitative determination of the drug. Both the methods have been applied for the determination of the drug in two commercially available tablets and the results are highly precise and accurate.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"16 1","pages":"29-36"},"PeriodicalIF":0.0,"publicationDate":"2005-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86880631","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}
H. Ding, Mei-Ying Liu, Wen-liang Chang, Hang-Ching Lin
Three new sesquiterpenoids, atractylenolide V, Atractylenolide VI and Atractylenolide VII, together with four known sesqiterpenoids were isolated from the rhizomes of Atractylodes macrocephala. Their structures were established on the basis of spectral evidence.
{"title":"New sesquiterpenoids from the rhizomes of Atractylodes macrocephala","authors":"H. Ding, Mei-Ying Liu, Wen-liang Chang, Hang-Ching Lin","doi":"10.7019/CPJ.200502.0037","DOIUrl":"https://doi.org/10.7019/CPJ.200502.0037","url":null,"abstract":"Three new sesquiterpenoids, atractylenolide V, Atractylenolide VI and Atractylenolide VII, together with four known sesqiterpenoids were isolated from the rhizomes of Atractylodes macrocephala. Their structures were established on the basis of spectral evidence.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"14 1","pages":"37-42"},"PeriodicalIF":0.0,"publicationDate":"2005-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76454492","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 yeast Hansenula polymorpha was used as a host for the expression of the gamma chain pep tide of the F(subscript ab) fragment of the mouse anticreatine kinase-MIgG antibody. Two expression systems were de signed and assembled based on the promoters of the highly expressed enzymes, formate dehydrogenase (FMD) and methanol oxidase MOX of H. polymorpha. Two expression plasmid vectors, pGAGU and pHAAI, with FMD and MOX promoters, respectively, were constructed and transformed into H. polymorpha LR9. The expression of the gamma chain gene yielded about 400mg/L and 550mg/L, representing 7% and 10% of the total cell protein under the control of FMD and MOX promoters, respectively. The prepro-alpha was in completely processed and most of the gamma chain peptide accumulated within the cells, especially under the control of the FMD promoter.
{"title":"Expression of Heavy Chain Peptide Gamma of Mouse Anticreatine Kinase IgG Antibody in the Yeast Hansenula polymorpha","authors":"H. Abdel-salam, G. Enan, C. Hollenberg","doi":"10.7019/CPJ.200406.0147","DOIUrl":"https://doi.org/10.7019/CPJ.200406.0147","url":null,"abstract":"The yeast Hansenula polymorpha was used as a host for the expression of the gamma chain pep tide of the F(subscript ab) fragment of the mouse anticreatine kinase-MIgG antibody. Two expression systems were de signed and assembled based on the promoters of the highly expressed enzymes, formate dehydrogenase (FMD) and methanol oxidase MOX of H. polymorpha. Two expression plasmid vectors, pGAGU and pHAAI, with FMD and MOX promoters, respectively, were constructed and transformed into H. polymorpha LR9. The expression of the gamma chain gene yielded about 400mg/L and 550mg/L, representing 7% and 10% of the total cell protein under the control of FMD and MOX promoters, respectively. The prepro-alpha was in completely processed and most of the gamma chain peptide accumulated within the cells, especially under the control of the FMD promoter.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"22 1","pages":"147-158"},"PeriodicalIF":0.0,"publicationDate":"2004-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85519051","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}
Fengtian Wu, G. Chen, Meiqin Chen, Fong-Chi Cheng, J. Chern
Four 8-aryl-4-(N-cyclopropylmethyl-N-propyl)amino-2-methylquinazolines were synthesized, and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 22 and 23 possessed high rCRHR1 affinities of K(subscript i)=13 and 50 nM, respectively. The quinazoline derivatives showed parallel SAR to the other known bicyclic system; the ortho-substituent on the 8-aryl ring is indispensable.
{"title":"Studies on Quinazolines. 12.^1 Design of 4-Amino-8-arylquinazoline Derivatives as Potential Non-Peptide Corticotropin-Releasing Hormone Receptor I (CRHR1) Antagonists","authors":"Fengtian Wu, G. Chen, Meiqin Chen, Fong-Chi Cheng, J. Chern","doi":"10.7019/CPJ.200404.0097","DOIUrl":"https://doi.org/10.7019/CPJ.200404.0097","url":null,"abstract":"Four 8-aryl-4-(N-cyclopropylmethyl-N-propyl)amino-2-methylquinazolines were synthesized, and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 22 and 23 possessed high rCRHR1 affinities of K(subscript i)=13 and 50 nM, respectively. The quinazoline derivatives showed parallel SAR to the other known bicyclic system; the ortho-substituent on the 8-aryl ring is indispensable.","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"72 1","pages":"97-109"},"PeriodicalIF":0.0,"publicationDate":"2004-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77443911","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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