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마이크로파를 이용한 강한 항균제인 새로운 N1-치환된 5-Cyano-pyrimidine 유도체의 합성
Pore, Yogesh,Patil, Gaurav,Tamboli, Ijaj,Chavan, Vaibhav,Kamble, Kirti,Nikam, Shital,Kuchekar, Bhanudas 대한화학회 2008 대한화학회지 Vol.52 No.1
연구의 목적은 N1과 6번 자리에 다른 치환기를 가진 5-cyano가 치환된 pyrimidine 아날로그의 새로운 시리즈의 합성과 그것들의 항균성과 항진균성의 활성도에 대해 평가하기 위해서이다. 이 화합물은 MORE technique 를 이용한 potassium carbonate 의 존재하에서 ethylcyanoacetate, 치환된 thioureas, 적당한 알데히드의 제 3차 축합으로 합성 되어졌다. 항균성과 항진균성의 활성도는 25 mg의 농도에서 cup-plate 방법으로 측정되었다. 억제구역은 mm로 측정 되어졌다. 모든 화합물은 좋은 항균성과 항진균성을 보여주었다. P1과 P5는 S.aureus과 E.coli에 대해 최대 활성도를 보여주었고, P6은 모든 종류의 미생물에 대해 좋은 활성도를 보여주었다. P8 화합물은 C. albicans 에 대해 좋은 효과가 있음을 알아냈다. Norfloxacin와 griseofulvin는 합성된 화합물의 활성도와 비교되는 기준물질로 사용되었다. 6번 자리에 p-hydroxy와 p-methoxy로 치환된 phenyl moiety를 가진 gram-양성 미생물에 대해 강력했고, 6번 자리에 이것들이 없는 phenyl moiety 를 가진 아날로그는 gram-음성 활성도를 가졌다,6번 자리에 p-dimethylamino로 치환된 phenyl moiety를 가진 화합물은 적당한 활성을 보여준다.. 게다가 N1자리에서 단지 fluorine을 포함한 아날로그는 상당한 항진균성을 가졌음을 밝혀냈다. N1자리에서 aryl moiety 의 전자 끌게 치환과 마찬가지로 전자 주게 치환은 화합물의 결정된 능력에 중요한 역할을 함을 제시한다. purpose of the study was to synthesize new series of 5-cyano substituted pyrimidine analogues with different substitutions at N1 and 6 positions and to evaluate them for antibacterial and antifungal activities. The desired compounds were synthesized by tertiary condensation of ethylcyanoacetate, substituted thioureas and suitable aldehyde in presence of potassium carbonate using MORE technique. The antibacterial and antifungal activities were evaluated by cup plate method in the concentration of 25 mg. The zone of inhibition was measured in mm. All the compounds have shown significant antibacterial and antifungal activities. The maximum activity was shown by P1 and P5 against S.aureus and E.coli respectively, while P6 has shown significant activity against all types of microorganisms. The compound P8 has been found to be significantly effective against C. albicans. Norfloxacin and griseofulvin were used as standards to compare the activites of synthesized compounds. It is concluded that analogues containing p-hydroxy, p-methoxy substituted phenyl moiety at 6 position have been found to be more potent against gram-positive microorganisms, while analogues lacking these substituents on phenyl moiety possessed gram-negative activity. The compounds having p-dimethylamino substituent on phenyl moiety at 6 positions have shown moderate activity. Further, only fluorine containing analogue at N1 position was found to possess appreciable antifungal activity. This suggests that electron donating substituent on aryl moiety as well as electron withdrawing substituent at N1 plays important role in determining potency of the compounds.
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Ashwini Patil,Yogesh Pore,Yogesh Gavhane,Shitalkumar Patil,Sachinkumar Patil 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.3
Spherical agglomerates of ezetimibe (EZT)were prepared with hydrophilic polymers; polyvinyl pyrrolidoneK30 (PVP) and/or poloxamer 188 (poloxamer) atdrug to polymer ratios of 1:1 (w/w) by spherical crystallizationtechnique, in order to improve its physicochemicaland micromeritic properties. Three different bridging liquids;chloroform, dichloromethane and/or ethyl acetatealong with good solvent acetone and poor solvent waterwere used to form six batches of agglomerates. Initialcharacterization of all batches in terms of micromeritic andphysicochemical properties resulted in optimization of (A3,EZT:PVP:ethyl acetate) and (B3, EZT:poloxamer:ethylacetate) batches and hence further investigated for drug–polymer interaction, crystallinity and morphology usingFTIR, XRPD, DSC and SEM techniques. The resultsindicated presence of hydrogen bonding, crystallinity andspherical shape in agglomerates. Therefore, the optimizedagglomerates (B3) were directly compressed into tablet. Unfortunately, drug release from the tablet was not satisfactory,suggesting a need of disintegrant from dissolutionpoint of view. Therefore, these agglomerates were recompressedincorporating certain excipients and evaluated asper pharmacopoeia. The dissolution rate of prepared tabletwas similar to that of marketed tablet (p[0.05). It couldbe concluded that spherical crystallization could be one ofthe effective and alternative approaches for improvedperformance of EZT and its tablet formulation.
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Priyanka Bhosale,Yogesh Pore,Fahim Sayyad 한국약제학회 2012 Journal of Pharmaceutical Investigation Vol.42 No.6
The aim of the present study was to enhance the physicochemical properties of poorly aqueous soluble carvedilol (CRV) by preparing its microparticles in presence and/or in absence of a hydrophilic carrier. The polymeric microparticles of CRV were prepared with polyvinylpyrrolidone K30 with or without addition of adsorbents like Aerosil200 and/or Sylysia350 by using spray drying technique. The dissolution profiles revealed that the drug and polymer ratio and colloidal silica both played critical role in solubility enhancement. The spray dried microparticles and drug alone were characterized by differential scanning calorimetry (DSC), X-ray powder diffraction, Fourier transformation infrared spectroscopy (FTIR), particle size analysis and scanning electron microscopy (SEM). DSC analysis showed that CRV transformed from the crystalline state to amorphous state by spray drying, confirmed by disappearance of its melting peak. The results of the X-ray analysis were in agreement with the thermal analysis data. It did not show characteristic crystalline drug peaks which confirmed that the amorphous form of CRV was present in the CRV loaded microparticles. FTIR analysis demonstrated hydrogen bonding interaction with an absence of significant chemical interaction between CRV and polymer. Spherical microparticles were yielded with smooth surfaces as observed by SEM. All in all, this work reveals that spray drying is a suitable technique for preparation of microparticles with improved physicochemical properties of CRV.
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