• Title/Summary/Keyword: team project

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Synthesis and Some Properties of 4'-Phenyl-5'-Norcarbocyclic Adenosine Phosphonic Acid Analogues

  • Liu, Lian Jin;Kim, Eun-Ae;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.32 no.5
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    • pp.1662-1668
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    • 2011
  • Steric and electronic parameters of 4'-substituents play significant roles in steering the conformation of nucleoside analogues. In order to investigate the relationship of 4'-substituent with antiviral enhancement, novel 4'-phenyl-5'-norcarbocyclic adenosine phosphonic acid analogues were racemically synthesized via de novo acyclic stereoselective route from propionaldehyde 5. The phenyl substituted cyclopentenols 15a and 15b as key intermediates were successfully constructed via reiterative carbonyl addition of Grignard reagents and ring-closing metathesis of corresponding divinyl 14. The synthesized nucleoside phosphonic acids analogues 19, 20, 21, and 23 were subjected to antiviral screening against HIV-1.

2'-Spirocyclopropyl-carbocyclic Nucleoside as a Novel Scaffold for Potent Anti-HCV Agents

  • Li, Hua;Yoo, Jin-Cheol;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.32 no.4
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    • pp.1146-1152
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    • 2011
  • The discovery of 2'-spirocyclopropyl-ribocytidine (J. Med. Chem. 2010, 53, 8150-8160) as a potent inhibitor of RNA synthesis by NS5B ($IC_{50}=7.3{\mu}M$), the RNA polymerase encoded by hepatitis C Virus (HCV), has led to the synthesis and biological evaluation of several carbocyclic versions of 2'-spiropropyl-nucleosides. The cyclopentenol intermediate 7 was successfully constructed via ring-closing metathesis (RCM) from divinyl 6. Spirocyclopropanation of enone 8 was effected by using (2-chloroethyl)-dimethylsulfonium iodide and potassium tert-butoxide to form the desired intermediate 9. The synthesized nucleoside analogues 21-24 were assayed for their ability to inhibit HCV RNA replication in a subgenomic replicon Huh7 cell line. Among them, the cytosine nucleoside analogue 22 exhibited significant anti-HCV activity ($EC_{50}= 8.2{\mu}M$).

Effect of Ethanolamine Salts and Enhancers on the Percutaneous Absorption of Meloxicam from a Pressure Sensitive Adhesive Matrix

  • Ki, Han-Moe;Cheong, Hyun-Ah;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.37 no.3
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    • pp.173-177
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    • 2007
  • The purpose of this study was to investigate the effect of salt formation on the percutaneous absorption of meloxicam through hairless mouse skin from a pressure sensitive adhesive (PSA) matrix. In addition, the influences of enhancers on the permeation of meloxicam or meloxicam-ethanolamine (MX-EA) salts across the hairless mouse skin were evaluated using a flow-through diffusion cell system. The salt formation of meloxicam resulted in lower permeation rate than the parent drug. $Span^{(R)}$ 80 provided the highest enhancing effect for meloxicam and meloxicam monoethanolamine salt. The maximum amount of the drug that can be loaded without retarding permeation rate was different depending on the compound. No relationship was found between the fluxes of meloxicam or MX-EA salts from saturated solutions and those from PSA matrices containing the same enhancer.

Racemic Synthesis of Novel 6'-Methylene-5'-norcarbocyclic Purine Phosphonic Acid Analogues via Mitsunobu Reaction

  • Kim, Eun-Ae;Liu, Lian Jin;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.32 no.8
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    • pp.2689-2694
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    • 2011
  • Novel 5'-norcarbocyclic adenine and guanine phosphonic acid analogues with 6'-electronegative moiety such as unsaturated C-C bond were designed and synthesized from commercially available 2-methylene-propane-1,3-diol (4). Regioselective Mitsunobu reaction successfully proceeded from an allylic functional group (${\pm}$)-12b at low reaction temperature in polar cosolvent (DMF/1,4-dioxane) to give purine phosphonate analogues (${\pm}$)-13 and (${\pm}$)-20. The purine nucleoside phosphonate and phosphonic acid analogues were subjected to antiviral screening against HIV-1. Guanine analogue (${\pm}$)-23 shows significant anti-HIV activity in PBM cell lines ($EC_{50}=8.1\;{\mu}M$).

Synthesis and Potent Anti-leukemic Activity of Novel 5'-Norcarbocyclic C-nucleoside Phosphonic Acids

  • Kim, Seyeon;Kim, Eunae;Oh, Chang-Hyun;Yoo, Kyung Ho;Hong, Joon Hee
    • Bulletin of the Korean Chemical Society
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    • v.35 no.12
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    • pp.3502-3508
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    • 2014
  • The first synthetic route to 5'-norcarbocyclic C-nucleoside [7-oxa-7,9-dideazadenosine (furo[3,2-d]pyrimidine) and 9-deazaadenosine (pyrrolo[3,2-d]pyrimidine)] phosphonic acids from commercially available 1,3-dihydroxy cyclopentane was described. The key C-C bond formation from sugar to base precursor was performed using Knoevenagel-type condensation from a ketone derivative. Synthesized C-nucleoside phosphonic acids were tested for anti-HIV activity as well as anti-leukemic activity. Compound 26 showed significant anti-leukemic activity.

Design and Synthesis of Novel 2'(β)-Fluoro-3'(α)-hydroxy-threose Nucleosides: Iso-FMAU Analogues as Potent Antiviral Agents

  • Kim, Seyeon;Jee, Jun-Pil;Hong, Joon Hee
    • Journal of Integrative Natural Science
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    • v.8 no.2
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    • pp.99-106
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    • 2015
  • Novel 2'(${\beta}$)-fluoro-3'(${\alpha}$)-hydroxy-threose nucleosides (iso-FMAU) as antiviral agents were designed and racemically synthesized from Solketal. Condensation successfully proceeded from a glycosyl donor 9 under $Vorbr{\ddot{u}}ggen$ conditions yielded the nucleoside analogues. Ammonolysis and hydrolysis of isopropylidene protection group gave the desired nucleoside analogues 12, 15, 18, and 19. The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2 and HCMV. Compound 12 displayed some anti-HCMV activity ($EC_{50}=24.7{\mu}g/ml$) without exhibiting any cytotoxicity up to $100{\mu}M$.

The development of the MMI system for automating steel-making process (제철 공정 자동화를 위한 MMI 시스템 개발)

  • Lee, Dae-Sung;Kim, Yoon-Ha;Joo, Moon-Jab
    • Proceedings of the KIEE Conference
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    • 2002.07d
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    • pp.2469-2471
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    • 2002
  • MMI 시스템은 제철 공정에서 발생되는 다양한 데이터를 조업자에게 쉽고 빠르게 전달하기 위해, real time operating system에서 동작하는 제철공정의 주된 제어 프로세스와 인터페이스 한다. 따라서 MMI 시스템은 제철 공정의 주된 제어 프로세스와 ethernet network을 통해 공유 데이터들을 통신하도록 개발되고, MMI 시스템은 M/S window operating system과 DDE(Dynamic Data Exchange) 라이브러리 환경을 기반으로 개발된다. 수 개의 MMI client PC와 1 개의 MMI server로 구성되는 MMI 시스템은 MMI client들 사이의 공유 데이터가 동기화될 수 있도록 최적 packet 양을 도출하고, 신뢰성 높은 데이터 전송을 위한 특별한 데이터 핸들링 방법을 사용한다. MMI 시스템은 GUI(Graphic User Interface)를 사용하여 조업자에게 친숙한 window 화면을 제공하므로, MMI 시스템의 화면 수정, 첨가 및 삭제가 비용 부담없이 용이하게 진행되므로, 기존 제철 공정에서 사용하던 OCP(Operating Control Panel)들이 MMI 시스템으로 대체되고 있다.

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Harmonic Distortion Control for Electric Propulsion (전기 추진선을 위한 고조파 제어 사례 연구)

  • Kim, Ju-Wan;Lee, Choong-Yeol;Seo, Kun-Kyung
    • Special Issue of the Society of Naval Architects of Korea
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    • 2008.09a
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    • pp.38-45
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    • 2008
  • The application of the electric propulsion system to the vessels has recently become common due to the latest technology for controlling the electric motors with variable speed. However it has been found that harmonic distortion exists in the electric propulsion system, which consists of an electric motor, a converter and an inverter, and this harmonic distortion has a harmful effect on the system. In this paper, the definition of the harmonic distortion and problems caused by the harmonic distortion in the electric propulsion of the vessels are introduced and the practical solutions for the problems are investigated.

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A study on the Plan for Organization Activation use analysis of Success factor Integration Information System (통합정보시스템 구축 프로젝트 성공 요인 분석을 통한 조직 활성화 방안에 대한 연구)

  • Park, Jong-Ki;Kang, Kyong-Sik
    • Proceedings of the Safety Management and Science Conference
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    • 2006.11a
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    • pp.367-372
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    • 2006
  • Since 1990's, many enterprises have constructed Integration Information System. Especially, they want to become an advanced company use ERP package. Already, ERP system come to high level which is stabilized and support independent business process of many industry sectors. Therefore, important success factors for ERP project are change management and organization activation. Although most companies had previous good plans, but those are not satisfied. Because of failed to change management and discontinued next activity for promotion. This paper studied success factors of project team and plan for organization activation. Also, it proposed next study subject about investigate the role of the member of task force team as a factor that makes the ERP system a success. The results of this study can be used for a successful construction of the ERP system as a solution about internal problems of Project team.

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A study on the Plan for Organization Activation use analysis of Success factor Integration Information System (통합정보시스템 구축 프로젝트 성공 요인 분석을 통한 조직 활성화 방안에 대한 연구)

  • Park, Jong-Ki;Kang, Kyong-Sik
    • Journal of the Korea Safety Management & Science
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    • v.8 no.5
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    • pp.231-242
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    • 2006
  • Since 1990's, many enterprises have constructed Integration Information System. Especially, they want to become an advanced company use ERP package. Already, ERP system come to high level which is stabilized and support independent business process of many industry sectors. Therefore, important success factors for ERP project are change management and organization activation. Although most companies had previous good plans, but those are not satisfied. Because of failed to change management and discontinued next activity for promotion. This paper studied success factors of project team and plan for organization activation. Also, it proposed next study subject about investigate the role of the member of task force team as a factor that makes the ERP system a success. The results of this study can be used for a successful construction of the ERP system as a solution about Internal problems of Project team.