• Title/Summary/Keyword: Biological Synthesis

Search Result 1,240, Processing Time 0.027 seconds

Facile Synthesis of 2',5'-Dideoxy-, 2',3'-Dideoxy- and 3'-Deoxy-1, N6-ethenoadenosine Nucleosides

  • Chae, Whi-Gun
    • Biotechnology and Bioprocess Engineering:BBE
    • /
    • v.4 no.1
    • /
    • pp.17-20
    • /
    • 1999
  • Facile synthetic methods of 2',5'-dideoxy-, 2',3'-dideoxy- and 3'-deoxy-1, N6-ethenoadenosine nucleosides by either an enzymatic dideoxyribosyl transfer reaction or a simple chemical reaction were proposed. The synthesis products were isolated and purified by preparative HPLC and their structures were confirmed by 1H NMR (500 MHz) and FAB-MS including high resolution mass measurement. These modified nucleoside analogs have not been reported yet. Therefore, these modified nucleoside analogs are of potential value to be studied further for biological activity such as anticancer or antiviral.

  • PDF

Synthesis and Biological Evaluation of 9-[2-Fluoro-4-hydroxy-3-hydroxymethyl-2-butenyl]adenine and its Related Compounds as Open-chain Analogues of Neplanocin A

  • Choi, Myung-Hee;Kim, Hee-Doo
    • Archives of Pharmacal Research
    • /
    • v.20 no.5
    • /
    • pp.501-506
    • /
    • 1997
  • Novel 9-[2-fluoro-4-hydroxy-3-hydroxymethyl-2-butenyl]adenine and its related compounds were designed and synthesized as open-chain analogues of neplanocin A. Alkylation of adenine or pyrimidine bases with the mesylate 4 was chosen as a simple approach to the synthesis of 2-fluoro-2-butenylated nucleosides. Mesylate 4 was prepared from dihydroxyacetone dimer via four steps in 58% overall yield. The synthesized compounds were evaluated their antiviral activity against HSV, HIV and Polio viruses.

  • PDF

Synthesis and Biological Evaluation of 3-Amino-4-aryl-piperidine Derivatives as BACE 1 Inhibitors

  • Lim, Hee-Jong;Jung, Myung-Hee;ChoiLee, Ihl-Young;Park, Woo-Kyu
    • Bulletin of the Korean Chemical Society
    • /
    • v.27 no.9
    • /
    • pp.1371-1376
    • /
    • 2006
  • BACE 1 ($\beta$-secretase), a membrane bound aspartic protease, is a key enzyme in the process of amyloid precursor protein (APP) into A$\beta$ peptide which is considered to play a causative role in Alzheimers Disease (AD). Here, we reported the synthesis and inhibitory activity of optically active 3-amino-4-aryl-piperidines.

Synthesis and Conformation of Novel 3'-Branched Threosyl-5'-Deoxyphosphonic Acid Nucleoside Analogues

  • Shen, Guang Huan;Kang, Lien;Kim, Eun-Ae;Lee, Won-Jae;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
    • /
    • v.33 no.8
    • /
    • pp.2574-2580
    • /
    • 2012
  • The discovery that threosyl phosphonate nucleoside (PMDTA, $EC_{50}=2.53{\mu}M$) is a potent anti-HIV agent has led to the synthesis and biological evaluation of 5'-deoxy versions of threosyl phosphonate nucleosides. In the present study, (E)-3'-phosphonoalkenyl and 3'-phosphonoalkyl nucleoside analogues 13, 16, 20 and 23 were synthesized from acetol and tested for anti-HIV activity and cytotoxicity. The adenine analogue 16 was found to exhibit moderate in vitro anti-HIV-1 activity ($EC_{50}=22.2{\mu}M$).

CuI Nanoparticles as New, Efficient and Reusable Catalyst for the One-pot Synthesis of 1,4-Dihydropyridines

  • Safaei-Ghomi, Javad;Ziarati, Abolfazl;Teymuri, Raheleh
    • Bulletin of the Korean Chemical Society
    • /
    • v.33 no.8
    • /
    • pp.2679-2682
    • /
    • 2012
  • A simple one-pot synthesis of two derivatives of 1,4-dihydropyridines has been described under reflux conditions using copper iodide nanoparticles (CuI NPs) as a catalyst in high yields. This method demonstrated four-component coupling reactions of aldehydes and ammonium acetate via two pathways. In one route, the reaction was performed using 2 eq ethyl acetoacetate while in the other one 1 eq ethyl acetoacetate and 1 eq malononitrile were used. The CuI NPs was reused and recycled without any loss of activity and product yield. It is noteworthy to state that wide range of the 1,4-dihydropyridines have attracted large interest due to pharmacological and biological activities.

Microwave Assisted One-pot Synthesis of Novel α-Aminophosphonates and heir Biological Activity

  • Rao, Alahari Janardhan;Rao, Pasupuleti Visweswara;Rao, Valsani Koteswara;Mohan, Challamchalla;Raju, Chamarthi Naga;Reddy, Cirandur Suresh
    • Bulletin of the Korean Chemical Society
    • /
    • v.31 no.7
    • /
    • pp.1863-1868
    • /
    • 2010
  • A simple and efficient synthesis of various $\alpha$-aminophosphonates (3a-l) by the reaction of substituted aromatic/heterocyclic aldehydes, 2-amino-6-methoxy-benzothiazole and dibutyl/diphenyl phosphites under microwave irradiation without catalyst was accomplished. The phosphonates were characterized by elemental analysis, IR, $^1H$, $^{13}C$- and $^{31}PNMR$ spectra. They showed promising antimicrobial, anti-oxidant activities depending on the nature of bioactive groups at the $\alpha$-carbon.

Discovery and Synthesis of Novel N-Cyanopyrazolidine and N-Cyanohexahydropyridazine Derivatives as Cathepsin Inhibitors

  • Song, Jong- Hwan;Kim, Sun-Gi;No, Zae-Sung;Hyun, Young-Lan;Jeon, Dong-Ju;Kim, Ik-Yon
    • Bulletin of the Korean Chemical Society
    • /
    • v.29 no.8
    • /
    • pp.1467-1471
    • /
    • 2008
  • The design, synthesis, and biological evaluation of structurally novel N-cyanopyrazolidine and N-cyanohexahydropyridazine derivatives as cathepsin inhibitors are described. In vitro assay reveals that several compounds exhibit highly potent and selective profiles against cathepsins K or S.

Application of Cl3CCONH2/PPh3 towards the Synthesis of Bioactive Amides

  • Chaysripongkul, Skydow;Pluempanupat, Wanchai;Jang, Doo-Ok;Chavasiri, Warinthorn
    • Bulletin of the Korean Chemical Society
    • /
    • v.30 no.9
    • /
    • pp.2066-2070
    • /
    • 2009
  • $Cl_3CCONH_2$ coupled with $PPh_3$ was determined to be an effective reagent for the conversion of carboxylic acids to their corresponding acid chlorides. Subsequently, these acid chlorides were successfully trapped with amines in the presence of 4-picoline, yielding amides. This practical and efficient protocol can be utilized for the synthesis of biological amides in excellent yields.

Interrelationship of Runx2 and estrogen pathway in skeletal tissues

  • Jeong, Jae-Hwan;Choi, Je-Yong
    • BMB Reports
    • /
    • v.44 no.10
    • /
    • pp.613-618
    • /
    • 2011
  • Two key molecules in skeletal tissues are bone formation master transcription factor Runx2 and the steroid hormone estrogen. It is well known that these two molecules play pivotal roles in bone homeostasis; however, the functional interaction between Runx2 and estrogen synthesis in skeletal tissues is largely unknown. Recent studies have indicated that there is a positive relationship between Runx2 and the estrogen biosynthesis pathway. In this review, a possible functional link between Runx2 and estrogen synthesis pathway in skeletal tissues will be discusses as well as the biological significance of this interaction.

Synthesis and Biological Activities of (4-Arylpiperazinyl)piperidines as Nonpeptide BACE 1 Inhibitors

  • Boja, Poojary;Won, Sun-Woo;Suh, Dong-Hoon;Chu, Jeong-Hyun;Park, Woo-Kyu;Lim, Hee-Jong
    • Bulletin of the Korean Chemical Society
    • /
    • v.32 no.4
    • /
    • pp.1249-1252
    • /
    • 2011
  • Inhibition of BACE 1 activity is considered as a promising therapeutic target for Alzheimer's Disease (AD). Synthesis and inhibitory activities of (4-arylpiperazinyl)piperidines by bioisosteric replacement of a biaryl group with an arylpiperazine as BACE 1 inhibitors are described. The resulting (4-arylpiperazinyl)piperidines represent novel nonpeptide BACE 1 inhibitors with improved in vitro potency.