• Title/Summary/Keyword: Imidazopyridine

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Cross-Coupling Reaction of 2-halo1-methyl-1H-imidazo[4,5-b]pyridine Offers a New Synthetic Route to Mutagenic Heterocyclic Amine-PHIP and DMIP

  • Sajith, Ayyiliath M.;Muralidharan, Arayambath;Karuvalam, Ranjith P.;Haridas, Karickal R.
    • Journal of the Korean Chemical Society
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    • v.57 no.3
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    • pp.361-364
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    • 2013
  • A modified synthetic approach to the synthesis of heterocyclic food mutagens, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PHIP) and 2-amino-1,6-dimethylimidazo[4,5-b]pyridine (DMIP) is reported. This route highlights an optimized palladium catalysed Buchwald cross-coupling of 2-halo-1-methyl-imidazo[4,5-b]pyridine with benzophenoneimine followed by acidic hydrolysis to yield compound 7. Using finely tailored conditions, Suzuki cross-coupling reactions with highly efficient catalytic systems were performed as the final step on 8 to introduce the aryl group and methyl group on the heterocyclic core.

[ ${\beta}-Amyloid$ ] Imaging Probes (베타아밀로이드 영상용 프로브)

  • Jeong, Jae-Min
    • Nuclear Medicine and Molecular Imaging
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    • v.41 no.2
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    • pp.112-117
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    • 2007
  • Imaging distribution of ${\beta}-amyloid$ plaques in Alzheimer's disease is very important for early and accurate diagnosis. Early trial of the ${\beta}-amyloid$ plaques includes using radiolabeled peptides which can be only applied for peripheral ${\beta}-amyloid$ plaques due to limited penetration through the blood brain barrier (BBB). Congo red or Chrysamine G derivatives were labeled with Tc-99m for imaging ${\beta}-amyloid$ plaques of Alzheimer patient's brain without success due to problem with BBB penetration. Thioflavin T derivatives gave breakthrough for ${\beta}-amyloid$ imaging in vivo, and a benzothiazole derivative [C-11]6-OH-BTA-1 brought a great success. Many other benzothiazole, benzoxazole, benzofuran, imidazopyridine, and styrylbenzene derivatives have been labeled with F-18 and I-123 to improve the imaging quality. However, [C-11]6-OH-BTA-1 still remains as the best. However, short half-life of C-11 is a limitation of wide distribution of this agent. So, it is still required to develop an Tc-99m, F-18 or I-123 labeled agent for ${\beta}-amyloid$ imaging agent.

A Case of Seizures after Zolpidem Withdrawal (고용량 졸피뎀 복용 중단 이후 발생한 경련발작 1례)

  • Moon, Hyung Jun;Lee, Jung Won;Yoo, Byeong Dae
    • Journal of The Korean Society of Clinical Toxicology
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    • v.11 no.2
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    • pp.127-129
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    • 2013
  • The imidazopyridine, zolpidem, a non-benzodiazepine hypnotic drug, is widely-prescribed for insomnia. It is regarded as a good alternative to benzodiazepine because of the reduced possibility for abuse and development of dependence. However, more recently, due to the reduced possibility for abuse and development of dependence, it is regarded as a good alternative to benzodiazepine. adverse effects of zolpidem have been recognized. The objective of this report is to provide information on the potential for occurrence of benzodiazepine-like withdrawal seizure in patients who chronically take zolpidem continually. We present and discuss a case of seizure after sudden interruption of the protracted use of an abusively high dose of zolpidem. Zolpidem may not be the ideal drug for longterm pharmacotherapeutic management of insomnia. Clinicians should administer zolpidem at a low-dose for a short period of time for prevention of drug abuse and dependence and the potential for occurrence of benzodiazepine- like withdrawal seizure.

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