• Archives of Pharmacal Research
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• 제13권4호
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• pp.342-346
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• 1990

Several new pyridine, pyridinethione, pyrazole [3, 4-b]-pyridine, pyrido [1, 2-a]-1, 3-thiazine and pyrido[1, 2-a] pyridine thione derivatives have be synthesised via the reactions of 2-methyl-3-ethoxycarbonyl-4-phenyl-5-cyano-1, 4, 5, 6-tetrahydro-pyridine-6-one 2 with different rfeagents. The structures of the newly synthesised derivatives were established on the basis of elemental analyses and spectral data studies.

• Bulletin of the Korean Chemical Society
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• 제23권12호
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• pp.1845-1847
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• 2002

• Archives of Pharmacal Research
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• 제22권2호
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• pp.194-201
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• 1999

The reaction of thiocyanoacetamide (1) with ${\alpha},{\beta}$-unsaturated ketones 2a,b resulted in the formation of the corresponding newly synthesized 1(H)-pyridinethione derivatives 3a,b. Compounds 3a,b were used as synthons for the preparation of 2-S-alkyl-, 2-S-acetamidopyridine, thieno[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives via a wide range of reactions with different reagents. The antimicrobial activity of some of the newly synthesized compounds was tested. Compounds 3a, 11a, 15a, and 19a,b were found to be the most active ones.

• Archives of Pharmacal Research
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• 제12권3호
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• pp.201-206
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• 1989

The reaction of acetoacetanilide (1) with the $\alpha$-cyanocinnamonitrile derivatives 2 yielded the Michael adducts 4 which could be converted into the pyrano [2, 3, -c] pyrazole derivatives 5 via their reaction with hydrazine hydrate. Cyclisation of 4 afforded the derivatives 10. The pyranopyrazoles 9 reacted with different activated nitrile derivatives (3a-c) to give the pyrano [2, 3-c] pyridine derivatives 13. 16 and 19 respectively. The biological activity of the synthesised heterocyclic derivatives was investigated and discussed.

• Bulletin of the Korean Chemical Society
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• 제22권11호
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• pp.1217-1223
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• 2001

A series of benzimidazole derivatives containing oxycyclic pyridine was prepared and evaluated for their gastric H+ /K+ -ATPase inhibitory activity. Several of the synthesized compound exhibited potent antisecretion in pylorus-ligated rats when administered intradoudenally. Their inhibitory activities were equivalent or comparable to omeprazole.

• Bulletin of the Korean Chemical Society
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• 제34권10호
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• pp.3073-3082
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• 2013

Designed and synthesized twenty-four 2,4-diaryl benzofuro[3,2-b]pyridine derivatives were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Various aryl groups such as phenyl, 2- or 3- furyl, 2- or 3-thienyl, and 2-pyridyl were substituted at 2- or 4- position of central pyridine. Compounds 8, 12, 13, and 14, with 2-furyl either at 2- or 4- position of central pyridine showed the significant topoisomerase II inhibitory activity at 100 ${\mu}M$.

• Archives of Pharmacal Research
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• 제18권1호
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• pp.27-30
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• 1995

The Hantzsh reaction of 7-hydroxy-8-methoxy-2-oxo-2H-benzopyran-6-carboxaldehyde (1) with ethyl acetoacetate and ammonia yields the dihydropyridine derivative 2 together with the pyridine derivative 3 and the eight membred ring derivative 4. Reaction of 1 with ethyl cyanoacetate and malononitrile gives the iminodicoumarin derivatives 5 and 6 respectiely. The latter compound was reacted with butan-2-one and acetophenone to produce the Michael adduct 71, b and the 2-aminopyridine derivatives 8a, b.

• Archives of Pharmacal Research
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• 제13권3호
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• pp.274-277
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• 1990

It has been found that $\alpha, \beta$-unsaturated nitrile derivatives 1-3 reached with S- methylisothiourea to give the prpone derivatives 4-6 respectively. Cyclisation of 4-6 using ethanolic hydrochloric acid afforded the pyridine derivatives 7-9 in good yields. On the other hand, the reactions of hydrazine hydrate and of phenylhydrazine with each of 7-9 gave the corresponding pyrazolopyridine derivatives 10-15. The structures of the newly synthesised derivatives were assigned on the basis of elemental analyses, IR and $^1H$-NMR spectral data studies.

• Archives of Pharmacal Research
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• 제22권5호
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• pp.496-501
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• 1999

The reaction of epi-androsterone with cyanoacetyl hydrazine (2) gave the hydrazone derivative 3. The reactivity of 3 towards chemical reagents was studied to give pyridine, thiazole and thiophene derivatives.

• Bulletin of the Korean Chemical Society
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• 제31권12호
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• pp.3760-3764
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• 2010

We screened 10,000 heterocyclic small molecules and identified a novel hit core skeleton of 3-(8-chloro-6-(trifluoromethyl) imidazo[1,2-a]pyridine-2-yl)phenyl acetate derivatives. It has been selected as a potential glucagon-like peptide 1 receptor (GLP-1R) activator and demonstrated its effects in increasing GLP-1 secretion, and thereby increasing the glucose responsiveness in both in vitro and pharmacology analyses. Further studies are currently underway to optimize the potency and selectivity of 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl acetate derivatives (hit compounds 2 and 8), and address their in vivo efficacy and therapeutic potential. These molecules may serve as useful evidence showing that compounds with a 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl acetate moiety are selective GLP-1R agonists, and have potential as anti-diabetic treatment agents.