Biochemical and pharmacological characteristics of a newly synthesized H+-K+ATPase inhibitor, YJA20379-1, 2-amino-4,5-dihydro-8-phenylimidazole [2,1-b]thiazolo[5,4-g]benzothiazole

Sohn, Sang-Kwon; Chang, Man-Sik; Choi, Woojin; Kim, Kyu‐Bong; Woo, Tae-Wook; Lee, Seok-Bong; Chung, Yong-Joon

doi:10.1139/y99-026

Cited by 4 publications

(2 citation statements)

References 27 publications

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“…Among nitrogen-containing heterocyclic compounds, thiazoles are of immense interest to medicinal and industrial chemists due to their diverse biological activities such as antiglutamate, antiparkinson [32], antimicrobial [33], anthelmintic, anti-in�ammatory [34], antihyperlipidemic, antihypertension and antioxidant properties as well as inhibition of enzymes such as acetylcholine esterase [35], aldose reductase [36], lipoxygenase [37], ATPase [38], and HCV helicase [39]. In general, heterocyclic systems encompassing pyran unit have found application as pharmaceuticals, agrochemicals, and veterinary products [40].…”

Section: Introductionmentioning

confidence: 99%

NiO Nanoparticles: An Efficient Catalyst for the Multicomponent One‐Pot Synthesis of Novel Spiro and Condensed Indole Derivatives

Sachdeva

Dwivedi

Bhattacharjee

et al. 2012

Journal of Chemistry

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An efficient catalytic protocol for the synthesis of novel spiro[indoline-3,4′-pyrano[2,3-c]thiazole]carbonitriles and condensed thiazolo[5′′,4′′:5′,6′]pyrano[4′,3′:3,4]furo[2,3-b]indole derivatives is developed in a one-pot three-component approach involving substituted 1H-indole-2,3-diones, activated methylene reagent, and 2-thioxo-4-thiazolidinone under conventional heating and microwave irradiation. This paper describes the use of NiO nanoparticles as catalyst for the synthesis of novel spiro and condensed indole derivatives by Knoevenagel condensation followed by Michael addition. The advantageous features of this methodology are operational simplicity, high yield processing, and easy handling. The particle size of NiO nanoparticle was determined by XRD. After reaction course, NiO nanoparticles can be recycled and reused without any apparent loss of activity.

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Section: Introductionmentioning

confidence: 99%

NiO Nanoparticles: An Efficient Catalyst for the Multicomponent One‐Pot Synthesis of Novel Spiro and Condensed Indole Derivatives

Sachdeva

Dwivedi

Bhattacharjee

et al. 2012

Journal of Chemistry

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“…2-Amino-4,5-dihydro-8-phenylimidazo[2,1-b]thiazolo [4,5-g]benzothiazole (YJA 20379-1) has potent antiulcer activities in several ulcer models in rats and is demonstrated to be a potent proton pump inhibitor of which IC 50 of H + /K-ATPase activity is 24 µmol/l [1]. The inhibitory action of the drug on Helicobacter pylori growth in vitro has been reported [2].…”

Section: Introductionmentioning

confidence: 99%

General Pharmacological Properties of YJA 20379-1, a Novel Proton Pump Inhibitor with Antiulcer Activities

Lee

Cho

Cheon

et al. 2011

Arzneimittelforschung

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The general pharmacological properties of YJA 20379-1 (2-amino-4,5-dihydro-8-phenylimidazo[2,1-b]thiazolo[4,5-g]benzo thi azole), a novel proton pump inhibitor with antiulcer activities, were investigated in mice, rats, guinea pig and rabbits. YJA 20379-1 at oral doses of 50, 100 and 200 mg/kg did not affect the general behaviour, hexobarbital hypnosis, motor coordination and body temperature in mice. The drug does not have analgesic and anticonvulsant action at 200 mg/kg p.o. The locomotor activity was not affected at 100 mg/kg p.o., but at 200 mg/kg, the activity was suppressed. YJA 20379-1 (at 2 x 10(-4) g/ml) did neither produce any contraction nor relaxation of isolated organs such as rat fundus, rat uterus, guinea pig ileum and guinea pig vas deferens, and the drug did not antagonize the contractile response to several spasmogens, such as histamine, acetylcholine, serotonin and oxytocin, and the drug up to 200 mg/kg p.o. did not affect pupil size of mice. The intestinal propulsion in mice was not affected up to 200 mg/kg p.o. The gastric emptying in rats was not affected at 100 mg/kg p.o., even if retardation in gastric emptying occurred at 200 mg/kg. YJA 20379-1 did not show anti-inflammatory action nor did it affect urinary excretion up to 200 mg/kg p.o. From these results, it is suggested that YJA 20379-1 at the high dose of 100 mg/kg p.o. may not exert any adverse effects.

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Synthesis of 2-arylbenzimidazoles and 2-arylbenzothiazoles in both room temperature and microwave condition catalyzed by hexamethylenetetramine–bromine complex

Khosravi

Kazemi²

2012

Chinese Chemical Letters

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Biochemical and pharmacological characteristics of a newly synthesized H⁺-K⁺ATPase inhibitor, YJA20379-1, 2-amino-4,5-dihydro-8-phenylimidazole [2,1-b]thiazolo[5,4-g]benzothiazole

Cited by 4 publications

References 27 publications

NiO Nanoparticles: An Efficient Catalyst for the Multicomponent One‐Pot Synthesis of Novel Spiro and Condensed Indole Derivatives

NiO Nanoparticles: An Efficient Catalyst for the Multicomponent One‐Pot Synthesis of Novel Spiro and Condensed Indole Derivatives

General Pharmacological Properties of YJA 20379-1, a Novel Proton Pump Inhibitor with Antiulcer Activities

Synthesis of 2-arylbenzimidazoles and 2-arylbenzothiazoles in both room temperature and microwave condition catalyzed by hexamethylenetetramine–bromine complex

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