FR145715, a novel histamine H2 receptor antagonist, with specific anti-Helicobacter pylori activities

Ishikawa, H.; Ito, Hiroya; Higaki, Masahide; Higaki, Mika; Matsumoto, Yoshimi; Kamimura, Toshiaki; Katsura, Yousuke; Tomishi, Tetsuo; Inoue, Yoshikazu; Takasugi, Hisashi; Tomoi, Masaaki; Krakowka, Steven; Yoshida, Keizo

doi:10.1016/s0014-2999(99)00466-5

Cited by 8 publications

(7 citation statements)

References 20 publications

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“…Regarding the mode of anti- H. pylori action, both compounds ( 28 and 36 ) showed bactericidal effect (data to be published elsewhere). We selected 28 and 36 as candidates for further pharmacological evaluation, and the results on one of them, 28 (FR145175), have been reported in a journal of pharmacology 5 Antimicrobial Activity of 28 , 36 , and the Reference Compounds against Various Organisms MIC (μg/mL) (range)organisms ( n ) 28 36 bismuth salicylatemetronidazoleamoxicillin H. pylori (10) 0.32 0.017 8.7 5.4 0.021 (0.2−0.39) (0.0030−0.05) (1.56−25) (0.0063−0.1) C. jejuni (8) >100 20.5 7.4 30 2.2 (12.5−50) (6.25−12.5) (0.78−100) (0.39−6.25) C. difficile (4) >100 >100 50 0.2 0.28 (0.1−0.39) (0.1−0.78) C. perfrigens (6) >100 >100 >100 1.75 0.027 (0.78−3.13) (0.025−0.05) B. fragilis (10) >100 >100 50 0.59 2.1 (0.39−0.78) (0.2−12.5) N. gonorrhea s (10) >100 >100 4.7 >100 7.7 (3.13−6.25) (0.39−100) N. meningitidis (10) >100 >100 12.5 >100 0.056 (3.13−100) (0.05−0.1) …”

Section: Resultsmentioning

confidence: 99%

Anti-HelicobacterpyloriAgents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and Some Structurally Rigid Derivatives

et al. 2000

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In order to find a new class of anti-Helicobacter pylori (H. pylori) agents, a series of 4-[(3-acetamido)phenyl]-2-(substituted guanidino)thiazoles and some structurally rigid analoges were synthesized and evaluated for antimicrobial activity against H. pylori. Among the compounds obtained, high anti-H. pyrori activities were observed in benzyl derivative 34 (MIC = 0.025 microg/mL) and phenethyl derivatives 35 and 36 (MIC = 0.037 microg/mL and 0.017 microg/mL). Though alkyl derivatives generally showed lower activity, the 2-methoxyethyl derivative 28 preserved significant activity (MIC = 0.32 microg/mL) and also exhibited more potent gastric antisecretory activity than ranitidine. Structural restriction by bridging between the thiazole and the phenyl rings with an alkyl chain did not improve the activity in this series.

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Section: Resultsmentioning

confidence: 99%

Anti-HelicobacterpyloriAgents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and Some Structurally Rigid Derivatives

et al. 2000

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“…In addition, FR145715 exhibits specific anti-microbial activities against strains of H. pylori with a mean minimal MIC value of 0.32 µg/mL [274]. …”

Section: Fr145715mentioning

confidence: 99%

Helicobacter pylori Current Chemotherapy and New Targets for Drug Design

Williamson¹

2001

CPD

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Helicobacter pylori infection is a major cause of many diseases of the gastrointestinal tract, including gastritis, non-ulcer dyspepsia, peptic ulcer disease, and gastric cancers. It is estimated that more than half of the human race is affected by this organism. Although effective treatments are available which will eliminate the organism in about 90 percent; of cases in developed countries, the pandemic occurrence of Helicobacter pylori infection coupled with its ability to develop resistance to our current arsenal of antimicrobial regimens and subsequently reinfect patients makes the pathogenic potential of this microorganism a major global health concern. Provided is a review of the current and evolving therapeutic regimens used in the eradication of Helicobacter pylori, the difficulties associated with in vitro drug screening, as well as potentially new therapeutic targets. In addition, the discovery, the unique physiology, biochemistry, and pathogenicity of this remarkable microorganism is examined.

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“…The target for neuroprotective agents for neurocognitive repair and inhibition of neuron-function damage developed according to cognitive deficits across multiple domains in substantial intellectual impairment (8,9). In addition, although the theoretic mechanism of anti-histamine agents in cranial nerve involvement are well understood, treatment of this type of disease remains limited and lacks preclinical investigation (10)(11)(12). Therefore, investing the mechanism of anti-histamine in the treatment of cranial nerve involvement is important to better explain therapeutic effects according to observations.…”

Section: Introductionmentioning

confidence: 99%

Neuroprotective effect of lurasidone via antagonist activities on histamine in a rat model of cranial nerve involvement

et al. 2018

Mol Med Report

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Cranial nerve involvement frequently involves neuron damage and often leads to psychiatric disorder caused by multiple inducements. Lurasidone is a novel antipsychotic agent approved for the treatment of cranial nerve involvement and a number of mental health conditions in several countries. In the present study, the neuroprotective effect of lurasidone by antagonist activities on histamine was investigated in a rat model of cranial nerve involvement. The antagonist activities of lurasidone on serotonin 5‑HT7, serotonin 5‑HT2A, serotonin 5‑HT1A and serotonin 5‑HT6 were analyzed, and the preclinical therapeutic effects of lurasidone were examined in a rat model of cranial nerve involvement. The safety, maximum tolerated dose (MTD) and preliminary antitumor activity of lurasidone were also assessed in the cranial nerve involvement model. The therapeutic dose of lurasidone was 0.32 mg once daily, administered continuously in 14‑day cycles. The results of the present study found that the preclinical prescriptions induced positive behavioral responses following treatment with lurasidone. The MTD was identified as a once daily administration of 0.32 mg lurasidone. Long‑term treatment with lurasidone for cranial nerve involvement was shown to improve the therapeutic effects and reduce anxiety in the experimental rats. In addition, treatment with lurasidone did not affect body weight. The expression of the language competence protein, Forkhead‑BOX P2, was increased, and the levels of neuroprotective SxIP motif and microtubule end‑binding protein were increased in the hippocampal cells of rats with cranial nerve involvement treated with lurasidone. Lurasidone therapy reinforced memory capability and decreased anxiety. Taken together, lurasidone treatment appeared to protect against language disturbances associated with negative and cognitive impairment in the rat model of cranial nerve involvement, providing a basis for its use in the clinical treatment of patients with cranial nerve involvement.

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FR145715, a novel histamine H2 receptor antagonist, with specific anti-Helicobacter pylori activities

Cited by 8 publications

References 20 publications

Anti-HelicobacterpyloriAgents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and Some Structurally Rigid Derivatives

Anti-HelicobacterpyloriAgents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and Some Structurally Rigid Derivatives

Helicobacter pylori Current Chemotherapy and New Targets for Drug Design

Neuroprotective effect of lurasidone via antagonist activities on histamine in a rat model of cranial nerve involvement

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