Synthesis of new derivatives of aryl-clonazepam via Suzuki Cross-coupling reaction

Salman, Mohammed; Abdul-Rida, Nabeel A.

doi:10.5155/eurjchem.7.2.152-155.1403

Cited by 3 publications

(2 citation statements)

References 26 publications

(26 reference statements)

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“…General procedure for the synthesis of the biaryl derivatives of clonazepam via Suzuki cross-coupling reaction to prepare 88, 89 compound according to the published articles. 16,30 Using these procedures, two compound were prepared and then many tests were performed to record and named as new compound related to benzodiazepine group 1 H-NMR 13 C-NMR, according to action was classified as long acting type.…”

Section: Discussionmentioning

confidence: 99%

“…General procedure was applied for the synthesis of the biaryl derivatives of clonazepam via Suzuki cross-coupling reaction to prepare 88, 89 compound according to the previous report. 16,30 Group 4: 4 mice were administrated with 88 compound (T 3 ) at same dose 30 mg/kg/ TID three times weekly for 4 weeks by stomach tube. Actually hypnotic effect of drugs was recorded in the first day of treatment with single dose of 50 mg/kg intra peritoneal (IP), and then analgesic state was recorded in the fourth day of first week only after given 30 mg/kg TID weekly.…”

Section: Methodsmentioning

confidence: 99%

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Study efficacy of new model of derivative clonazepam on hypnotic, sedative, blood hematology and evaluation reproductive function in male mice

Jassim

Hamad

Abed

et al. 2016

jcms

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Objectives This study includes the investigation of hypnotic and sedative effect of new generation agent synthesis from parent clonazepam and evaluates adverse effect on the reproductive system and an attempt to improve hypnotic effect and lower toxicity. Methods Sixteen male mice were randomly divided into four groups. The first day of treatment with single dose of 50 mg/kg intraperitoneal (IP) hypnotic effect then analgesic state was recorded in the 4th day of first week only after given 30 mg/kg orally, and then the experiment was persistent for 4 weeks to evaluate reproductive activity. Result The effect of diazepam on biochemical blood parameters showed that there is a slight increase in the WBC number of clonazepam group and 88 compound while there is no significant difference at the probability level 0.05 or 0.01, in 89 compound. RBC count in our result reveals a slight increase in 88 compound without significant difference than control. Our result shows significant increase in HB level in 88 compound to reach 13.18 ± 0.40 with no significant difference with control. PCV level reveals non-significant in all groups. Our results of the abnormal sperm morphology are shown after 4 weeks of the treatment. Conclusion clonazepam (T 1) and 88 compound (T 3) with high dose 50 mg/kg have good hypnotic action with complete muscle relaxant. In addition to all, agents have good analgesic effect but T 2 showed prominent result. Finally, clonazepam and its related agent 88, 89 compound reveal adverse effect on reproductive function but may be very slightly in 94 compound.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Study efficacy of new model of derivative clonazepam on hypnotic, sedative, blood hematology and evaluation reproductive function in male mice

Jassim

Hamad

Abed

et al. 2016

jcms

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A retrospective-prospective review of Suzuki–Miyaura reaction: From cross-coupling reaction to pharmaceutical industry applications

Farhang

Akbarzadeh²,

Rabbani³

et al. 2022

Polyhedron

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Characterization and Synthesis of New Model of Derivative Colonazepam and Clinical Trial to Inspection of Adverse Effect in Male Mice

Awni¹,

Aboktifa

Salman

et al. 2020

IOP Conf. Ser.: Earth Environ. Sci.

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Prepare new derivatives 5-(3-Fluoro-biphenyl-2-yl)-7-nitro-1,3-dihydro-benzo[e] [1,4]diazepin-2-ol (88)and 5-Nitro-2’-(7-nitro-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-5-yl)-biphenyl-3-carboxylic acid (89)compound from clonazepam and identified by spectrum of 13C-NMR and showed spectrum 1H-NMR . Clonazepam has massive adverse effect on prostate,lung,liver,kidney and spleen 3-new derivatives 5-(3-Fluoro-biphenyl-2-yl)-7-nitro-1,3-dihydro-benzo[e] [1,4]diazepin-2-ol (88) has limited effect and there is no clear changes in most organs studies.4-5-Nitro-2’-(7-nitro-2-oxo-2,3-dihydro-1Hbenzo[e][1,4]diazepin-5-yl)-biphenyl-3-carboxylic acid (89)compound has significant adverse effect but still less potent than clonazepam. OBJECTIVE To characterization and synthesis of new drugs related to clonazepam as well as to overcome massive adverse effect of clonazepam and increase the potency and half live of drugs.

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Synthesis of new derivatives of aryl-clonazepam via Suzuki Cross-coupling reaction

Cited by 3 publications

References 26 publications

Study efficacy of new model of derivative clonazepam on hypnotic, sedative, blood hematology and evaluation reproductive function in male mice

Study efficacy of new model of derivative clonazepam on hypnotic, sedative, blood hematology and evaluation reproductive function in male mice

A retrospective-prospective review of Suzuki–Miyaura reaction: From cross-coupling reaction to pharmaceutical industry applications

Characterization and Synthesis of New Model of Derivative Colonazepam and Clinical Trial to Inspection of Adverse Effect in Male Mice

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