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BENZISOXAZOLE-3-CARBOXAMIDE AND BENZISOTHIAZOLE-3-CARBOXAMIDE AS POTENTIAL ATYPICAL ANTIPSYCHOTIC AGENTS

A series of benzisoxazole- and benzisothiazole-3-carboxamides has been prepared and tested for potential antipsychotic activity. In general, the compounds showed an affinity for dopamine D-2 and serotonin 5HT(2A) and 5HT(1A) receptors. Several Members of this series have demonstrated activity in animal models predictive of potential antipsychotic activity. In addition, compounds 18, 19, 22, 27, 28, 43, and 44 have also shown a potential for reduced EPS liability as suggested by the ratio of activity seen in mesolimbic-mediated vs nigrostriatal-mediated behavioral assays.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

24-Sep-21 News The Best Chemistry compound: C9H16O4

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Regioselective synthesis of 4,5,6,7-tetrahydro-2,1-benzisoxazole

The title benzisoxazole (3) is prepared isomerically pure by condensation of 2-(diethoxymethyl)cyclohexanone with hydroxylamine hydrochloride.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

23-Sep News Can You Really Do Chemisty Experiments About C9H16O4

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Formation of 2-sulphamoylacetylphenol from zonisamide under aerobic conditions in rat liver microsomes

1. The antiepileptic agent zonisamide, 1,2-benzisoxazole-3-methanesulphonamide, was metabolized reductively to 2-sulphamoyl-acetylphenol (SMAP) not only under anaerobic conditions but also under aerobic conditions in liver microsomes of rat pretreated with phenobarbital or dexamethasone. 2. NADPH was required for the formation of SMAP from zonisamide under aerobic conditions. In addition, the reductive metabolism of zonisamide under these conditions was substantially inhibited by carbon monoxide, ketoconazole, and cimetidine, known inhibitors of cytochrome P450. 3. The formation of SMAP under aerobic conditions in liver microsomes was increased by pretreatment of rat with triacetyloleandomycin (TAO) and was increased by the treatment of the microsomes with ferricyanide. 4. These results imply that zonisamide is metabolized reductively to SMAP by a cytochrome P450 belonging to the 3A subfamily under aerobic conditions as well as anaerobic conditions.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

9/17 News Extended knowledge of C9H16O4

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Medium Effects in Biologically Related Catalysis

Enzymes catalyze chemical reaction in aqueous media, but their active sites significantly differ in properties from water. In this chapter, the work on selected chemical reactions with important biological roles is reviewed to assess our current understanding of the effect of the environment that surrounds the reactive species. In particular, simple medium effects such as the ones provided by organic solvents, ionic liquids, and simple micelles are focused on. The findings that led to the computational design of enzymes that catalyze the Kemp elimination, a prototypical proton transfer reaction that has fascinated researchers for more than a century, are discussed.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

14 Sep 2021 News Never Underestimate The Influence Of C9H16O4

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A CONVENIENT METHOD FOR THE PRODUCTION OF ORTHO-AMINO AND N-ALKYLAMINOBENZOPHENONES

ortho-Amino and N-alkylaminobenzophenones 3 have been prepared in good yields by the reductive cleavage of 2, 1-benzisoxazole and its salts with Zn-AlCl3.6H2O/THF system.

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Benzisoxazole – Wikipedia,
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10/9/2021 News Interesting scientific research on C9H16O4

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The effects of pH, buffer concentration and temperature on conversion rate of potassium oxime-O-sulfonates of 2-hydroxybenzaldehyde and 2-hydroxyacetophenone to benzisoxazole or 2-methylbenzoxazole, respectively, were examined. The mechanisms of both reactions have been proposed.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

9 Sep 2021 News Discover the magic of the C9H16O4

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Purpose: The antiepileptic effects of zonisamide (ZNS) have been well documented experimentally and clinically. The purpose of this study was to examine whether ZNS reduces cerebral damage after transient focal ischemia in rats. Methods: Ischemia was induced by a transient occlusion of the left middle cerebral artery (MCA) with a 3-0 nylon monofilament for 90 min. Neurological evaluation was performed by measuring the event of neurological deficit of the contralateral forepaw and hindpaw at 10 min and 1 day after MCA occlusion (MCAo). Brain infarct size was determined by measuring triphenyltetrazonium chloride-negative stained area of the serial brain sections 1 day after MCAo. Results: The pre-or postischemic treatment with ZNS [(10-100 mg/kg p.o.), 30 min before and 4 h after or 15 min and 4 h after the occlusion] markedly reduced cerebral damage in the ipsilateral hemisphere and the neurological deficit induced by transient ischemia. The reducing effect on the damage was observed in the cortical and subcortical regions. Preischemic treatment with carbamazepine (CBZ 60 mg/kg p.o. twice 30 min before and 4 h after MCAo) tended to reduce the cerebral damage and neurological deficit, but the lower dose (20 mg/kg p.o. twice) did not. Valproate (VPA 1,000 mg/kg p.o. twice) also had no effect. Conclusions: ZNS at the anticonvulsant dose, unlike CBZ and VPA, ameliorated the brain infarction and the event of neurological deficit after transient focal cerebral ischemia. These data suggest that ZNS has therapeutic potential in protecting against ischemic cerebral damage, such as stroke.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Decrypt The Mystery Of 123-99-9

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Photoexcited o-nitro chromophore in o-nitrobenzylic systems has led to the design and development of many useful photochromic systems such as photolabile protecting groups, photoresists, for controlled release of bioactive compounds, as well as efficient photosynthons giving direct access to many important molecular systems that are otherwise difficult to obtain. This brief review cites a few examples showing the photochemistry of 2-nitrodiphenylalkanes and alkenes, which find useful in the synthesis of 2,1-benzisoxazole derivatives, dibenzo(c,f)-(1,2)diazepin-N-oxides and N,N-dioxides, acridones, isatogens etc., that are present in many pharmaceutical drugs.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

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Zonisamide is increasingly used in pediatric neurology but there are no experimental data for immature animals. Zonisamide (12.5-100 mg/kg i.p.) was tested against pentetrazol-induced seizures in 7-, 12-, 18-, 25- and 90-day-old rats. Minimal clonic seizures were not suppressed by zonisamide. Selective suppression of tonic phase of generalized tonic-clonic seizures was demonstrated in all age groups. This effect indicates possible action of zonisamide against generalized tonic-clonic seizures during brain maturation. (C) 2010 Published by Elsevier B.V.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

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Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. 123-99-9, Name is Water-soluble azelaic acid, molecular formula is C9H16O4, Quality Control of Water-soluble azelaic acid, belongs to benzisoxazole compound, is a common compound. In a patnet, author is NAKASA, H, once mentioned the new application about 123-99-9.

The reductive metabolism of 1,2-benzisoxazole-3-methanesulfonamide (zonisamide) to 2-sulfamoylacetylphenol (SMAP) was observed in liver microsomes from female rats, as well as male rats, but the SMAP-producing activity in female rats was 4-fold lower than that found in male rats. In addition, the reductive metabolism of zonisamide in liver microsomes was induced by the treatment of male rats with phenobarbital. However, the SMAP-producing activity did not correlate positively with the amounts of P-450 2B1 and P-450 2C11 immunochemically determined. In contrast, the reductive metabolism of zonisamide was also found to be induced by the pretreatment of male rats with pregnenolone 16alpha-carbonitrile, triacetyloleandomycin, and dexamethasone. Furthermore, the SMAP-producing activity correlated highly with the amount of P-450 cross-reactive with antihuman P-450 3A4 antibody, suggesting that P-450 3A1/2 may function in the reductive metabolism of zonisamide. In addition, the P-450 PCNa (3A2) exhibited the SMAP-producing activity in a reconstituted system. The antihuman P-450 3A4 antibody inhibited markedly the formation of SMAP from zonisamide in male rat liver microsomes. These results indicate that cytochrome(s) P-450 belonging to P-450 3A subfamily may be predominantly responsible for the reductive metabolism of zonisamide in rat liver microsomes.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics