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Selective inhibitors

In case poor overall enantioselectivity is observed owing to the presence of two competing enzymes with different enantioselectivities, one of the most straightfor- [Pg.207]


CgH,3BrN202. A soil-acting herbicide. White crystalline solid, m.p. 158-159" C. It is a non-selective inhibitor of photosynthesis used for weed control In citrus and cane fruit plantations. It is relatively non-toxic to animal life. [Pg.67]

D. M. Byrd and W. A. Carter iu W. A. Carter, ed.. Selective Inhibitors of Viral Function, Chemical Rubber Co. Press, Qeveland, Ohio, 1973, p. 329. [Pg.507]

A large number of a-hydroxybenzylbenzimidazole [50-97-5] (HBB, 39), C24H22N2O, derivatives has been prepared and extensively studied as selective inhibitors of the RNA containing enterovimses (91). Although none of these derivatives have shown any antiviral activity in animals, l,2-bis(5-methoxy-2-benzimidazol-2-yl)-l,2-ethanediol [16656-27-2] (40), C2gH2gN404, was found to be active against an experimentally induced rhino vims infection in chimpanzees (92). However, the in vivo antiviral efficacy was accompanied by significant toxicity. [Pg.309]

MAO is known to occur in at least two forms, MAO A and MAO B, based on substrate selectivity, inhibition by various dmgs, and cloning experiments. Clorgyline [17780-72-2] is a specific inhibitor of MAO A, which displays a substrate specificity for NE and serotonin. Deprenyl [2323-36-6] is a selective inhibitor of MAO B, and displays a substrate preference for P-phenylethylamine and benzyl amine. Dopamine and tyramine are substrates for both enzymes. [Pg.358]

How do the mutations identified by phage display improve binding specificity There is as yet no direct stmctural information on the phage-selected inhibitors however they can be modeled using data from the crystal structures of other Kunitz domains bound to serine proteinases. These studies lead to the conclusion that the mutations identified by phage display improve binding specificity by maximizing complementarity between the... [Pg.362]

CDP840 is a selective inhibitor of the PDE-IV isoenzyme and interest in the compound arises from its potential application as an antiasthmatic agent. Chemists at Merck Co. used the asymmetric epoxidation reaction to set the stereochemistry of the carbon framework and subsequently removed the newly established C-O bonds." Epoxidation of the trisubstituted olefin 51 provided the desired epoxide in 89% ee and in 58% yield. Reduction of both C-O bonds was then accomplished to provide CDP840. [Pg.41]

LY311727 is an indole acetic acid based selective inhibitor of human non-pancreatic secretory phospholipase A2 (hnpsPLA2) under development by Lilly as a potential treatment for sepsis. The synthesis of LY311727 involved a Nenitzescu indolization reaction as a key step. The Nenitzescu condensation of quinone 4 with the p-aminoacrylate 39 was carried out in CH3NO2 to provide the desired 5-hydroxylindole 40 in 83% yield. Protection of the 5-hydroxyl moiety in indole 40 was accomplished in H2O under phase transfer conditions in 80% yield. Lithium aluminum hydride mediated reduction of the ester functional group in 41 provided the alcohol 42 in 78% yield. [Pg.150]

Selection of Corrosion Inhibitors. When selecting inhibitors for use, it is always important to consider the following useful suggestions ... [Pg.1330]

Van Beeren HC, Jong WMC, Kaptein E et al (2003) Dronedarone acts as a selective inhibitor of 3,5,3 -triiodothyronine binding to thyroid hormone receptor-a. in vitro and in vivo evidence. Endocrinology 144 552-558... [Pg.102]

Schumacher HR Jr (2005) Febuxostat a non-purine, selective inhibitor of xanthine oxidase for the management of hyperaricaemia in patients with gout. Expert Opin Investig Drugs 14 893-903... [Pg.139]

A number of rationally designed MMP inhibitors have shown some promise in the treatment of pathologies, which MMPs are suspected to be involved in. However, most of these, such as Marimastat (BB-2516), a broad spectrum MMP inhibitor, or trocade (Ro 32-3555), an MMP-1 selective inhibitor, have performed poorly in clinical trials. The failure of Marimastat was partially responsible for the folding of British Biotech, which developed it. The failure of... [Pg.746]

Ubiquitous mitochondrial monoamine oxidase [monoamine oxygen oxidoreductase (deaminating) (flavin-containing) EC 1.4.3.4 MAO] exists in two forms, namely type A and type B [ monoamine oxidase (MAO) A and B]. They are responsible for oxidative deamination of primary, secondary, and tertiary amines, including neurotransmitters, adrenaline, noradrenaline, dopamine (DA), and serotonin and vasoactive amines, such as tyramine and phenylethylamine. Their nonselec-tive and selective inhibitors ( selective MAO-A and -B inhibitors) are employed for the treatment of depressive illness and Parkinson s disease (PD). [Pg.783]

Transporter (gene) Distribution Km (pmol/l) Major function Selective inhibitor... [Pg.837]

Transporter Moderately selective inhibitors in clinical use Highly selective inhibitors (>50-fold) Nonselective inhibitors... [Pg.841]

Glucocorticoids increase the risk of gastrointestinal complications caused by NSAEDs. Considerable caution is necessary when using NSAIDs in patients with severe liver and kidney damage and they should not be combined with coumarines. Owing to the limited experience obtained, these precautions and contraindications also apply to COX-2-selective inhibitors. [Pg.874]

Due to the short period of clinical use, the interaction profile of COX-2-selective inhibitors cannot be entirely described at the present time. [Pg.874]

Ibuprofen is the most thoroughly researched 2-ary lpropionic acid. It is a relatively weak, non-selective inhibitor of COX. In epidemiological studies, ibuprofen compared to all other conventional NSAIDs, has the lowest relative risk of causing severe gastrointestinal side effects. Because of this, ibuprofen is the most frequently used OTC ( over the counter , sale available without prescription) analgesic. Ibuprofen is highly bound to plasma proteins and has a relatively short elimination half-life ( 2 h). It is mainly glucuronidated to inactive metabolites that are eliminated via the kidney. [Pg.875]

The indications for these agents are in principle identical to those of the non-selective NSAIDs although the substances have not yet received approval for the whole spectrum of indications of the conventional NSAIDs. Because they lack COX-1-inhibiting properties, COX-2-selective inhibitors show fewer side effects than conventional NSAIDs. However, they are not free of side effects because COX-2 has physiological functions that are blocked by the COX-2 inhibitors. The most frequently observed side effects are infections of the upper respiratory tract, diarrhoea, dyspepsia, abdominal discomfort and headache. Peripheral oedema is as frequent as with conventional NSAIDs. The frequency of gastrointestinal complications is approximately half that observed with conventional NSAIDs. [Pg.875]

The PDE3 inhibitor, cilostazol, has been used as an antithrombotic agent and is currently being used in patients being treated for intermittent claudication. Cilostazol is also used for the prevention of restenosis after treatments such as angioplasty. Another PDE3 selective inhibitor, milrinone, has been used in the treatment of congestive heart failure. Milrinone also has been shown to increase the conductance of the CFTR transporter in vitro. [Pg.965]

Dipyridamole is a PDE5/PDE6 selective inhibitor that is used widely in conjunction with aspirin to reduce clotting and prevent stroke. More recent studies with a fixed combination of these two drugs (Aggrenox) has been shown in the recent European Stroke Prevention Study 2 to be of greatly added benefit over aspirin alone for prevention of recurrent stroke. [Pg.965]

Dynamic kinetic resolution of a-alkyl-P-keto ester was conducted successfully using biocatalysts. For example, baker s yeast gave selectively syn(2R, 3S)-product [29a] and the selectivity was enhanced by using selective inhibitor [29b] or heat treatment of the yeast [29c]. Organic solvent was used for stereochemical control of G. candidum [29d]. Plant cell cultures were used for reduction of 2-methyl-3-oxobu-tanoate and afforded antialcohol with Marchantia [29e,f] and syn-isomer with Glycine max [29f]. [Pg.221]

Neyts J (2006) Selective inhibitors of hepatitis C vims replication. Antiviral Res 71 363-371... [Pg.49]


See other pages where Selective inhibitors is mentioned: [Pg.113]    [Pg.445]    [Pg.515]    [Pg.257]    [Pg.309]    [Pg.315]    [Pg.318]    [Pg.538]    [Pg.35]    [Pg.123]    [Pg.165]    [Pg.406]    [Pg.466]    [Pg.693]    [Pg.744]    [Pg.784]    [Pg.872]    [Pg.874]    [Pg.889]    [Pg.975]    [Pg.1004]    [Pg.207]    [Pg.29]    [Pg.29]    [Pg.83]    [Pg.133]    [Pg.144]   
See also in sourсe #XX -- [ Pg.207 ]

See also in sourсe #XX -- [ Pg.41 ]




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5-HT-selective reuptake inhibitors

A Selective serotonin re-uptake inhibitors (

Allosteric sites, inhibitor selectivity

And selective serotonin receptor inhibitors

Antidepressants Monoamine oxidase inhibitors Serotonin-selective

Antidepressants selective noradrenaline reuptake inhibitor

Antidepressants selective norepinephrine reuptake inhibitors

Antidepressants selective serotonin inhibitors

Antidepressants selective serotonin reuptake inhibitors

Antipsychotic drugs selective serotonin reuptake inhibitors with

Anxiety selective serotonin reuptake inhibitors

Attention deficit disorder selective norepinephrine reuptake inhibitors

COX2 selective inhibitors

Chemical inhibitors, selection

Corrosion inhibitors selection

Cyclooxygenase-2 Selective Inhibitors

Cyclooxygenase-2 inhibitors selectivity

Dasatinib inhibitor selectivity

Depression selective noradrenaline reuptake inhibitors

Depression selective serotonin reuptake inhibitors

Depressive disorders selective serotonin reuptake inhibitors

Development of Selective COX-2 Inhibitors

Dihydrofolate reductase inhibitors selective toxicity

Dopamine- selective reuptake inhibitors

EGFR (epidermal growth factor inhibitor selectivity

ErbB selective inhibitors

Gefitinib inhibitor selectivity

Hormonal) Selective serotonin re-uptake inhibitors (

Identification of Selective Inhibitors

Imatinib inhibitor selectivity

Inhibitors Selectivity

Inhibitors norepinephrine-selective contrasted

Inhibitors selection

Inhibitors selection

Inhibitors target selection

Insomnia selective serotonin reuptake inhibitors

Lapatinib inhibitor selectivity

Look up the names of both individual drugs and their drug groups to access full information Selective serotonin re-uptake inhibitors (

Medications selective serotonin reuptake inhibitors

Metabolic inhibitor selectivity

Mirtazapine selective serotonin reuptake inhibitors with

Monoamine oxidase inhibitors selective

Monoamine oxidase inhibitors selective irreversible

NSAIDs) Selective serotonin re-uptake inhibitors (

Nausea selective serotonin receptor inhibitors

Nefazodone selective serotonin reuptake inhibitors with

Non-selective Monoamine Reuptake Inhibitor

Nonsteroidal anti-inflammatory drugs selective cyclooxygenase-2 inhibitors

Obsessive-compulsive disorder selective serotonin reuptake inhibitors

PI3K-selective inhibitors

Panic disorder selective serotonin reuptake inhibitors

Phosphodiesterase inhibitors selective

Posttraumatic stress disorder selective serotonin reuptake inhibitors

Protein kinase family inhibitor selectivity

Protein synthesis inhibitors selective action

Protein target isoform selective inhibitor

Reboxetine selective serotonin reuptake inhibitors with

Schizophrenia Selective serotonin reuptake inhibitors

Selected serotonin reuptake inhibitors

Selection of Inhibitor

Selective Biochemical Inhibitors

Selective COX-2 inhibitors

Selective Inhibitors of Cyclooxygenase-2 (COX

Selective Serotonin-Norepinephrine Reuptake Inhibitors

Selective Serotonine Reuptake Inhibitors

Selective cholesterol absorption inhibitors

Selective dissolving solubility inhibitors

Selective noradrenaline reuptake inhibitors

Selective noradrenergic reuptake inhibitors

Selective norepinephrine reuptake inhibitors

Selective norepinephrine reuptake inhibitors action

Selective norepinephrine reuptake inhibitors depression

Selective norepinephrine reuptake inhibitors efficacy

Selective norepinephrine reuptake inhibitors response

Selective norepinephrine reuptake inhibitors side effects

Selective pyrrolidine inhibitors

Selective serotonin and norepinephrine reuptake inhibitors

Selective serotonin inhibitors

Selective serotonin re-uptake inhibitors

Selective serotonin re-uptake inhibitors SSRIs)

Selective serotonin receptor inhibitor (SSRI

Selective serotonin reuptake inhibitor behavioral

Selective serotonin reuptake inhibitor metabolic

Selective serotonin reuptake inhibitors

Selective serotonin reuptake inhibitors (SSRIs side effects

Selective serotonin reuptake inhibitors . See

Selective serotonin reuptake inhibitors Citalopram Fluoxetine

Selective serotonin reuptake inhibitors Fluvoxamine Paroxetine Sertraline

Selective serotonin reuptake inhibitors MAOIs

Selective serotonin reuptake inhibitors MDMA)

Selective serotonin reuptake inhibitors SSRIs)

Selective serotonin reuptake inhibitors about

Selective serotonin reuptake inhibitors action

Selective serotonin reuptake inhibitors administration

Selective serotonin reuptake inhibitors adverse effects

Selective serotonin reuptake inhibitors alprazolam

Selective serotonin reuptake inhibitors amphetamines

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Selective serotonin reuptake inhibitors and

Selective serotonin reuptake inhibitors anxiety disorders

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Selective serotonin reuptake inhibitors benzodiazepines

Selective serotonin reuptake inhibitors buspirone

Selective serotonin reuptake inhibitors characteristics

Selective serotonin reuptake inhibitors chemical structures

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Selective serotonin reuptake inhibitors citalopram

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Selective serotonin reuptake inhibitors clozapine

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Selective serotonin reuptake inhibitors depression from

Selective serotonin reuptake inhibitors discontinuation

Selective serotonin reuptake inhibitors discontinuation syndrome

Selective serotonin reuptake inhibitors dosing

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Selective serotonin reuptake inhibitors drug interactions

Selective serotonin reuptake inhibitors drug overdose

Selective serotonin reuptake inhibitors drug withdrawal

Selective serotonin reuptake inhibitors drugs

Selective serotonin reuptake inhibitors during pregnancy

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Selective serotonin reuptake inhibitors efficacy

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Selective serotonin reuptake inhibitors enhanced

Selective serotonin reuptake inhibitors escitalopram

Selective serotonin reuptake inhibitors extended-release

Selective serotonin reuptake inhibitors fluoxetine

Selective serotonin reuptake inhibitors fluvoxamine

Selective serotonin reuptake inhibitors gastrointestinal

Selective serotonin reuptake inhibitors general

Selective serotonin reuptake inhibitors haloperidol

Selective serotonin reuptake inhibitors hyponatremia with

Selective serotonin reuptake inhibitors immediate

Selective serotonin reuptake inhibitors in children

Selective serotonin reuptake inhibitors in children and adolescents

Selective serotonin reuptake inhibitors in obsessive-compulsive disorder

Selective serotonin reuptake inhibitors indications

Selective serotonin reuptake inhibitors interactions

Selective serotonin reuptake inhibitors labeling

Selective serotonin reuptake inhibitors lactation

Selective serotonin reuptake inhibitors limits

Selective serotonin reuptake inhibitors lithium

Selective serotonin reuptake inhibitors liver

Selective serotonin reuptake inhibitors long-term effects

Selective serotonin reuptake inhibitors mediation

Selective serotonin reuptake inhibitors metabolism

Selective serotonin reuptake inhibitors moclobemide

Selective serotonin reuptake inhibitors monoamine oxidase

Selective serotonin reuptake inhibitors mood disorders from

Selective serotonin reuptake inhibitors nefazodone

Selective serotonin reuptake inhibitors nervous system

Selective serotonin reuptake inhibitors olanzapine

Selective serotonin reuptake inhibitors overdose

Selective serotonin reuptake inhibitors overview

Selective serotonin reuptake inhibitors paroxetine

Selective serotonin reuptake inhibitors pharmacodynamic

Selective serotonin reuptake inhibitors pharmacokinetic

Selective serotonin reuptake inhibitors pharmacology

Selective serotonin reuptake inhibitors pindolol

Selective serotonin reuptake inhibitors risperidone

Selective serotonin reuptake inhibitors second-generation effects

Selective serotonin reuptake inhibitors selectivity differences

Selective serotonin reuptake inhibitors sertraline

Selective serotonin reuptake inhibitors structure

Selective serotonin reuptake inhibitors suicidality from

Selective serotonin reuptake inhibitors toxicity

Selective serotonin reuptake inhibitors tramadol

Selective serotonin reuptake inhibitors trazodone

Selective serotonin reuptake inhibitors tricyclic antidepressant interactions with

Selective serotonin reuptake inhibitors tricyclic antidepressants

Selective serotonin reuptake inhibitors triptans

Selective serotonin reuptake inhibitors venlafaxine

Selective serotonin reuptake inhibitors with stimulants

Selective serotonin reuptake inhibitors withdrawal

Selective serotonin reuptake inhibitors withdrawal from

Selective serotonin reuptake inhibitors, 128 sumatriptan

Selective serotonin uptake inhibitor

Selectivity Searching for Cathepsin K-Selective Inhibitors

Selectivity dioxygenase inhibitors

Selectivity uptake inhibitors

Serotonin reuptake inhibitors, selective dosage

Serotonin reuptake inhibitors, selective interaction with other drugs

Serotonin reuptake inhibitors, selective pharmacokinetics

Serotonin reuptake inhibitors, selective side effects

Social anxiety disorder selective serotonin reuptake inhibitors

Sorafenib inhibitor selectivity

Stainless steels inhibitor selection

Subject selective serotonin reuptake inhibitors

Subtype selective inhibitors

Sunitinib inhibitor selectivity

Synaptosomal Serotonin Uptake and Its Selective Inhibitors (SSRI)

Tissue-selective inhibitor

Trazodone selective serotonin reuptake inhibitors with

Tricyclic antidepressants selective serotonin reuptake inhibitor interactions

Vomiting selective serotonin receptor inhibitors

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