By increasing our understanding of the physiological roles of the individual PDE isoforms, in parallel with the development of even more selective inhibitors of these enzymes, it is highly likely that better therapeutically active drugs will emerge. (biomedjournal.com)
Derivatives3
23 However, we have observed that the reaction of carbazole ( 1 ) with various car- boxylic acids ( 2 ) in the presence of TFAA and H 3 PO 4 a ff orded the corresponding N -acyl carbazoles ( 3 or A , path a) instead of C-acylated derivatives (path b, Scheme 1). (dokumen.tips)
A series of novel carbazole-based mono-/bis-thiocarbohydrazone derivatives were synthesized. (sioc-journal.cn)
Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Carbazole-Based Mono-/Bis-thiocarbohydrazone Derivatives[J]. Chinese Journal of Organic Chemistry, 2020, 40(1): 162-174. (sioc-journal.cn)
Alkaloids1
In addition to its natural occurrences in alkaloids isolated from plants, the carbazole framework has been found to be an integral part of many bioactive compounds and therefore (like indole) is considered as a privileged sca ff old in the area of new drug discovery. (dokumen.tips)
Hydroxylation1
This enzyme participates in benzoate degradation via hydroxylation and carbazole degradation. (wikipedia.org)
Indoles1
21 b While N-acylation of indoles has been studied well, only a few reports are available on the N-acylation of carbazoles. (dokumen.tips)
Compounds3
Novel host compounds consisting of carbazole and nitrile groups are disclosed. (justia.com)
Molecular docking results indicated that the target compounds 4d and 4a entered the active sites of Cdc25B and PTP1B enzymes, respectively, and thiocarbohydrazone and carbazole groups play the importent role of activity. (sioc-journal.cn)
Alk(en)yl trisulfides (R-SSS-R') are organosulfur compounds produced by crushed garlic and other Allium vegetables. (shengsci.com)
Derivative2
Our anticipation was further supported by an earlier report that the carbazole derivative B (Fig. 1) was found to be cytotoxic when tested against mouse mammary carcinoma FM3A cells. (dokumen.tips)
In this present study, the flexible and extra precision docking simulation were performed on twenty new carbazole tethered pyrrole derivative against InhA by using Glide v5.6. (thepharmajournal.com)
Characterization1
Fig. 1: Extent of characterization of the Rieske oxygenase enzyme superfamily. (nature.com)
Potent1
5,9-Dimethyldibenzo[c,g]carbazole (DMDBC), a potent mouse hepatocarcinogen, has been shown to induce a non-linear increase in mutant frequency in the liver of the transgenic MutaMouse. (shengsci.com)
Compound1
Carbazole Alkaloid is a plant-based compound that catalyzes natural healing and the curry leaf has this in spades. (com.bd)
Humans1
Inducers of Phase II enzymes, already consumed by humans as food additives, medicines or as constituents of vegetables, can prevent experimental carcinogenesis. (shengsci.com)
Mono1
Rieske oxygenases are examples of enzymes with the ability to perform precise mono- or dioxygenation reactions on a variety of substrates. (nature.com)
Reaction2
The enzyme o-pyrocatechuate decarboxylase (EC 4.1.1.46) catalyzes the chemical reaction 2,3-dihydroxybenzoate ⇌ {\displaystyle \rightleftharpoons } catechol + CO2 This enzyme belongs to the family of lyases, specifically the carboxy-lyases, which cleave carbon-carbon bonds. (wikipedia.org)
Based on these structures, substrate-bound structures, and mutagenesis experiments, we implicate specific residues in substrate positioning and the divergent reaction selectivity observed in these two enzymes. (nature.com)
Disruption2
TY - JOUR T1 - Targeted disruption of the gene encoding the classical nitroreductase enzyme in Salmonella typhimurium Ames test strains TA1535 and TA1538. (unboundmedicine.com)
In microorganisms, mercury toxicity results in protein denaturation, cell envelope disruption, inhibition of cell division and enzyme activities, destruction of nucleic acids, and transcription inhibition (Khan et al. (springeropen.com)
Class3
The systematic name of this enzyme class is 2,3-dihydroxybenzoate carboxy-lyase (catechol-forming). (wikipedia.org)
Understanding the structural features of Rieske oxygenases responsible for control over selectivity is essential to enable the development of this class of enzymes for biocatalytic applications. (nature.com)
In the Rieske oxygenase class, work to date has been conducted on a small sample of enzymes, specifically those that perform dioxygenation of aromatic rings. (nature.com)
Function2
SR13668 did not cause untoward hematology, clinical chemistry, or coagulation effects in dogs or monkeys with the exception of a modest, reversible increase in liver function enzymes in monkeys. (sri.com)
In the introduction to a recent paper in the journal Cell , "P7C3 Neuroprotective Chemicals Function by Activating the Rate-Limiting Enzyme in NAD Salvage", not a word about American football is mentioned. (promegaconnections.com)
Extent1
The Y1194F silencing mutation yielded an enzyme that could be activated to a similar extent as the wild type but with significantly slower activation kinetics, underlying the importance of this residue, which is conserved among different tyrosine kinase receptors. (ox.ac.uk)
Expression1
Their findings are supported by earlier reports that programmed expression of NAMPT enzyme protected mammalian cells from genotoxic stress (3) as well as extending life span of budding yeast (4). (promegaconnections.com)
Found2
Histidine is found in many proteins and enzymes and is required for the form and binding capabilities of haemoglobin. (tsijournals.com)
Furthermore, we found that the Ca 2+ effector enzyme protein kinase C (PKC) is essential for the Ca 2+ -dependent regulation of Rho GTPases during the transduction of guidance signals. (jneurosci.org)
Development2
Recent focus in the tubercular drug research is on the development of agents inhibiting the enzyme targets involved in potential role in the life cycle of the pathogen. (thepharmajournal.com)
SR13668 (2,10-dicarbethoxy-6-methoxy-5,7-dihydro-indolo-(2,3-b)carbazole), is a new candidate cancer chemopreventive agent under development. (sri.com)
Structure1
PDB codes represent the first structure determined for each enzyme. (nature.com)
Drug1
A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE) selectively in the brain. (biomedjournal.com)
Properties1
We anticipated that small molecules based on N -acyl carbazoles ( A , Fig. 1) might show anticancer properties. (dokumen.tips)
Role1
They play an integral role in metabolic processes and are essential micronutrients and cofactors of several enzymes, required in redox processes and stabilization of molecules through electrostatic interactions and regulation of osmotic pressure (Bruins et al. (springeropen.com)
Small1
The new and e ff ective yet simple strategies for the rapid access to small molecules of potential pharmacological interest are of great demand both in academic and industrial R&D. Motivated by this fact we have developed a simple strategy for the N-acyla- tion of carbazoles. (dokumen.tips)
Brain1
As a solution to damaged cells, Curcumin (curry leaf extract) has been noted to protect the enzymes within the brain cells that are vulnerable to deterioration. (com.bd)
Studies2
Structural studies on enzymes with divergent selectivities have the potential to illuminate critical features that are responsible for selectivity and provide valuable insight on how reactivity can be controlled in biocatalytic reactions. (nature.com)
In the present research work the docking studies was performed on the human pathogenic bacterial enzyme InhA from its parent domain Mycobacterium Tuberculosis . (thepharmajournal.com)
Active1
and 3) active P7C3 variants enhanced activity of purified NAMPT enzyme. (promegaconnections.com)
Common1
20 In view of the reported antitumor pro- perties of condensed N -acylindoles 21 a the N -acyl carbazole framework attracted our particular attention due to their common structural features. (dokumen.tips)
Effect2
Effect of carvedilol on reactive oxygen species and enzymes linking innate and adaptive immunity. (nel.edu)
Pecivová J, Macicková T, Lojek A, Gallová L, Cíz M, Nosál' R, Holománová D. Effect of carvedilol on reactive oxygen species and enzymes linking innate and adaptive immunity. (nel.edu)