Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 7 de 7
Filter
Add more filters










Database
Language
Publication year range
1.
Adv Exp Med Biol ; 1196: 109-115, 2020.
Article in English | MEDLINE | ID: mdl-32468312

ABSTRACT

Stroke is becoming a main cause of early death and disability in developing countries like India, and it is mostly enhanced by increased predominance of major risk factors. A detailed knowledge about the nature and magnitude of the stroke cases in this particular area is not only important for acute treatment but also it helps to prevent hospital admissions due to reoccurring stroke. The present study was conducted in the Department of Stroke at MGM Hospital, Warangal, India, to study the patterns of stroke admissions. All the collected data were compiled and analyzed using appropriate statistical tools. The mean age of study population was found to be 58.9 ± 18. Only 2.7% of stroke incidents occurred in people aged ≤40 years old, 4.9% of cases concerned people between 41 and 50 years old, 18.2% of the incidents happened when the subjects were between 51 and 60 years old, and in 74.2% of the cases, the individuals were ≥60 years old. The frequencies of ischemic (IS), subarachnoid hemorrhage (SAH), and intracerebral hemorrhage (ICH) in Warangal region were 57.9%, 7.3%, and 29.2%, respectively. A statistically significant association was found for both smoking (χ2 = 419.1 and p < 0.001) and alcohol (χ2 = 68.7 and p < 0.001) as risk factors in stroke. From this study, it was apparent that in Telangana region, there is a need to provide structured clinical management in treating emergency stroke cases and implement stroke care services with organized multidisciplinary teams.


Subject(s)
Stroke/epidemiology , Adult , Cerebral Hemorrhage/epidemiology , Hospitals , Humans , India/epidemiology , Middle Aged , Prevalence , Risk Factors , Subarachnoid Hemorrhage/epidemiology
2.
Adv Exp Med Biol ; 1195: 189-198, 2020.
Article in English | MEDLINE | ID: mdl-32468477

ABSTRACT

In the present work, new indole derivatives, i.e., 5-[N,N-di alkyl amino alkoxy] azaindole 2,3- di-one derivatives, are synthesized and characterized. These compounds were subjected to acute toxicity and then screened for antiepileptic activity on maximal electroshock seizure (MES) model in albino Wistar rats. In that study 5-[2-dimethyl amino ethoxy] Azaindole-3-hydrazone,2-one and 5-[2- dimethyl amino ethoxy] Azaindole 2-one,3-thiothiosemicarbazone(IIIa) showed good antiepileptic activity and less neurotoxicity compared to phenytoin. The purpose of the present study is to investigate the effect of 5-[2-dimethyl amino ethoxy] Indole 2,3- di one and 5-[2-dimethyl amino ethoxy] Azaindole 2-one,3-thiosemicarbazone(IIIa) derivatives on biogenic amines concentrations in rat brain after induction of seizures by MES method. The aim of study was relationship between seizure activities and altered the monoamines such as Noradrenaline (NA), Dopamine (DA), Serotonin (5-HT) in forebrain of rats in MES seizure models. In MES model, study of 5-[2-dimethyl amino ethoxy] Azaindole 3-hydrazone,2-one(Va) and 5-[2-dimethyl amino ethoxy]Azaindole 2-one,3-thiosemicarbazone(IIIa) (100 mg/kg) showed significant restoration of the decreased levels of brain monoamines such as noradrenaline, dopamine, and 5-hydroxytryptamine. Thus, this study suggests that 5-[2-Dimethyl amino ethoxy] Azaindole 3-hydrazone,2-one (V) and 5-[2-dimethyl amino ethoxy] Azaindole 2-one,3-thiosemicarbazone (IIIa) increased the monoamines on rat brain, which may decrease the susceptibility to MES-induced seizure in rats.


Subject(s)
Anticonvulsants/chemical synthesis , Anticonvulsants/therapeutic use , Indoles/chemical synthesis , Indoles/therapeutic use , Thiosemicarbazones/chemical synthesis , Thiosemicarbazones/therapeutic use , Alcohols/chemical synthesis , Alcohols/chemistry , Alcohols/pharmacology , Alcohols/therapeutic use , Animals , Anticonvulsants/chemistry , Anticonvulsants/pharmacology , Disease Models, Animal , Hydrazones/chemical synthesis , Hydrazones/chemistry , Hydrazones/pharmacology , Hydrazones/therapeutic use , Indoles/chemistry , Indoles/pharmacology , Rats , Rats, Wistar , Seizures/drug therapy , Thiosemicarbazones/chemistry , Thiosemicarbazones/pharmacology
3.
Adv Exp Med Biol ; 988: 39-48, 2017.
Article in English | MEDLINE | ID: mdl-28971387

ABSTRACT

The new heterocyclic compounds are used to treat epilepsy. In the present work new indole derivatives i.e. 5-[2(3)-di alkyl amino alkoxy] Indole 2,3-di-one derivatives are synthesized and characterized and these compounds was subjected to acute toxicity and then screened for antiepileptic activity on Maximal Electroshock (MES) seizures model in albino wistar rats. In that study 5-[2-dimethyl amino ethoxy] Indole 2,3 dione and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) showed good antiepileptic activity and less neurotoxicity compared to phenytoin. The purpose of the present study is to investigate the effect of 5-[2-dimethyl amino ethoxy] Indole 2,3-di one and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) derivatives on biogenic amines concentrations in rat brain after induction of seizures by Maximal Electro Shock(MES) method. Our aim of study was relationship between seizure activities and altered the monoamines such as noradrenaline (NA), dopamine (DA), serotonin (5-HT) in forebrain of rats in MES seizure models. In MES model, study of 5-[2-dimethyl amino ethoxy] Indole 2,3 dione(IIIa) and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) (100 mg/kg) showed significantly restored the decreased levels of brain monoamines such as Noradrenaline, Dopamine & 5-Hydroxy Triptamine. Thus, this study suggests that study of 5-[2-Dimethyl amino ethoxy] Indole 2,3-dione(IIIa) and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) increased the monoamines on rat brain, which may be decreased the susceptibility to MES induced seizure in rats.


Subject(s)
Anticonvulsants/pharmacology , Biogenic Amines/analysis , Brain Chemistry , Indoles/pharmacology , Seizures/drug therapy , Animals , Brain , Electroshock , Rats , Rats, Wistar
4.
Adv Exp Med Biol ; 988: 139-147, 2017.
Article in English | MEDLINE | ID: mdl-28971395

ABSTRACT

In the present work, some new 5-[2(3)-dialkylamino alkoxy] Indole 2,3-diones were prepared from 5-hydroxy isatin. A mixture of 5-hydroxy isatin, dialkylamino alkylhalide in alcoholic potassium hydroxide was stirred at room temperature for 6 h to get the 5-[2(3)-dialkylamino alkoxy] Indole 2,3-diones. The structures of the products were characterized by IR, NMR, MASS Spectral studies. All the compounds were evaluated for anti-inflammatory activity. Some of these compounds showed good anti-inflammatory activity compared with standard compound Indomethacin.


Subject(s)
Anti-Inflammatory Agents/chemistry , Drug Design , Indoles/chemistry , Isatin , Magnetic Resonance Spectroscopy
5.
Adv Exp Med Biol ; 822: 129-37, 2015.
Article in English | MEDLINE | ID: mdl-25416982

ABSTRACT

In the present work, some new 5-Hydroxyindole 3-thiosemicarbazone 2-ones and 5-[2(3)-dialkylaminoalkoxy] Indole 3-hydrazone 2-ones were prepared from 5-hydroxy isatin. The structures of the products were characterized by IR, NMR, and MASS Spectral studies. All the compounds were examined for antioxidant activity by using 1,1-diphenyl-2-picryl-hydrazyl and hydrogen peroxide (H2O2), and the total antioxidant capacity by a phosphomolybdenum assay. In general, the derivatives were found to exhibit antioxidant activity. Further, the compounds with dialkyl amino alkoxy at the C5 position demonstrated significant antioxidant activity.


Subject(s)
Antioxidants/pharmacology , Biphenyl Compounds/antagonists & inhibitors , Hydrogen Peroxide/antagonists & inhibitors , Isatin/pharmacology , Picrates/antagonists & inhibitors , Antioxidants/chemical synthesis , Antioxidants/chemistry , Biphenyl Compounds/chemistry , Biphenyl Compounds/metabolism , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology , Hydrazones/chemical synthesis , Hydrazones/chemistry , Hydrazones/pharmacology , Hydrogen Peroxide/chemistry , Hydrogen Peroxide/metabolism , Indoles/chemical synthesis , Indoles/chemistry , Indoles/pharmacology , Isatin/chemical synthesis , Isatin/chemistry , Magnetic Resonance Spectroscopy , Mass Spectrometry , Models, Chemical , Molecular Structure , Oxidation-Reduction/drug effects , Picrates/chemistry , Picrates/metabolism , Spectrophotometry, Infrared , Thiosemicarbazones/chemical synthesis , Thiosemicarbazones/chemistry , Thiosemicarbazones/pharmacology
6.
Adv Exp Med Biol ; 822: 119-28, 2015.
Article in English | MEDLINE | ID: mdl-25416981

ABSTRACT

In the present work, some new 5-[2(3)-dialkylamino alkoxy] Indole 3-thiosemicarbazone 2-ones and 5-[2(3)-dialkylamino alkoxy] Indole 3-hydrazone 2-one were prepared from 5-hydroxy isatin. The structures of the products were characterized by IR, NMR, and MASS Spectral studies. All the compounds were examined for antiepileptic activity by maximal electroshock seizure (MES) and pentylenetetrazole (PTZ) induced convulsion method. These compounds were also evaluated for their neurotoxicity study by rotarod method. Some of these compounds showed good antiepileptic activity when compared with standard drug Phenytoin and all the compounds showed less neurotoxicity when compared with standard drug Diazepam.


Subject(s)
Anticonvulsants/pharmacology , Isatin/pharmacology , Seizures/prevention & control , Alcohols/chemistry , Animals , Anticonvulsants/chemical synthesis , Anticonvulsants/chemistry , Electroshock/adverse effects , Hydrazones/chemical synthesis , Hydrazones/chemistry , Hydrazones/pharmacology , Indoles/chemical synthesis , Indoles/chemistry , Indoles/pharmacology , Isatin/chemical synthesis , Isatin/chemistry , Magnetic Resonance Spectroscopy , Male , Mass Spectrometry , Mice , Models, Chemical , Molecular Structure , Motor Activity/drug effects , Pentylenetetrazole , Schiff Bases/chemistry , Seizures/chemically induced , Seizures/etiology , Seizures/physiopathology , Spectrophotometry, Infrared , Thiosemicarbazones/chemical synthesis , Thiosemicarbazones/chemistry , Thiosemicarbazones/pharmacology
7.
Drug Metabol Drug Interact ; 25(1-4): 3-16, 2010.
Article in English | MEDLINE | ID: mdl-21417789

ABSTRACT

P-Glycoprotein (P-gp), the most extensively studied ATP-binding cassette transporter, functions as a biological barrier by extruding toxic substances and xenobiotics out of cells. Drug efflux pumps such as P-gp play a functional role in determining the pharmacokinetics of drugs administered by oral and parenteral routes. Determining the activity of drug efflux transport proteins has important implications in the identification of substrates and/or inhibitors. The significant role of the small intestine in reducing the oral bioavailability of drugs is due to metabolic enzymes and efflux transporters. The role of cytochrome P-450 3A (CYP3A) and P-gp in intestinal drug disposition has been highlighted. This review examines the structure, localisation and functional role of P-gp, the mechanism of drug efflux and drug-herb interactions.


Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism , Cytochrome P-450 Enzyme System/metabolism , Herb-Drug Interactions/physiology , Plant Preparations/adverse effects , Plant Preparations/metabolism , ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors , Animals , Cytochrome P-450 Enzyme Inhibitors , Enzyme Inhibitors/pharmacology , Humans , Intestinal Absorption/drug effects , Intestinal Absorption/physiology , Intestinal Mucosa/metabolism , Pharmaceutical Preparations/metabolism
SELECTION OF CITATIONS
SEARCH DETAIL
...