scholarly journals Synthesis and Antihypertensive Screening of New Derivatives of Quinazolines Linked with Isoxazole

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Mujeeb Ur Rahman ◽  
Ankita Rathore ◽  
Anees A. Siddiqui ◽  
Gazala Parveen ◽  
M. Shahar Yar
Keyword(s):  
Adrenergic Receptor ◽  
Hydroxylamine Hydrochloride ◽  
Antihypertensive Activity ◽  
Albino Rats ◽  
Duration Of Action ◽  
Prolonged Duration ◽  
Anaesthetized Rats ◽  
Blocking Property ◽  
Derivatives Of

A series of 7-substituted-3-(4-(3-(4-substitutedphenyl)-4,5-dihydroisoxazol-5-yl)phenyl)-2-substituted quinazolin-4(3H)-one(1–30)have been synthesized by the cyclization of (E)-3-(4-(3-substitutedphenyl)acrylolyl)phenyl)-2-(substitutedphenyl)-7-substituted quinazolin-4-(3H)-one with hydroxylamine hydrochloride. The synthesized compounds were examined for theirin vivoantihypertensive activity using albino rats. All the titled compounds exhibited good to moderate antihypertensive activity. Compounds 7-Chloro-3-(4-(3-(4-chlorophenyl)-4,5- dihydroisoxazol-5-yl)phenyl)-2-p-tolylquinazolin-4(3H)-one(23)and 7-Chloro-3-(4-(3-(4-chlorophenyl)-4,5-dihydroisoxazol-5-yl)phenyl)-2-(4-methoxyphenyl)quinazolin-4(3H)-one(24)exhibited potent antihypertensive activity through their anticipatedα1-adrenergic receptor blocking property similar to its clinically used analogue, prazosin, without affecting heart rate with prolonged duration of action when tested in adrenaline induced hypertension in anaesthetized rats.

Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo

1986 ◽  
Vol 29 (10) ◽  
pp. 2088-2093 ◽  
Author(s):  
Suvit Thaisrivongs ◽  
Donald T. Pals ◽  
Douglas W. Harris ◽  
Warren M. Kati ◽  
Steve R. Turner
Keyword(s):  
Renin Inhibitor ◽  
Duration Of Action ◽  
Design And Synthesis ◽  
Prolonged Duration

Anti-Hypertensive Activity of Hydro Alcoholic Extract of Cìraka Cūraṇam on High Salt Loaded Wistar Albino Rats

2021 ◽  
Vol 8 (5) ◽  
pp. 110-115
Author(s):  
Sujeethasai K ◽  
Manoharan A ◽  
Santhanakumar M
Keyword(s):  
Heart Diseases ◽  
Premature Death ◽  
Antihypertensive Activity ◽  
Albino Rats ◽  
Alcoholic Extract ◽  
Deoxycorticosterone Acetate ◽  
Wistar Albino Rats ◽  
Animal House ◽  
Hypertensive Activity

Background: Hypertension is called as Silent killer. The most important risk factor for heart diseases and stroke and it may leads to premature death. Several medicinal plants have high effective in anti-hypertensive and anti-thrombotic activity without any side effects. Aim: To evaluate the anti-hypertensive activity of hydro alcoholic extract of Cìraka cūraṇam on deoxycorticosterone acetate (DOCA) salt induced wistar albino rats. Study design: Observational in-vivo study Place and duration of study: Animal house, Dept. of Pharmacology, Arulmigu Kalasalingam College of Pharmacy, Krishnankoil, Srivilliputtur,Tamilnadu. Materials and methods: Antihypertensive activity was conducted on wistar albino rats by determining serum Sodium and Potassium levels by using semi auto analyzer (RA-50, Bayer Diagnostics), using specific kits (Auto span, India) at 500 and 550 nm respectively and left carotid artery (for recording BP) was cannulated under aseptic conditions with polyethylene cannula filled with 1% heparin in normal saline. Rest procedure, which was stated under the 2K1C-model was followed and BP was observed in terms of mm of Hg. Results: The Cìraka cūraṇam possesses strong antihypertensive effect against DOCA-salt hypertensive rats, which is evidenced by a considerable decrease in blood pressures. Keywords: Anti-hypertensive activity, Cìraka cūraṇam, Wistar albino rats, Deoxycorticosterone acetate.

Kinin B1 receptor antagonists with multi-enzymatic resistance properties

2002 ◽  
Vol 80 (4) ◽  
pp. 287-292 ◽  
Author(s):  
Witold Neugebauer ◽  
Paul A Blais ◽  
Stephanie Hallé ◽  
Catherine Filteau ◽  
Domenico Regoli ◽  
...  
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Human Platelets ◽  
Converting Enzyme ◽  
Receptor Antagonists ◽  
Rabbit Lung ◽  
Duration Of Action ◽  
Prolonged Duration ◽  
Bradykinin Antagonists

The kinin B1 receptor has been implicated in a variety of pathological states; therefore, potent, selective, and specific antagonists with prolonged duration of action in vivo are needed. Using R-715 (AcLys[D-β-Nal7,Ile8] desArg9BK) as a template, new peptides containing α-MePhe in position 5, Oic in position 2, and AcOrn instead of AcLys at the N-terminal were prepared and tested for their antagonist potency, their selectivity, and their specificity for the kinin B1 receptor. In vitro metabolic stabilities toward aminopeptidase M (from human plasma), aminopeptidase P (from human platelets), and angiotensin-converting enzyme (purified from rabbit lung) were also investigated. The results of this study indicate that the three modifications applied separately are as well tolerated as they are when present conjointly in the template R-715. Indeed, pA2 values of R-715 (ranging from 8.40 to 8.5) do not differ significantly from the analogues R-954 and R-955 (both ranging from 8.4 to 8.6) when measured at kinin B1 receptors from rabbit aortas and human umbilical veins. Moreover, the chemical modifications utilized in the peptides R-954 and R-955 have provided resistance against aminopeptidases M and P, as well as the angiotensin-converting enzyme, unlike the early (e.g., Lys[Leu8]desArg9BK) and more recent (e.g., R-715, B-9858) generations of B1 receptor antagonists. Ongoing in vivo assays will validate the assumption that the analogues R-954 and R-955 have a prolonged duration of action.Key words: bradykinin, antagonists, B1 receptors, peptidases, metabolism.

ChemInform Abstract: Design and Synthesis of a Potent and Specific Renin Inhibitor with a Prolonged Duration of Action in vivo.

ChemInform ◽  
1987 ◽  
Vol 18 (11) ◽  
Author(s):  
S. THAISRIVONGS ◽  
D. T. PALS ◽  
D. W. HARRIS ◽  
W. M. KATI ◽  
S. R. TURNER
Keyword(s):  
Renin Inhibitor ◽  
Duration Of Action ◽  
Design And Synthesis ◽  
Prolonged Duration

Acyl-Enzymes as Thrombolytic Agents in Dog Models of Venous Thrombosis and Pulmonary Embolism

1984 ◽  
Vol 51 (02) ◽  
pp. 248-253 ◽  
Author(s):  
R J Dupe ◽  
P D English ◽  
R A G Smith ◽  
J Green
Keyword(s):  
Pulmonary Embolism ◽  
Side Effects ◽  
Venous Thrombosis ◽  
Active Site ◽  
Acute Pulmonary Embolism ◽  
Quantitative Model ◽  
Beagle Dog ◽  
Thrombosis Model ◽  
Derivatives Of

SummaryA quantitative model of venous thrombosis in the beagle dog is described. The model was adapted to permit ageing of isolated experimental clots in vivo. A model of acute pulmonary embolism in this species is also described. In the venous thrombosis model, infusion of streptokinase (SK) or SK-activated human plasmin gave significant lysis but bolus doses of SK. plasmin complex were ineffective. Active site anisoylated derivatives of SK. plasminogen complex, SK-activated plasmin and activator-free plasmin were all active when given as bolus doses in both models. At lytic doses, the acyl-enzymes caused fewer side-effects attributable to plasminaemia than the corresponding unmodified enzymes.

Synthesis and In Vivo Antimalarial Activity of Novel Derivatives of 6- Mercaptopurine

2013 ◽  
Vol 10 (8) ◽  
pp. 741-747 ◽  
Author(s):  
Roberta Soares ◽  
Roberta Corrales ◽  
Fernanda Lopes ◽  
Marcio Alves ◽  
Adilson Silva ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Derivatives Of

Derivatives of Deoxypodophyllotoxin Induce Apoptosis Through Bcl-2/Bax Proteins Expression

2020 ◽  
Vol 20 ◽  
Author(s):  
Ya-Nan Li ◽  
Ni Ning ◽  
Lei Song ◽  
Yun Geng ◽  
Jun-Ting Fan ◽  
...  
Keyword(s):  
Annexin V ◽  
Mtt Method ◽  
Anthriscus Sylvestris ◽  
Anti Tumor Activity ◽  
Derivatives Of ◽  
Toxicity In Vitro ◽  
Ht 29 ◽  
Mcf 7

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.

Cardiovascular Effects of Micromeria graeca (L.) Benth. ex Rchb in Normotensive and Hypertensive Rats

2020 ◽  
Vol 20 (8) ◽  
pp. 1253-1261
Author(s):  
Mourad Akdad ◽  
Mohamed Eddouks
Keyword(s):  
Blood Pressure ◽  
Cardiovascular System ◽  
Arterial Blood Pressure ◽  
Antihypertensive Activity ◽  
Computer Assisted ◽  
Hypertensive Rats ◽  
Vasorelaxant Effect ◽  
Arterial Blood

Aims: The present study was performed in order to analyze the antihypertensive activity of Micromeria graeca (L.) Benth. ex Rchb. Background: Micromeria graeca (L.) Benth. ex Rchb is an aromatic and medicinal plant belonging to the Lamiaceae family. This herb is used to treat various pathologies such as cardiovascular disorders. Meanwhile, its pharmacological effects on the cardiovascular system have not been studied. Objective: The present study aimed to evaluate the effect of aqueous extract of aerial parts of Micromeria graeca (AEMG) on the cardiovascular system in normotensive and hypertensive rats. Methods: In this study, the cardiovascular effect of AEMG was evaluated using in vivo and in vitro investigations. In order to assess the acute effect of AEMG on the cardiovascular system, anesthetized L-NAME-hypertensive and normotensive rats received AEMG (100 mg/kg) orally and arterial blood pressure parameters were monitored during six hours. In the sub-chronic study, rats were orally treated for one week, followed by blood pressure assessment during one week of treatment. Blood pressure was measured using a tail-cuff and a computer-assisted monitoring device. In the second experiment, isolated rat aortic ring pre-contracted with Epinephrine (EP) or KCl was used to assess the vasorelaxant effect of AEMG. Results: Oral administration of AEMG (100 mg/kg) provoked a decrease of arterial blood pressure parameters in hypertensive rats. In addition, AEMG induced a vasorelaxant effect in thoracic aortic rings pre-contracted with EP (10 μM) or KCl (80 mM). This effect was attenuated in the presence of propranolol and methylene blue. While in the presence of glibenclamide, L-NAME, nifedipine or Indomethacin, the vasorelaxant effect was not affected. Conclusion: This study showed that Micromeria graeca possesses a potent antihypertensive effect and relaxes the vascular smooth muscle through β-adrenergic and cGMP pathways.

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