Synthesis and inotropic evaluation of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)piperidine-4-carboxamides.

Bioorg Med Chem Lett

Changbai Mountain Key Laboratory of Natural Resources and Functional Molecules, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, PR China.

Published: May 2009

A series of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl) piperidine-4-carboxamides has been synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit-heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 1-(2-fluorobenzyl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)piperidine-4-carboxamide 6a was the most potent, increasing stroke volume by 11.92+/-0.35% (milrinone: 6.36+/-0.13%) at 1x10(-4)M.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2009.03.089DOI Listing

Publication Analysis

Top Keywords

stroke volume
8
synthesis inotropic
4
inotropic evaluation
4
evaluation 1-substituted-n-45-dihydro-1-methyl-[124]triazolo[43-a]quinolin-7-ylpiperidine-4-carboxamides
4
1-substituted-n-45-dihydro-1-methyl-[124]triazolo[43-a]quinolin-7-ylpiperidine-4-carboxamides series
4
series 1-substituted-n-45-dihydro-1-methyl-[124]triazolo[43-a]quinolin-7-yl
4
1-substituted-n-45-dihydro-1-methyl-[124]triazolo[43-a]quinolin-7-yl piperidine-4-carboxamides
4
piperidine-4-carboxamides synthesized
4
synthesized evaluated
4
evaluated positive
4

Similar Publications

Risk factors of posthemorrhagic seizure in spontaneous intracerebral hemorrhage.

Neurosurg Rev

January 2025

Division of Neurosurgery, Department of Surgery, Faculty of Medicine Siriraj Hospital, Mahidol University, 2 Wang Lang Road, Bangkok Noi, Bangkok, 10700, Thailand.

Seizure is a relatively common neurological consequence after spontaneous intracerebral hemorrhage (SICH). This study aimed to investigate risk factors of early, late, and overall seizures in patients with SICH. Retrospective analysis was performed on all patients with SICH who completed two years of follow-up.

View Article and Find Full Text PDF

This study aimed to evaluate the hemodynamic and ventricular performance of neonates with hypoxic-ischemic encephalopathy (HIE) undergoing therapeutic hypothermia using conventional and advanced echocardiographic techniques. This observational, prospective study included 22 neonates with HIE matched with 22 healthy neonates. Echocardiographic studies were performed 24 h after achieving target temperature during hypothermia and 24 h after rewarming.

View Article and Find Full Text PDF

The prognostic impact of arterial spin labeling hyperperfusion in acute ischemic stroke: a systematic review and meta-analysis.

Acta Radiol

January 2025

Department of Radiology & Institute of Rehabilitation and Development of Brain Function, Nanchong Central Hospital, The Second Clinical Medical College of North Sichuan Medical College, Nanchong, Sichuan, PR China.

Hyperperfusion is related to vessel recanalization, tissue reperfusion, and collateral circulation. To determine the prognostic impact of hyperperfusion after an acute ischemic stroke (AIS) identified by arterial spin labeling (ASL) cerebral blood flow. Studies published in PubMed, Embase, and Cochrane Library databases were searched.

View Article and Find Full Text PDF

Spirometric pattern and cardiovascular risk: a prospective study of 0.3 million Chinese never-smokers.

Lancet Reg Health West Pac

January 2025

Department of Epidemiology & Biostatistics, School of Public Health, Peking University, Beijing 100191, China.

Background: Existing studies have not provided robust evidence about the CVD risk of non-smoking patients with restrictive spirometric pattern (RSP) or airflow obstruction (AFO), and how the risk is modified by body shape. We aimed to bridge the gap.

Methods: We used never-smokers' data from the China Kadoorie Biobank (CKB) and performed Cox models by sex (278,953 females and 50,845 males).

View Article and Find Full Text PDF

Rat models of postintracerebral hemorrhage pneumonia induced by nasal inoculation with or intratracheal inoculation with LPS.

Front Immunol

January 2025

State Key Laboratory of Traditional Chinese Medicine Syndrome, Department of Neurology, Guangdong Provincial Academy of Chinese Medical Sciences, Guangdong Provincial Hospital of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, China.

Background: A stable and reproducible experimental bacterial pneumonia model postintracerebral hemorrhage (ICH) is necessary to help investigating the pathogenesis and novel treatments of Stroke-associated pneumonia (SAP).

Aim: To establish a Gram-negative bacterial pneumonia-complicating ICH rat model and an acute lung injury (ALI)-complicating ICH rat model.

Methods: We established two standardized models of post-ICH pneumonia by nasal inoculation with () or intratracheal inoculation with lipopolysaccharide (LPS).

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!