PMID: 15344840Sep 4, 2004Paper

Studies on 3-diethylaminocarbonyl-1,4,5,6,7,8-hexahydroquinoline derivatives and their calcium channel antagonistic activities in vitro

Arzneimittel-Forschung
Emrah KismetliA Linden

Abstract

In this study, thirteen 2,6,6-trimethyl-3-carbamoyl-4-aryl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives were synthesized and screened for their calcium channel antagonistic actitivities. The hexahydroquinoline derivatives were synthesized according to Hantzsch reaction. The structures of the compounds were elucidated by IR, 1H-NMR, 13C-NMR, Distortionless Enhancement Polarization Transfer (DEPT), Correlation Spectroscopy (COSY), mass spectroscopy and elemental analyses. The calcium antagonistic activities of the compounds were determined by tests performed on isolated rat ileum and lamb carotid artery. In isolated rat ileum, compounds 8, 12 and 13 were found to be more active than nicardipine (CAS 55985-32-5) at a concentration of 10(-5) mol/L. At the concentration 10(-4) mol/L, compounds 7 and 12 were more active than nicardipine and compounds 5, 8 and 13 were equipotent. In lamb carotid artery studies, at the concentration 10(-5) mol/L all compounds were found to be less active than nicardipine; at the concentration 10(-4) mol/L compounds 5 and 13 showed greater inhibition than nicardipine. At this concentration, compound 9 was found to be as active as nicardipine.

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.