Synthesis and molecular modelling studies of prenylated pyrazolines as MAO-B inhibitors.
Summary of "Synthesis and molecular modelling studies of prenylated pyrazolines as MAO-B inhibitors."
A series of N-substituted-3-[(2'-hydroxy-4'-prenyloxy)-phenyl]-5-phenyl-4,5-dihydro-(1H)-pyrazolines were synthesized and tested on human monoamine oxidase-A and -B isoforms. Structure-activity relationships and molecular modelling showed that some substitutions, such as benzyloxy or chlorine atom, improve the best interaction with active site of hMAO-B.
Dipartimento di Chimica e Tecnologie del Farmaco, Università di Roma La Sapienza P.le Aldo Moro, 5, 00185 Rome, Italy. firstname.lastname@example.org
This article was published in the following journal.
Name: Bioorganic & medicinal chemistry letters
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/20934874
- DOI: http://dx.doi.org/10.1016/j.bmcl.2010.09.061
Medical and Biotech [MESH] Definitions
Water-soluble, copper-containing low molecular weight polypeptides obtained from the culture medium of Streptomyces verticillus. They are specific inhibitors of DNA synthesis in bacteria and have been found to act as antitumor agents. They have also been used against rust fungi of plants.
Studies designed to examine associations, commonly, hypothesized causal relations. They are usually concerned with identifying or measuring the effects of risk factors or exposures. The common types of analytic study are CASE-CONTROL STUDIES; COHORT STUDIES; and CROSS-SECTIONAL STUDIES.
Protein Synthesis Inhibitors
Compounds which inhibit the synthesis of proteins. They are usually ANTI-BACTERIAL AGENTS or toxins. Mechanism of the action of inhibition includes the interruption of peptide-chain elongation, the blocking the A site of ribosomes, the misreading of the genetic code or the prevention of the attachment of oligosaccharide side chains to glycoproteins.
Nucleic Acid Synthesis Inhibitors
Compounds that inhibit cell production of DNA or RNA.
Hydroxymethylglutaryl-coa Reductase Inhibitors
Compounds that inhibit HMG-CoA reductases. They have been shown to directly lower cholesterol synthesis.
An efficient Zn(ii)-catalyzed intermolecular double hydroamination of 1,3-enynes with aryl hydrazines, for the synthesis of pyrazolines, has been discussed.
Two new tetracyclic prenylated acylphloroglucinols, chipericumins A (1) and B (2), were isolated from the roots of Hypericum chinense, together with two new tricyclic prenylated acylphloroglucinols, c...
A novel series of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines (5a-o) has been synthesized and the structures of newly synthesized compounds were characterized by IR, (1)H NMR and ma...
A general, metal-free, highly enantioselective Brønsted acid catalyzed [3+2] cycloaddition between hydrazones and alkenes has been developed that affords pyrazolidine derivatives. The resulting opt...
Phytoalexins from soya are mainly characterised as prenylated pterocarpans, the glyceollins. Extracts of non-soaked and soaked soya beans, as well as that of soya seedlings, grown in the presence of R...
HMG CoA reductase inhibitors (statins) are commonly used to treat high cholesterol (HC) in both type 1 and type 2 diabetes mellitus (DM). Several studies have shown benefits of statin amon...
The purpose of this study is to determine if diabetic retinopathy can be treated with prostaglandin analogues, prostaglandin synthesis inhibitors or carbonic anhydrases inhibitors.
Cholesterol is the precursor of glucocorticoids, mineralocorticoids and sex steroids. Both adrenal and non-adrenal (ovarian + testicular) all steroid hormones are primarily synthesized usi...
To establish a serial ascertainement of specimens from patients with bone sarcomas to be used in ongoing cytogenetic and molecular genetic analyses. These data will be integrated and corre...
Our hypothesis is that a new method of depth of anaesthesia monitoring, using theoretically based time series modelling will result in improved ability to determine nitrous oxide anaesthet...