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Ramelteon: a melatonin receptor agonist for the treatment of insomnia

Devi V, Shankar PK

J Postgrad Med, 2008 2 26;54(1):45-8.
PMID: 18296808

Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for the treatment of insomnia characterized by difficulty in sleep onset. It is a nonscheduled drug since it lacks the potential for abuse and does not interact with neurotransmitter receptors most associated with these phenomena. Although the effects of ramelteon use > 5 weeks are unknown, the available data confirms its safety and efficacy for short-term use. Clinical use and future research should uncover more information about ramelteon's properties.

Matched MeSH terms: Indenes/administration & dosage; Indenes/pharmacology*; Indenes/therapeutic use*
Optimization of microencapsulation process for self-healing polymeric material

Then S, Gan SN, Noor Hayaty Abu Kasim

Sains Malaysiana, 2011;40:1179-1186.

A series of poly(urea-formaldehyde) (PUF) microcapsules filled with dicyclopentadiene (DCPD) was successfully prepared by in situ polymerization. The effect of diverse process parameters and ingredients on the morphology of the microcapsules was observed by SEM, optical microscopy (OM) and digital microscopy. Different techniques for the characterization of the chemical structure and the core content were considered such as FT-IR and 1H-NMR as well as the characterization of thermal properties by DSC. High yields of free flowing powder of spherical microcapsules were produced. The synthesized microcapsules can be incorporated into another polymeric host material. In the event the host material cracks due to excessive stress or strong impact, the microcapsules would rupture to release the DCPD, which could polymerize to repair the crack.

Matched MeSH terms: Indenes
High Throughput Residue Analysis of Indaziflam and its Metabolites in Palm Oil Using Liquid Chromatography-Tandem Mass Spectrometry

Halim N, Kuntom A, Shinde R, Banerjee K

J AOAC Int, 2020 Sep 01;103(5):1237-1242.
PMID: 33241391 DOI: 10.1093/jaoacint/qsaa041

BACKGROUND: Indaziflam (IND) is a herbicide that is used in palm oil plantations for broad spectrum management of weeds. Until now, no validated method has been available for residue estimation of this herbicide in palm oil products.
OBJECTIVE: In this study, we report a rapid method for the residue analysis of IND and its metabolites, viz., IND-carboxylic acid, diaminotriazine, and triazine indanone in a wide range of palm oil matrices using liquid chromatography-tandem mass spectrometry (LC-MS/MS).
METHOD: The optimized sample preparation workflows included two options: (1) acetonitrile extraction (QuEChERS workflow), followed by freezing at -80°C and (2) acetonitrile extraction, followed by cleanup through a C18 solid phase extraction (SPE) cartridge. The optimized LC runtime was 7 min. All these analytes were estimated by LC-MS/MS multiple reaction monitoring.
RESULTS: Both sample preparation methods provided similar method performance and acceptable results. The limit of quantification (LOQ) of IND, IND-carboxylic acid, and triazine indanone was 0.001 mg/kg. For diaminotriazine, the LOQ was 0.005 mg/kg. The method accuracy and precision complied with the SANTE/12682/2019 guidelines of analytical quality control.
CONCLUSIONS: The potentiality of the method lies in a high throughput analysis of IND and its metabolites in a single chromatographic run with high selectivity and sensitivity. Considering its fit-for-purpose performance, the method can be implemented in regulatory testing of IND residues in a wide range of palm oil matrices that are consumed and traded worldwide.
HIGHLIGHTS: This work has provided a validated method for simultaneous residue analysis of indaziflam and its metabolites in crude palm oil and its derived matrices with high sensitivity, selectivity, and throughput.

Matched MeSH terms: Indenes
The effect of melatonin on delirium in hospitalised patients: A systematic review and meta-analyses with trial sequential analysis

Ng KT, Teoh WY, Khor AJ

J Clin Anesth, 2020 Feb;59:74-81.
PMID: 31279283 DOI: 10.1016/j.jclinane.2019.06.027

OBJECTIVES: Melatonin is an endogenous hormone, which regulates circadian rhythms and promotes sleep. In recent years, several randomised controlled trials examining the prophylactic use of melatonin to prevent delirium were published with conflicting findings. The primary aim of this review was to determine the effect of melatonin on the incidence of delirium in hospitalised patients.
DATA SOURCES: MEDLINE, EMBASE and CENTRAL were systematically searched from their inception until December 2018.
REVIEW METHODS: All randomised clinical trials were included.
RESULTS: Sixteen trials (1634 patients) were included in this meta-analysis. Incidence of delirium was not significantly lower in patients who received melatonin, with an odd ratio, OR (95%Cl) of 0.55 (0.24-1.26); ρ = 0.16, certainty of evidence = low, trial sequential analysis = inconclusive. However, patients who randomised to melatonin had a significantly shorter length of stay in intensive care units, with a mean difference, MD (95%CI) of -1.84 days (-2.46, -1.21); ρ 

Matched MeSH terms: Indenes/administration & dosage*; Indenes/adverse effects
A facile stereoselective synthesis of dispiro-indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids and evaluation of their antimycobacterial, anticancer and AchE inhibitory activities

Bharkavi C, Vivek Kumar S, Ashraf Ali M, Osman H, Muthusubramanian S, Perumal S

Bioorg Med Chem, 2016 11 15;24(22):5873-5883.
PMID: 27687968 DOI: 10.1016/j.bmc.2016.09.044

A facile stereoselective synthesis of novel dispiro indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids has been achieved by 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from ninhydrin and sarcosine/thiaproline, on a series of 3-benzylidenethiochroman-4-ones. The synthesised compounds were screened for their antimycobacterial, anticancer and AchE inhibition activities. Compound 4l (IC50 1.07μM) has been found to exhibit the most potent antimycobacterial activity compared to cycloserine (12 times), pyrimethamine (37 times) and ethambutol (IC50 <1.56μM) and 6l (IC50=2.87μM) is more active than both cycloserine (4 times) and pyrimethamine (12 times). Three compounds, 4a, 6b and 6i, display good anticancer activity against CCRF-CEM cell lines. Compounds 6g and 4g display maximum AchE inhibitory activity with IC50 values of 1.10 and 1.16μmol/L respectively.

Matched MeSH terms: Indenes/pharmacology; Indenes/chemistry
Development of anti-acanthamoebic approaches

Mungroo MR, Tong T, Khan NA, Anuar TS, Maciver SK, Siddiqui R

Int Microbiol, 2021 Aug;24(3):363-371.
PMID: 33754231 DOI: 10.1007/s10123-021-00171-3

Acanthamoeba keratitis is a sight-endangering eye infection, and causative organism Acanthamoeba presents a significant concern to public health, given escalation of contact lens wearers. Contemporary therapy is burdensome, necessitating prompt diagnosis and aggressive treatment. None of the contact lens disinfectants (local and international) can eradicate Acanthamoeba effectively. Using a range of compounds targeting cellulose, ion channels, and biochemical pathways, we employed bioassay-guided testing to determine their anti-amoebic effects. The results indicated that acarbose, indaziflam, terbuthylazine, glimepiride, inositol, vildagliptin and repaglinide showed anti-amoebic effects. Compounds showed minimal toxicity on human cells. Therefore, effects of the evaluated compounds after conjugation with nanoparticles should certainly be the subject of future studies and will likely lead to promising leads for potential applications.

Matched MeSH terms: Indenes/pharmacology