We report here the synthesis, the biological evaluation and the molecular modeling studies of new imidazo[1,2-a]pyridines derivatives designed as potent kinase inhibitors. This collection was obtained from 2-aminopyridines and 2-bromoacetophenone which afforded final compound in only one step. T...

A series of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides was designed and synthesized as new tropomyosin receptor kinases (Trks) inhibitors by utilizing a structure-guided optimization strategy. One of the most potent compounds 9o suppressed TrkA/B/C with IC50 values of 2.65, 10.47 a...

FLT3 inhibitors have been explored as a viable therapy for acute myeloid leukemia (AML). However, the clinical outcomes of these FLT3 inhibitors were underwhelming except AC220. Therefore, the development of novel FLT3 inhibitors with high potency against both FLT3-WT and FLT3-ITD mutants are st...

New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines sho...

Structural misassignments are often seen for complex natural products, but this can also be an issue with seemingly simpler structures. In this paper, we describe how, using a 15N-labelled analogue, we established that the Dimroth rearrangement can occur in imidazo[1,2-a]pyrimidines and result i...

ObjectiveTo compare the risk of developing Alzheimer’s disease (AD) dementia in late mild cognitive impairment (LMCI), early MCI (EMCI), and subjective memory impairment (SMI) with normal test performance.

Radium needles that were once implanted into tumours as a cancer treatment are now obsolete and constitute a radioactive waste problem, as their half-life is 1600 years. We are investigating the reduction of radium by transmutation by bombarding Ra-226 with high-energy neutrons from a neutron so...

Radium needles that were once implanted into tumours as a cancer treatment are now obsolete and constitute a radioactive waste problem, as their half-life is 1600 years. The reduction of radium by photonuclear transmutation by bombarding Ra-226 with high-energy photons from a medical linear acce...

The initial clinical trials for treatment of acute myeloid leukemia have demonstrated the effectiveness of the alpha emitter 213Bi in killing cancer cells. Bismuth-213 is obtained from a radionuclide generator system from decay of 10-days 225Ac parent. Recent pre-clinical studies have also shown...

The effects of MCI-225, a novel psychoactive compound, and reference drugs on attention behavior were studied using visual stimulus induced vertical eye tracking movements in midpontine pretrigeminal (PTG) feline preparation. Surgery was performed under ether anesthesia and subsequently switched...

We have previously reported that MCI-225, a selective noradrenaline (NA) reuptake inhibitor with serotonin (5-HT)3 receptor antagonism, shows antidepressant-like properties in experiments using rodents. In this study, we investigated the effect of MCI-225 in anxiety models in comparison with dia...

Effects of MCI-225, [4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-d]pyrimidine monohydrate hydrochloride] on experimental amnesia were studied in rats and compared with those of THA [9-amino-1,2,3,4-tetrahydroacridine]. In the Morris-type water maze task, MCI-225 (1–10 mg/kg, PO) red...

The effects of MCI-225 on amnesia, the cerebral glucose metabolism, and choline acetyltransferase (ChAT) activity in basal forebrain (BF)-lesioned rats were studied in comparison with those of tacrine. Bilateral BF lesions with ibotenic acid impaired the performance in passive avoidance (PA) tas...

The textile and dye industries are considered as one of the foremost sectors that pollutes environment. Technologies employing biological methods showed promising approach to remediate sites polluted with dye and dye intermediates. Bacterial consortium AR1 developed through culture enrichment me...

This research work designates for the assessment of effluent variables after dyeing of 100% cotton fabric with synthesized reactive dyes namely, Reactive Blue 19 (mono functional), Reactive Black 5 (homo bi-functional), and Reactive Red 195 and Reactive Yellow 145 (hetero bi-functional) dyes und...

A wide range of natural food colorants and coloring foodstuffs is available for the food industry to meet current costumer trends. Most natural pigments are more sensitive towards heat, light, and pH changes compared to their synthetic counterparts. Additionally, high dosages are often required ...

A method is described for efficient decolorization of reactive red 195 A dye (RR-195A) from aqueous and wastewater samples using modified Switchgrass Biochar (SB) by tetradecyltrimethyl ammonium bromide (TTAB) as a cationic surfactant for the formation of a novel SB-TTAB adsorbent. The different...

The facile synthesis of a new class of reactive hydrogen polysilsesquioxane (HPSQ, (HSiO1.5)n,) hollow spheres is reported in this work. HPSQ hollow spheres can be controllably fabricated from triethoxysilane (TES, HSi(OEt)3) as a sole precursor through a polystyrene template-directed sol–gel p...

Successful dyeing of lyocell, a biodegradable regenerated cellulose fiber, in fabric form is a challenging job. This article reports the successful reactive dyeing of lyocell fabrics with assistance of ultrasonic (US) energy via exhaust process, and compares the results with conventional (CN) ex...

The Nα-Boc and Nα-Fmoc protected derivatives of 2-amino-2,3-dihydro-1H-cyclopenta[b]anthracene-2-carboxylic acid (antAib), a novel fluorescent, achiral, α-amino acid, rigid analogue of the known 9-antAla and 2-antAla residues, and belonging to the class of Ciα→Ciα cyclized, Cα,α-disubsti...