The parallel solution-phase synthesis of a new combinatorial library of 3-[4-(R1-coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides 9 has been developed. The synthesis involves two steps: 1) the synthesis of core building blocks - 3- [4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acids, 6 - by the reaction of 3-(omega-bromacetyl)coumarins 1 with 3-amino(thioxo)methylcarbamoy...

[Structure: see text] The versatility of supramolecular chemistry has been exploited in constructing nanovalves based on mesoporous silica MCM-41 and the mutual recognition between secondary dialkylammonium ions and dibenzo[24]crown-8 (DB24C8). Naphthalene-containing dialkylammonium threads were tethered to the MCM-41, followed by loading with coumarin 460 and capping with DB24C8. Controlled re...

Present work describes the synthesis of coumarin Mannich bases 4-7 by the application of Mannich reaction on 7-hydroxy-4-methyl coumarin 3 using conventional as well as microwave technology to compare the feasibility, reaction time and yield of the product. For this, 7-hydroxy-4-methyl coumarin 3 was prepared using Pechmann condensation reaction and Mannich bases (4-7) were synthesized by the r...

The biologically relevant arenes ethyl salicylate and salicylic amide as well the fluorescent coumarin pyrene units were functionalized with a cyclopentadiene unit. Re 99mTc complexes of latter two synthesized fully characterized. During crystallization ligands, [2+2] [6+6] cycloadditions observed for modified coumarin. A light-induced mechanism, supported by DFT calculations, is proposed these...

Abstract Thrombosis is the leading cause of illness and mortality worldwide, posing a serious risk to human health life. Because antithrombotic drugs can prevent beginning progression thrombotic disorders, they are essential in management diseases. The substantial side effects unsatisfactory efficacy present stimulate search for novel, effective, safer therapies. Natural synthetic coumarins hav...

AIM To observe the biotransformation process of a Chinese compound, aesculin, by human gut bacteria, and to identify its metabolites in rat urine. METHODS Representative human gut bacteria were collected from 20 healthy volunteers, and then utilized in vitro to biotransform aesculin under anaerobic conditions. At 0, 2, 4, 8, 12, 16, 24, 48 and 72 h post-incubation, 10 mL of culture medium was...

BACKGROUND The perioperative management of anticoagulation in patients who are having implantation of a pacemaker or implantable cardioverter defibrillator (ICD) is a common clinical problem in which best clinical practise is not established. METHODS We performed a systematic review of the literature to assess the safety (pocket hematoma risk) and efficacy (thromboembolism risk) of different ...

Coumarin (1,2-benzopyrone) is a natural compound that has been used as a fragrance in the food and perfume industry and could have therapeutic usefulness in the treatment of lymphedema and different types of cancer. Several previous pharmacokinetic studies of coumarin have been performed in humans, which revealed extensive first-pass metabolism of the compound. 7-Hydroxycoumarin (7-HC) and its ...

Coumarin, a widely used fragrance ingredient, is a rat liver and mouse lung toxicant. Species differences in toxicity are metabolism-dependent, with injury resulting from the cytochrome P450-mediated formation of coumarin 3,4-epoxide (CE). In this study, the enzymes responsible for coumarin activation in liver and lung were determined. Recombinant human and rat CYP1A forms and recombinant human...

A green one-pot synthesis of 5H-Chromeno[4,3-b]pyridin-5-one derivatives which are the main core natural product Polyneomarline C is described by reaction 4-chloro-3-formyl coumarin and different cyclic acyclic compounds having active methylene group in presence Et3N NH4OAc EtOH. The advantages this strategy good yields, no need for chromatographic separation absence heavy metal catalysts toxic...