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Mukhtyar S. Saini*1 and Jaya Dwivedi 2

U2 - 10.1021/ja1018783

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K. Ilango et al, 53synthesized a new series of 3, 6-disubstituted-1, 2, 4-triazolo-[3, 4-b]-1, 3, 4- thiadiazoles. The compounds (15) were screened for antifungal activity against Candida albicans and Aspergillus niger using Ketoconazole as standard.

SYNTHESIS AND BIOLOGICAL SIGNIFICANCES OF 1, 2, 4-TRIAZOLE AND ITS DERIVATIVES: A REVIEW

The derivatization of Triazole is considered to be based on the phenomenon of bioisosterism in which replacement of oxygen of oxadiazole nucleus with nitrogen atom yields triazole analogue. There are two possible isomers of triazole (1, 2) depending on the position of nitrogen atom in the ring and are numbered as shown in Fig. 1. Out of the two triazoles, 1, 2, 4- triazole have drawn great attention to medicinal chemists from two decades due to its wide variety of activity 2, low toxicity and good Pharmacokinetic and Pharmacodynamic profiles. Its diversity in showing the pharmacological activities is mind blowingly identified well by the medicinal chemists as;

1155 Sixteenth Street N.W.Washington, DC 20036

1155 Sixteenth Street N.W.Washington, DC 20036

A series of novel blue-light-emitting 2-imidazo[5,1-]isoquinolinium chloride derivatives were synthesized by the reaction of isoquinoline with trifluoroacetimidoyl chlorides and isocyanides in dry CH2Cl2 in excellent yields. Fluorescence studies showed that the compounds absorb UV radiation and then emit blue light at about 481 nm with moderate to good fluorescence quantum yields. These compounds also showed high Stokes shifts, and can be used to develop ­ultrasensitive fluorescent molecular probes to study a variety of biological events and processes.

A series of novel blue-light-emitting 2-imidazo[5,1-]isoquinolinium chloride derivatives were synthesized by the reaction of isoquinoline with trifluoroacetimidoyl chlorides and isocyanides in dry CH2Cl2 in excellent yields. Fluorescence studies showed that the compounds absorb UV radiation and then emit blue light at about 481 nm with moderate to good fluorescence quantum yields. These compounds also showed high Stokes shifts, and can be used to develop ­ultrasensitive fluorescent molecular probes to study a variety of biological events and processes.

1155 Sixteenth Street N.W.Washington, DC 20036

1, 2, 3-TRIAZOLE 1, 2, 4-TRIAZOLE

As a result of 29 experiments with reaction times ranging from 10 to 30 min, an optimized procedure was derived that allowed the preparation of monastrol in 82%.

The three-component condensation of 1,3-diarylprop-2-en-1-one with ammonia and aldehydes/acetone or N-substituted -pyridones under ultrasonic irradiation was developed as a rapid and efficient solution-phase method for the high-yielding preparation of 2-aryl(hetaryl)-4,6-diaryl-1,2,5,6-tetrahydropyrimidines and 2,4-diaryl-1,5,9-triazaspiro[5.5]undec-1-enes.

SCHEME 2: Synthesis of a substituted 1, 2, 4-triazole from amide and a hydrazide
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  • © 2018 Merck KGaA, Darmstadt, Germany and/or its affiliates

    DO - 10.1021/ja1018783

  • Research on imidazo[2,1-?]isoquinoline derivatives

    Received: 05 August 2017Accepted after revision: 04 October 2017Publication Date:23 October 2017 (eFirst)

  • One-Pot Synthesis of Benzo[4,5]imidazo[2,1 …

    Todoulou O.G et al, 57 and 58-60 have evaluated the compounds (19-22) as below and found antifungal activity.

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Research on imidazo[2,1-α]isoquinoline derivatives

ABSTRACT: In the last few decades, to synthesize the different new heterocyclic compounds along their derivatives which were evaluated for their biological activities as antimicrobial, antiviral, antitumor, anticonvulsant, antifungal, the triazole moiety seems to be very small but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. In this review we provides a brief response of the medicinal chemistry of 1, 2, 4-triazole and its derivatives. A literature survey of procedures for the preparation of 1, 2, 4-triazole and 1, 2, 3-triazoles is presented by generalized synthetic method.

imidazo[1,2-b]isoquinoline-5,10-dione(CAS# 36142-27 …

Oligonucleotides carrying novel fluorescent compounds with a dipolar isoquinoline imidazo[1,2-]azine core were prepared. Analysis of the melting curves demonstrates that DNA duplexes carrying these fluorescent labels at their ends have a slight increase in DNA duplex stability. The UV absorption and fluorescent properties of the oligonucleotide conjugates were analyzed. The fluorescent label is sensitive to duplex formation, as cooperative melting curves are also observed at 366 nm and fluorescence has a large increase upon denaturation. Cell uptake studies allow observation of these fluorescently labeled oligonucleotides internalized into HeLa cells.

2-(3,4-Dichlorophenyl)imidazo[2,1-a]isoquinoline CAS#:

An efficient 1-difluoromethylation of tetrahydroisoquinolenes was achieved using TMSCF2SPh as a difluoromethylating agent and 2,2,6,6-tetramethylpiperidine-1-oxoammonium tetrafluoroborate (TEMPO+BF4) as an oxidant. The process provides an access to a variety of 1-difluoro(phenylsulfanyl)methylated tetrahydroisoquinoline adducts in good yields. These adducts were employed as key precursors for preparing fluorinated pyrrolo[2,1-]isoquinoline and benzo[]quinolizidines.

EFFICIENT SYNTHESIS OF IMIDAZO[2,1 …

Palladium-catalyzed direct arylation reactions are described with a broad range of azine and azole -oxides. In addition to aspects of functional group compatibility, issues of regioselectivity have been explored when nonsymmetrical azine -oxides are used. In these cases, both the choice of ligand and the nature of the azine substituents play important roles in determining the regioisomeric distribution. When azole -oxides are employed, preferential reaction is observed for arylation at C2 which occurs under very mild conditions. Subsequent reactions are observed to occur at C5 followed by arylation at C4. The potential utility of this methodology is illustrated by its use in the synthesis of a potent sodium channel inhibitor 1 and a Tie2 Tyrosine Kinase inhibitor 2.

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