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NATL INST SCIENCE COMMUNICATION; 2003;42(8):1950–7.

T1 - Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors

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The oxazolidinone class of antimicrobials represents a promising advance in the fight against resistant Gram-positive bacterial infections. Four novel oxazolidinone antimicrobial compounds, each containing a benzodioxin ring system, have been prepared. The general synthesis of each compound begins with the construction of a benzodioxin ring system containing a nitro substituent that ultimately becomes the nitrogen of the oxazolidinone ring. Three of the compounds utilize high yielding 'click chemistry' in their final step. The antimicrobial activities of the new oxazolidinones have been measured and the MIC against Staphylococcus aureus for one of the antimicrobials was determined to be 2-3 μg/mL, which is comparable to the well-known oxazolidinone, linezolid.

T1 - Synthesis and antifungal activities of novel 2-aminotetralin derivatives

A series of dialkyl [2-(4,6-dimethoxypyrimidin-2-yloxy)benzamido](aryl) methylphosphonates derivatives were designed and synthesized. All the new compounds were identified by elemental analysis, IR, 1H NMR, 31P NMR, and MS. Their antitumor activity against KB and CNE1 cells was examined. Some of the compounds showed potential antitumor activity, which provided some hints for further study of structure modification. In particular, the compounds 6i and 6j displayed more potent cytotoxic activities against KB in comparison with 5-FU.

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High field proton and carbon NMR spectra for compounds JX001–JX076 and Table S1 ()

N2 - The oxazolidinone class of antimicrobials represents a promising advance in the fight against resistant Gram-positive bacterial infections. Four novel oxazolidinone antimicrobial compounds, each containing a benzodioxin ring system, have been prepared. The general synthesis of each compound begins with the construction of a benzodioxin ring system containing a nitro substituent that ultimately becomes the nitrogen of the oxazolidinone ring. Three of the compounds utilize high yielding 'click chemistry' in their final step. The antimicrobial activities of the new oxazolidinones have been measured and the MIC against Staphylococcus aureus for one of the antimicrobials was determined to be 2-3 μg/mL, which is comparable to the well-known oxazolidinone, linezolid.

AB - The oxazolidinone class of antimicrobials represents a promising advance in the fight against resistant Gram-positive bacterial infections. Four novel oxazolidinone antimicrobial compounds, each containing a benzodioxin ring system, have been prepared. The general synthesis of each compound begins with the construction of a benzodioxin ring system containing a nitro substituent that ultimately becomes the nitrogen of the oxazolidinone ring. Three of the compounds utilize high yielding 'click chemistry' in their final step. The antimicrobial activities of the new oxazolidinones have been measured and the MIC against Staphylococcus aureus for one of the antimicrobials was determined to be 2-3 μg/mL, which is comparable to the well-known oxazolidinone, linezolid.

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The modifications were carried out by introducing ester groups at the C2 position on the skeleton and amino groups at the C11 position (Figure1, Compounds I and II).

The test results showed that in vitro, Compound IIa had higher antiplasmodial activity (IC50) against the NF54 strain than chloroquine and a low cytotoxic activity.
Furthermore, the compounds were tested forβ-haematin inhibition and they were found to be more active than chloroquine and artemisinin.

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    T1 - Synthesis and biological evaluation of novel phosphonates derivatives of as potential antitumor agents

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    T1 - A Novel Synthesis of Benzofuran and Related Compounds. I. The Vilsmeier Reaction of Phenoxyacetonitriles. (共著)

  • Synthesis of Novel Imidazole Compounds and …

    The oxirane of compound 3 is prepared and condensed withCS2 to yield the tricyclic system, thioxothienobenzopyrane21.

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Synthesis of novel anti malarial agents - Okayama University

N2 - Novel 2-aminotetralin derivatives were synthesized as antifungal agents. The 2-aminotetralin scaffold was chemically designed to mimic the tetrahydroisoquinoline ring of the lead molecule described before. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Compounds 10a, 12a, 12c, 13b, and 13d are more potent than fluconazole against seven testing human fungal pathogens. Compound 10b exhibits much higher antifungal activities against all of the four fluconazole-resistant clinic Candida albicans strains than the control drugs including amphotericin B, terbinafine, ketoconazole, and itraconazole. The mode of action of some compounds to the potential receptor lanosterol 14α-demethylase (CYP51) was investigated by molecular docking. The studies presented here provide a new structural type for the development of novel antifungal compounds. Furthermore, 10b was evaluated in vivo by a rat vaginal candidiasis model, and it was found that 10b significantly decreases the number of fungal colony counts.

Synthesis of Novel Bromodifluoromethyl(arylsulfonyl) Compounds

The research group of Assistant Professor Yudai Matsuda and Professor Ikuro Abe at Graduate School of Pharmaceutical Sciences, The University of Tokyo, has identified a new terpene synthase from filamentous fungi that synthesizes a diterpene (terpene consisting of 20 carbon atoms) hydrocarbon with a novel molecular architecture. It is notable that the enzyme has two distinct domains; one is the prenyltransferase (PT) domain synthesizing the 20-carbon linear compound (GGPP) from five-carbon isoprene units, and the other one is the terpene cyclase (TC) domain that cyclizes the linear substrate into the final product. Thus, the terpene synthase is just like the Chimera in Greek mythology as two enzymes are fused as a single protein.

Synthesis and antifungal activity of the novel triazole compounds

AB - Novel 2-aminotetralin derivatives were synthesized as antifungal agents. The 2-aminotetralin scaffold was chemically designed to mimic the tetrahydroisoquinoline ring of the lead molecule described before. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Compounds 10a, 12a, 12c, 13b, and 13d are more potent than fluconazole against seven testing human fungal pathogens. Compound 10b exhibits much higher antifungal activities against all of the four fluconazole-resistant clinic Candida albicans strains than the control drugs including amphotericin B, terbinafine, ketoconazole, and itraconazole. The mode of action of some compounds to the potential receptor lanosterol 14α-demethylase (CYP51) was investigated by molecular docking. The studies presented here provide a new structural type for the development of novel antifungal compounds. Furthermore, 10b was evaluated in vivo by a rat vaginal candidiasis model, and it was found that 10b significantly decreases the number of fungal colony counts.

Design and Synthesis of Novel Antileishmanial Compounds

Although several similar multitasking enzymes have been described prior to this study, an attempt to obtain novel compounds by artificial engineering of this class of terpene synthases has never been reported. Intriguingly, the PT domains of some other chimeric enzymes provide the 25-carbon linear product (GFPP) predominantly instead of the 20-carbon GGPP, which led the researchers to hypothesize that another compound could be obtained by swapping the domain of the PT domain and generating a new Chimera. Consequently, a new cyclized molecule with 25 carbon atoms was successfully produced by exchanging the PT domain into the GFPP synthesizing enzyme.

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