Studies on acyclic pyrimidines as inhibitors of mycobacteria

Srivastav, Naveen C.; Manning, Tracey; Kunimoto, Dennis; Kumar, Rakesh K.

doi:10.1016/j.bmc.2006.12.032

Cited by 37 publications

(43 citation statements)

References 20 publications

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“…The 5-aminouracil has been used as a starting material for the synthesis of other pyrimidines [2] or transition metal complexes [3]. The 1-[(2-hydroxyethoxy)methyl]-5-aminouracil exhibited anti-mycobacterium activity against mycobacterium bovis [4].…”

Section: Introductionmentioning

confidence: 99%

Experimental study on the thermochemistry of some amino derivatives of uracil

Silva

Amaral

Szterner

2011

The Journal of Chemical Thermodynamics

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Section: Introductionmentioning

confidence: 99%

Experimental study on the thermochemistry of some amino derivatives of uracil

Silva

Amaral

Szterner

2011

The Journal of Chemical Thermodynamics

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“…Similar activity was retained with the introduction of a 1-[(2-hydroxy-1-(hydroxymethoxy)ethoxy) methyl] moiety as acyclic sugar analog and 5-decynyl Figure 13C) [121].…”

Section: Nucleoside Analogs With Unclear Targetmentioning

confidence: 86%

“…Within this new series, compounds bearing different 5-(1-azido-2-haloethyl)-substituents (61-63) on the common 1-(2-hydroxyethoxy)methyl uracil scaffold, were reported to be endowed with moderate activity against M.tb (MIC 50 = 10 μg/ml) ( Figure 13C) [121]. Similar activity was retained with the introduction of a 1-[(2-hydroxy-1-(hydroxymethoxy)ethoxy) methyl] moiety as acyclic sugar analog and 5-decynyl Figure 13C) [121].…”

Section: Nucleoside Analogs With Unclear Targetmentioning

confidence: 96%

“…In an attempt to introduce further variability in the nucleoside scaffold, Kumar et al decided to synthesize nucleoside analogs in which the cyclic carbohydrate moiety is replaced with open-chain 'acyclic sugar moieties' [121]. Compounds with similar structure already proved to be effective therapeutic agents, possibly due to the ability of the acyclic side chain to mimic the interactions of the glycosyl portion with the putative target, although retaining flexibility [122].…”

Section: Nucleoside Analogs With Unclear Targetmentioning

confidence: 99%

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Nucleoside Analogs and Tuberculosis: New Weapons Against an Old Enemy

Ferrari

Serpi

2015

Future Med. Chem.

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Purine and pyrimidine nucleoside and nucleotide analogs have been extensively studied as anticancer and antiviral agents. In addition to this, they have recently shown great potential against Mycobacterium Tuberculosis, the causative agent of TB. TB ranks as the tenth most common cause of death in the world. The current treatment for TB infection is limited by side effects and cost of the drugs and most importantly by the development of resistance to the therapy. Therefore the development of novel drugs, capable of overcoming the drawbacks of the existing treatments, has become the focus of many research programs. In parallel to that, a tremendous effort has been made to elucidate the unique metabolism of this pathogen with the aim to identify new possible targets. This review presents the state of the art in nucleoside and nucleotide analogs in the treatment of TB. In particular, we report on the inhibitory activity of this class of compounds, both in enzymatic and whole-cell assays, providing a brief insight to which reported target these novel compounds are hitting.

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“…The model of a neutron here of interest [4,5] in what follows consists of a ud diquark at one end of a string of length L and tension τ and a u quark at the other end of the string. The mean electric dipole moment strength is thereby…”

Section: Figmentioning

confidence: 99%

Electric dipole moments and polarizability in the quark-diquark model of the neutron

et al. 2010

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For a bound state internal wave function respecting parity symmetry, it can be rigorously argued that the mean electric dipole moment must be strictly zero. Thus, both the neutron, viewed as a bound state of three quarks, and the water molecule, viewed as a bound state of ten electrons two protons and an oxygen nucleus, both have zero mean electric dipole moments. Yet, the water molecule is said to have a nonzero dipole moment strength d = eΛ with ΛH 2 O ≈ 0.385Ȧ. The neutron may also be said to have an electric dipole moment strength with Λneutron ≈ 0.612 f m. The neutron analysis can be made experimentally consistent, if one employs a quark-diquark model of neutron structure.

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Studies on acyclic pyrimidines as inhibitors of mycobacteria

Cited by 37 publications

References 20 publications

Experimental study on the thermochemistry of some amino derivatives of uracil

Experimental study on the thermochemistry of some amino derivatives of uracil

Nucleoside Analogs and Tuberculosis: New Weapons Against an Old Enemy

Electric dipole moments and polarizability in the quark-diquark model of the neutron

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