Antimycobacterial activity of 2-methyl-adenosine.
J Antimicrob Chemother. 2003.
PMID: 14563890
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Antimycobacterial activity of 2-methyl-adenosine.
J Antimicrob Chemother. 2003 Nov;52(5):801-8. doi: 10.1093/jac/dkg444. Epub 2003 Oct 16.
J Antimicrob Chemother. 2003.
PMID: 14563890
A hypoxic shift-down model was used to evaluate the effect of 2-methyl-adenosine on M. tuberculosis in a persistent state. Mechanism-of-action studies were conducted by examining the effect of 2-methyl-adenosine on the uptake of appropria …
A hypoxic shift-down model was used to evaluate the effect of 2-methyl-adenosine on M. tuberculosis in a persistent sta …
A synthetic antibiotic class overcoming bacterial multidrug resistance.
Nature. 2021 Nov;599(7885):507-512. doi: 10.1038/s41586-021-04045-6. Epub 2021 Oct 27.
Nature. 2021.
PMID: 34707295
Free PMC article.
When properly designed, fully synthetic routes can easily address these shortcomings(2). Here we report the structure-guided design and component-based synthesis of a rigid oxepanoproline scaffold which, when linked to the aminooctose residue of clindamycin, produces an an …
When properly designed, fully synthetic routes can easily address these shortcomings(2). Here we report the structure-guided design a …
2-Substituted 6-(Het)aryl-7-deazapurine Ribonucleosides: Synthesis, Inhibition of Adenosine Kinases, and Antimycobacterial Activity.
ChemMedChem. 2015 Jun;10(6):1079-93. doi: 10.1002/cmdc.201500081. Epub 2015 Apr 16.
ChemMedChem. 2015.
PMID: 25882678
A series of 6-(hetero)aryl- or 6-methyl-7-deazapurine ribonucleosides bearing a substituent at position 2 (Cl, F, NH2, or CH3) were prepared by cross-coupling reactions at position 6 and functional group transformations at position 2. ...The antimycobacter …
A series of 6-(hetero)aryl- or 6-methyl-7-deazapurine ribonucleosides bearing a substituent at position 2 (Cl, F, NH2, or CH3) …
The interactions of nitric oxide and adenosine on penicillin-induced epileptiform activity in rats.
Acta Neurobiol Exp (Wars). 2011;71(2):208-19.
Acta Neurobiol Exp (Wars). 2011.
PMID: 21731075
Free article.
In this study, the influence of nitric oxide (NO) and adenosine systems on penicillin-induced epileptiform activity was examined in rats. ...The obtained results suggest that NO and adenosine may decrease penicillin-induced epileptiform activity in rat …
In this study, the influence of nitric oxide (NO) and adenosine systems on penicillin-induced epileptiform activity was examin …
Antiplatelet activity of BRX-018, (6aS,cis)-malonic acid 3-acetoxy-6a9-bis-(2-methoxycarbonyl-acetoxy)-6,6a,7,11b-tetrahydro-indeno[2,1-c]chromen-10-yl ester methylester.
Thromb Res. 2005;115(4):309-18. doi: 10.1016/j.thromres.2004.09.018. Epub 2004 Oct 27.
Thromb Res. 2005.
PMID: 15668191
Brazilin (7,11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10 (6H)-tetrol), the major component of Caesalpinia sappan L., was reported to show antiplatelet activity through the inhibition of phospholipase A2 (PLA2) activity and the increase in intracellular free …
Brazilin (7,11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10 (6H)-tetrol), the major component of Caesalpinia sappan L., was reported t …
Anticonvulsant doses of 2-chloro-N6-cyclopentyladenosine, an adenosine A1 receptor agonist, reduce GABAergic transmission in different areas of the mouse brain.
J Pharmacol Exp Ther. 1993 Nov;267(2):844-51.
J Pharmacol Exp Ther. 1993.
PMID: 8246158
The possible relationship between A1 adenosine receptors and the gamma-aminobutyric acid (GABAA) receptor complex was evaluated in the mouse brain. ...CCPA (2.8-8.3 mumol/kg i.p.) antagonized the convulsions induced by pentylenetetrazol (398 mumol/kg i.p.), methy …
The possible relationship between A1 adenosine receptors and the gamma-aminobutyric acid (GABAA) receptor complex was evaluated in th …
Structure-activity relationship for nucleoside analogs as inhibitors or substrates of adenosine kinase from Mycobacterium tuberculosis. I. Modifications to the adenine moiety.
Biochem Pharmacol. 2006 Jun 14;71(12):1671-82. doi: 10.1016/j.bcp.2006.03.006. Epub 2006 Mar 10.
Biochem Pharmacol. 2006.
PMID: 16620788
Adenosine kinase (Ado kinase, EC 2.7.1.20) is a purine salvage enzyme that phosphorylates adenosine (Ado) to AMP. Ado kinase from Mycobacterium tuberculosis also catalyzes an essential step in the conversion of 2-methyl-Ado to a compound with se …
Adenosine kinase (Ado kinase, EC 2.7.1.20) is a purine salvage enzyme that phosphorylates adenosine (Ado) to AMP. Ado k …
Purine metabolism in Mycobacterium tuberculosis as a target for drug development.
Curr Pharm Des. 2007;13(6):599-608. doi: 10.2174/138161207780162863.
Curr Pharm Des. 2007.
PMID: 17346177
Review.
We have identified several purine nucleoside analogs that exhibit selective activity against Mycobacterium tuberculosis. The lead compound in this series is 2-methyl-adenosine (methyl-Ado), which is active against proliferating and nonpro …
We have identified several purine nucleoside analogs that exhibit selective activity against Mycobacterium tuberculosis. The lead com …
Structural basis of O-methylation of (2-heptyl-)1-hydroxyquinolin-4(1H)-one and related compounds by the heterocyclic toxin methyltransferase Rv0560c of Mycobacterium tuberculosis.
J Struct Biol. 2021 Dec;213(4):107794. doi: 10.1016/j.jsb.2021.107794. Epub 2021 Sep 21.
J Struct Biol. 2021.
PMID: 34506908
Structural and biochemical data suggest that H139 and T136 are key active site residues, with H139 acting as general base that activates the methyl-accepting hydroxy group. Our structural data may contribute to the design of Htm inhibitors or of antimycoba …
Structural and biochemical data suggest that H139 and T136 are key active site residues, with H139 acting as general base that act …
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
J Med Chem. 1988 Jun;31(6):1179-83. doi: 10.1021/jm00401a018.
J Med Chem. 1988.
PMID: 3373486
In a search for more selective A1 adenosine receptor agonists, N6-[(R)-(-)-1-methyl-2-phenethyl]-1-deazaadenosine (1-deaza-R-PIA, 3a), N6-cyclopentyl-1-deazaadenosine (1-deazaCPA, 3b), N6-cyclohexyl-1-deazaadenosine (1-deazaCHA, 3c), and the corresponding …
In a search for more selective A1 adenosine receptor agonists, N6-[(R)-(-)-1-methyl-2-phenethyl]-1-deazaadenosine (1-de …
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