Emanuele Perola
Overview
Explore the profile of Emanuele Perola including associated specialties, affiliations and a list of published articles.
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25
Citations
857
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Recent Articles
11.
Grillot A, Le Tiran A, Shannon D, Krueger E, Liao Y, ODowd H, et al.
J Med Chem
. 2014 Oct;
57(21):8792-816.
PMID: 25317480
Compound 3 is a potent aminobenzimidazole urea with broad-spectrum Gram-positive antibacterial activity resulting from dual inhibition of bacterial gyrase (GyrB) and topoisomerase IV (ParE), and it demonstrates efficacy in rodent...
12.
Clark M, Ledeboer M, Davies I, Byrn R, Jones S, Perola E, et al.
J Med Chem
. 2014 Jul;
57(15):6668-78.
PMID: 25019388
In our effort to develop agents for the treatment of influenza, a phenotypic screening approach utilizing a cell protection assay identified a series of azaindole based inhibitors of the cap-snatching...
13.
Perola E, Stamos D, Grillot A, Ronkin S, Wang T, LeTiran A, et al.
Bioorg Med Chem Lett
. 2014 Apr;
24(9):2177-81.
PMID: 24685546
A series of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV were identified and optimized to mid-to-low nanomolar potency against a variety of bacteria. However, in spite of...
14.
Gu W, Wang T, Maltais F, Ledford B, Kennedy J, Wei Y, et al.
Bioorg Med Chem Lett
. 2012 May;
22(11):3693-8.
PMID: 22560473
A series of 2,6-disubstituted aminoalkoxypyrimidine carboxamides (AAPCs) with potent inhibition of bacterial NAD(+)-dependent DNA ligase was discovered through the use of structure-guided design. Two subsites in the NAD(+)-binding pocket were...
15.
Wang T, Duncan L, Gu W, ODowd H, Wei Y, Perola E, et al.
Bioorg Med Chem Lett
. 2012 May;
22(11):3699-703.
PMID: 22560470
A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD(+)-dependent DNA ligase that possess potency against Gram-positive bacteria.
16.
Perola E, Herman L, Weiss J
J Chem Inf Model
. 2012 Mar;
52(4):1027-38.
PMID: 22448735
Target selection is a critical step in the majority of modern drug discovery programs. The viability of a drug target depends on two components: biological relevance and chemical tractability. The...
17.
Perola E
J Med Chem
. 2010 Mar;
53(7):2986-97.
PMID: 20235539
In order to investigate the evolution of binding efficiency in successful drug discovery programs, a data set of 60 lead/drug pairs with known binding affinities has been compiled and analyzed....
18.
Charifson P, Grillot A, Grossman T, Parsons J, Badia M, Bellon S, et al.
J Med Chem
. 2008 Aug;
51(17):5243-63.
PMID: 18690678
The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA...
19.
Bandarage U, Wang T, Come J, Perola E, Wei Y, Rao B
Bioorg Med Chem Lett
. 2007 Dec;
18(1):44-8.
PMID: 18054488
A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in...
20.
Rao B, Bandarage U, Wang T, Come J, Perola E, Wei Y, et al.
Bioorg Med Chem Lett
. 2007 Feb;
17(8):2250-3.
PMID: 17289381
A series of potent thiol-containing aryl sulfonamide TACE inhibitors was designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 4b has shown excellent...