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3 azolopyridine ureas as a novel scaffold with antitubercular activity acting through inhibition of DNA
4 esulted in compounds with moderate to potent antitubercular activity and improved physicochemical pro
6 Mycobacterium tuberculosis RNAP but lowered antitubercular activity in cell culture under both aerob
7 A inhibitors disclosed here display in vitro antitubercular activity superior to most current first l
8 ructure-activity relationships lining up the antitubercular activity were exploited for the rational
9 derivative 26 exhibited exceptionally potent antitubercular activity with an MIC99 under iron-deficie
10 assessed for biochemical potency, whole-cell antitubercular activity, and in vivo pharmacokinetic par
21 icals found with KatG, while the less potent antitubercular agent nicotinic acid hydrazide produced t
22 -carboxamide analogue, 3, as a highly potent antitubercular agent, and the subsequent chemical modifi
25 (Sal-AMS) is a prototype for a new class of antitubercular agents that inhibit the aryl acid adenyla
26 red the discovery of a novel class of potent antitubercular agents that unexpectedly possessed notabl
27 re a promising class of potent and selective antitubercular agents, if the metabolic liability can be
28 rotein and a validated target to develop new antitubercular agents, particularly for the treatment of
29 rotein and a validated target to develop new antitubercular agents, particularly for the treatment of
35 vely explored for their potential use as new antituberculars based on their excellent bactericidal pr
36 unction with isoniazid, but removed from the antitubercular chemotherapeutic arsenal due to toxic sid
44 sis is responsible for the activation of the antitubercular drug isonicotinic acid hydrazide (INH) an
45 s is inhibited by isoniazid, a key frontline antitubercular drug that is inactivated by mycobacterial
46 s the efficacy of ethionamide, a second-line antitubercular drug used to combat multidrug-resistant M
48 erium marinum to thiacetazone, a second line antitubercular drug, is associated with a severe decreas
50 e for increased resistance to the front-line antitubercular drug, isoniazid, by acetylating and hence
52 e originally been designed as hybrids of the antitubercular drugs BM212 (1) and SQ109 (2), which show
53 g pocket of Eis is a potential target of new antitubercular drugs expected to overcome aminoglycoside
55 ween these two components was provided using antitubercular drugs such as ethambutol or isoniazid kno
56 osis highlights the need for identifying new antitubercular drugs that can treat these infections.
58 ly) TB; hence the quest for highly effective antitubercular drugs with novel modes of action is imper
59 ation issues, including interactions between antitubercular drugs, antiretroviral drugs, and medicine
75 s of structure 1, previously assigned to the antitubercular marine natural product pseudopteroxazole,
76 acene-6,11,13-trione (1), proposed to be the antitubercular natural product eucapsitrione, has been s
85 p from initiation of treatment that included antitubercular therapy (ATT) with oral corticosteroids (
87 y virus (HIV)-infected patients on RIF-based antitubercular therapy in the French National Agency for
88 s in well-validated biosynthetic pathways in antitubercular therapy is a powerful strategy that remov
89 specific efflux pump inhibitors to standard antitubercular therapy should shorten the duration of cu
92 lu-Natal, South Africa, who received minimal antitubercular treatment and most of whom were HIV serop
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