2019
DOI: 10.1002/asia.201801805
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Synthesis and Investigation of Phthalazinones as Antitubercular Agents

Abstract: A series of 2‐ and 7‐substituted phthalazinones was synthesised and their potential as anti‐tubercular drugs assessed via Mycobacterium tuberculosis (mc26230) growth inhibition assays. All phthalazinones tested showed growth inhibitory activity (MIC <100 μm), and those compounds containing lipophilic and electron‐withdrawing groups generally exhibited better anti‐tubercular activity. Several lead compounds were identified, including 7‐((2‐amino‐6‐(4‐fluorophenyl)pyrimidin‐4‐yl)amino)‐2‐heptylphthalazin‐1(2H)‐o… Show more

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Cited by 9 publications
(4 citation statements)
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“…The hit 30 is a phthalazin‐1(2H)‐one derivative. The phthalazin‐1(2H)‐one derivatives possess a variety of bioactivities, such as antibacterial, 43 antitubercular, 44 antinociceptive, 45 and anticancer 46,47 activities. The interaction between the active site residues of tubulin and the two hits was analyzed, and further compared with standard drug paclitaxel.…”
Section: Resultsmentioning
confidence: 99%
“…The hit 30 is a phthalazin‐1(2H)‐one derivative. The phthalazin‐1(2H)‐one derivatives possess a variety of bioactivities, such as antibacterial, 43 antitubercular, 44 antinociceptive, 45 and anticancer 46,47 activities. The interaction between the active site residues of tubulin and the two hits was analyzed, and further compared with standard drug paclitaxel.…”
Section: Resultsmentioning
confidence: 99%
“…Abdelgawad and co-workers synthesized a series of phthalazone-tethered 1,2,3-triazole derivatives 517-518 by click cycloaddition reaction of alkyne-functionalized phthalazone 516 with different functionalized azides [169][170][171][172][173] in the presence of CuSO 4• 5H 2 O, sodium ascorbate and tris(benzyltriazolylmethyl)amine in H 2 O/tBuOH/CH 2 Cl 2 (Scheme 52). 174 Compounds 517-518 were tested for their biological activity and compound 518 was found to have antiproliferative activity.…”
Section: Scheme 51 Synthesis Of Compounds 515a-zjmentioning
confidence: 99%
“…Specifically, as the synthesis of 3‐unsubstituted phthalides is regarded, the representative synthetic methods include cyclocarbonylation of ortho ‐halobenzyl alcohol, [ 5 ] oxidation of phthalyl alcohol, [ 6 ] Cannizzaro‐type lactonization of dialdehyde, [ 7 ] reduction of phthalic anhydride, [ 8 ] oxidative annulation of ortho ‐methyl benzoic acid, [ 9 ] [2+2+2] cycloaddition of 1,6‐diyne, [ 10 ] and so on (Scheme 1a). Normally, in these reactions, advanced functionalized substrates are demanded.…”
Section: Figurementioning
confidence: 99%