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090			_aB-11078
245	1	0	_aSynthesis and in vitro antimycobacterial activity of B-ring modi.ed diaryl ether InhA inhibitors
490	0		_vBioorganic & Medicinal Chemistry Letters, 18(10), p.3029-3033, 2008
520	3		_aPrevious structure-based design studies resulted in the discovery of alkyl substituted diphenyl ether inhibitors of InhA, the enoyl reductase from Mycobacterium tuberculosis. Compounds such as 5-hexyl-2-phenoxyphenol 19 are nM inhibitors of InhA and inhibit the growth of both sensitive and isoniazid-resistant strains of Mycobacterium tuberculosis with MIC90 values of 1-2 lg/ mL. However, despite their promising in vitro activity, these compounds have ClogP values of over 5. In e.orts to reduce the lipophilicity of the compounds, and potentially enhance compound bioavailability, a series of B ring analogues of 19 were synthesized that contained either heterocylic nitrogen rings or phenyl rings having amino, nitro, amide, or piperazine functionalities. Compounds 3c, 3e, and 14a show comparable MIC90 values to that of 19, but have improved ClogP values.
700	1	2	_aAm Ende, C.W.
700	1	2	_aKnudson, S.E.
700	1	2	_aLiu, N.
700	1	2	_aChilds, J.
700	1	2	_aSullivan, T.J.
700	1	2	_aBoyne, M.
700	1	2	_aXu, H.
700	1	2	_aXu, H.
700	1	2	_aKnudson, D.L.
700	1	2	_aJohnson, F.
700	1	2	_aPeloquin, C.A.
700	1	2	_aSlaydend, R.A.
700	1	2	_aTonge, P.J.
856	4	0	_uhttps://drive.google.com/file/d/1t_qV-ZLZlTRaJ3qCERC4lT2zQ01fhu-6/view?usp=drivesdk _zPara ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx
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