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DTIC ADA184479: The Design, Synthesis and Screening of Potential Py... |
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by Defense Technical Information Center |
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In an attempt to improve the delivery a quaternary |
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pyridinium oxime regenerators of acetycholinesterase |
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(AChE) to the central nervous system (CNS), structural |
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analogs (I) and potential prodrugs (II) of N-methyl- |
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pyridinium 2-carbaldoxime (2-PAM) have been synthesized. |
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The potential prodrugs are dihydropyridinium oximes (pro- |
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2-PAM's), which posses electron withdrawing substituents |
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in the 3- or 5-position. As precursors to these prodrugs, |
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we have synthesized and characterized this year a series |
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of 5-substituted-2-PAM's (C1, CH3, CN, COHN2 substituted) |
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and a series of 3-substituted-2-PAM's (Br, C1, CH3 |
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substituted). These new analogs and the 5-substituted 2- |
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PAM's (I, Br substituted) and 3-substituted-2-PAM (I |
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substituted) synthesized last year were tested in vitro |
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for their ability to reactivate |
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diisopropylfluorophosphate (DEP)-inactivated AChE, in |
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vivo for their ability to protect mice from a challenge |
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dose (2 X LD50) of DFP and, and in vivo for their ability |
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to protect mice from a challenge dose (2x LD50) of Soman. |
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Date Published: 2018-02-16 01:42:15 |
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Identifier: DTIC_ADA184479 |
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Item Size: 42320560 |
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Language: english |
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Media Type: texts |
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# Topics |
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DTIC Archive; Borchardt,Ronald T ; KA... |
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