Antimicrobial determination of N-(aminoalkyl) and/or N-(Amidoalkyl) dinitrogen heterocyclic compositions
AssigneeIsis Pharmaceuticals, Inc.
InventorsPhillip Dan Cook, Andrew M. Kawasaki, Pei Pei Kung
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Abstract
Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The compounds and compositions of the invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents including employment as species for effecting combinatorial synthesis.
Claims25
A method of identifying a compound having antimicrobial activity comprising:
- preparing a composition comprising at least three compounds, each of said compounds having the formula:
- ##STR26## wherein each p is independently 0, 1 or 2;
- each x and y are independently 1, 2 or 3;
- each Q.sub.1 is independently --N(R.sub.15)--, --O-- or --S--;
- each R.sub.2 is hydrogen, C.sub.1 -.sub.6 alkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.20 alkaryl, pyran, pyrrolidone, benzothiazole, pyridine, benzoxazole, piperidine, piperazine, furan thiofuran pyrimidine, carbazole, or a moiety of the formula --(CH.sub.2).sub.m --R.sub.3 -R.sub.4 where:
- each m is 0 or 1;
- each R.sub.3 is --CH.sub.2 --, --C(.dbd.O)-- or --C(.dbd.S)--;
- and
- each R.sub.4 is --O--R.sub.5, C.sub.1 -C.sub.6 alkyl, C.sub.6 -C.sub.15 aryl or pyran, pyrrolidone, benzothiazole, pyrdine, benzoxazole, piperidine, piperazine, furan, thiofuran, pyrimidine, carbazole, where R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.6 -C.sub.15 aryl, C.sub.3 -C.sub.12 cycloalkyl, pyran, pyrrolidone, benzothiazole, pyridine, benzoxazole, piperidine, piperazine, furan, thiofuran, pyrimidine, carbazole or C.sub.7 -C.sub.20 alkaryl;
- each R.sub.11 is independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.20 alkaryl, C.sub.6 -C.sub.20 aryl, pyran, pyrrolidone, benzothiazole, pyridine, benzoxazole, piperidine, piperazine, furan, thiofuran, pyrimidine, carbazole or C.sub.3 -C.sub.20 cycloalkyl;
- each R.sub.12 is independently --CH.sub.2 -- or --C(.dbd.O)--;
- and
- each R.sub.15 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;
- assaying said composition to determine at least one biological activity of said plurality of compounds;
- and
- identifying which of said compounds contribute to said activity.
Dependencies are inferred from the claim text.