3514-15-6Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYSNTHESIS FOR BACTERIAL INFECTIONS
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Paragraph 0024; 0025, (2014/09/16)
The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYNTHESIS FOR BACTERIAL INFECTIONS
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Page/Page column 8, (2013/04/10)
The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial Fab I and can be used for the treatment of Staphylococcal infections.
FAB I INHIBITORS
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, (2008/06/13)
Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
Fab I inhibitors
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Page column 17, (2010/02/06)
Compounds of formula (I) and (II) are disclosed wherein, R1, R2, R3, R4, X, A, B, D and Q are as disclosed in the specification, and the compounds are FabI inhibitors useful in the treatment of bacterial infecti
Fab I inhibitors
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Page/Page column 13, (2010/02/07)
Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment of bacterial infections.
Methods of agonizing and antagonizing FabK
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, (2008/06/13)
The invention provides methods for using agonists and antagonists of FabK polypeptides, particularly to modulate the metabolism of bacteria or to treat bacterial infection.
Fab I inhibitors
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, (2008/06/13)
Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: wherein: R1is H, C1-6alkyl or Ar—C0-6alkyl; R2is H, C1-6alkyl, Ar—C0-6alkyl, HO—(CH2)n— or R′OC(O)—(CH2)n—; R3is A—C0-4alkyl, A—C2-4alkenyl, A—C2-4alkynyl, A—C3-4oxoalkenyl, A—C3-4oxoalkynyl, A—C1-4aminoalkyl, A—C3-4aminoalkenyl, A—C3-4aminoalkynyl, optionally substituted by any accessible combination of one or more of R10or R7; R5is H, C1-6alkyl, Ar—C0-6alkyl or C3-6cycloalkyl-C0-6alkyl; A is H, C3-6cycloalkyl, Het or Ar; R7is —COR8, —COCR′2R9, —C(S)R8, —S(O)kOR′, —S(O)kNR′R″, —PO(OR′), —PO(OR′)2, —B(OR′)2, —NO2, or tetrazolyl; R8is —OR′, —NR′R″, —NR′SO2R′, —NR′OR′, or —OCR′2CO(O)R′; R9is —OR′, —CN, —S(O)rR′, —S(O)kNR′2, —C(O)R′, C(O)NR′2, or —CO2R′; R10is H, halo, —OR11, —CN, —NR′R11, —NO2, —CF3, CF3S(O)r—, —CO2R′, —CONR′2, A—C0-6alkyl-, A—C1-6oxoalkyl-, A—C2-6alkenyl-, A—C2-6alkynyl-, A—C0-6alkyloxy-, A—C0-6alkylamino- or A—C0-6alkyl —S(O)r—; R11is R′, —C(O)R′, —C(O)NR′2, —C(O)OR′, —S(O)kR′, or —S(O)kNR′2; R′ is H, C1-6alkyl, Ar—C0-6alkyl or C3-6cycloalkyl-C0-6alkyl; R″ is R′, —C(O)R′ or —C(O)OR′; R′″ is H, C1-6alkyl, Ar—C0-6alkyl, HO-(CH2)2—, R′C(O)—, (R′)2NC(O)CH2— or R′S(O)2—; X is H, C1-4alkyl, OR′, SR′, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, —CN, N(R′)2, CH2N(R′)2, —NO2, —CF3, —CO2R′, —CON(R′)2, —COR′, —NR′C(O)R′, F, Cl, Br, I, or CF3S(O)r—; k is 1 or 2; m is 1, 2 or 3; n is 1 to 6; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI)
Miller, William H.,Seefeld, Mark A.,Newlander, Kenneth A.,Uzinskas, Irene N.,Burgess, Walter J.,Heerding, Dirk A.,Yuan, Catherine C. K.,Head, Martha S.,Payne, David J.,Rittenhouse, Stephen F.,Moore, Terrance D.,Pearson, Stewart C.,Berry, Valerie,DeWolf Jr., Walter E.,Keller, Paul M.,Polizzi, Brian J.,Qiu, Xiayang,Janson, Cheryl A.,Huffman, William F.
, p. 3246 - 3256 (2007/10/03)
Bacterial enoyl-ACP reductase (FabI) catalyzes the final step in each cycle of bacterial fatty acid biosynthesis and is an attractive target for the development of new antibacterial agents. Our efforts to identify potent, selective FabI inhibitors began w
Benzimidazoles/Imidazoles Linked to a Fibrinogen Receptor Antagonist Template Having Vitronectin Receptor Antagonist Activity
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, (2008/06/13)
Vitronectin receptor antagonists having the formula: STR1 which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.
