171050-01-4Relevant academic research and scientific papers
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
Bicyclic fibrinogen antagonists
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, (2008/06/13)
PCT No. PCT/US95/00248 Sec. 371 Date Jul. 3, 1996 Sec. 102(e) Date Jul. 3, 1996 PCT Filed Jan. 9, 1995 PCT Pub. No. WO96/18619 PCT Pub. Date Jul. 13, 1995Certain compounds within formula (I) are inhibitors of platelet aggregation: wherein A1 is NH or CH2;
Enantiospecific synthesis of SB 214857, a potent, orally active, nonpeptide fibrinogen receptor antagonist
Miller, William H.,Ku, Thomas W.,Ali, Fadia E.,Bondinell, William E.,Calvo, Raul R.,Davis, Larry D.,Erhard, Karl F.,Hall, Leon B.,Huffman, William F.,Keenan, Richard M.,Kwon, Chet,Newlander, Kenneth A.,Ross, Stephen T.,Samanen, James M.,Takata, Dennis T.,Yuan, Chuan-Kui
, p. 9433 - 9436 (2007/10/02)
An enantiospecific synthesis of SB 214857, a potent, nonpeptide fibrinogen receptor antagonist, is reported. The synthetic route employs as a key step an intramolecular aryl fluoride displacement to form the seven-membered ring of the 1,4-benzodiazepine s
