- THROMBIN INHIBITORS
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y 1 or O; c is CY 2 or N; d is CY 2; e is CY 1 or N; f is CY 1 or N; g is CY 1 or N; Y 1 is hydrogen, C 1-4 alkyl, or halogen; Y 2 is hydrogen, C 1-4 alkyl, C 3-7 cycloalkyl, halogen, NH 2, OH or C 1-4 alkoxy;A is and W, X, Z, R 3, R 4 and R 5 are defined in the specification.
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- Synthesis of 2,4-Diamino-6-(thioarylmethyl)pyrido[2,3-d]pyrimidines as dihydrofolate reductase inhibitors
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Six 2,4-diaminopyrido[2,3-d]pyrimidines with a 6-merhylthio bridge to an aryl group were synthesize and biologically evaluate as inhibitors of Pneumocystis carinii (pc) and Toxoplasma gondii (tg) dihydrofolate reductase (DHFR). The syntheses of analogues
- Gangjee, Aleem,Adair, Ona,Queener, Sherry F.
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p. 2929 - 2935
(2007/10/03)
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- Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from pneumocystis carinii
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A series of lipophilic soft drugs structurally related to the nonclassical dihydrofolate reductase (DHFR) inhibitors trimetrexate and piritrexim have been designed, synthesized, and evaluated in DHFR assays, with special emphasis on the inhibition of P. c
- Graffner-Nordberg,Kolmodin,?qvist,Queener,Hallberg
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p. 2391 - 2402
(2007/10/03)
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- Synthesis of substituted 2-aminonicotinonitriles
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Mono-, di-, and trisubstituted 2-aminonicotinonitriles 8, 13, 14, and 19 are prepared from ketonic Mannich-bases hydrochlorides 4 · HCl, enones 12, β-aminovinylketones 17, 3-aminoacroleines 18, vinamidinium perchlorates 21, and 3,3-diaminoacrylonitrile (3
- Troschutz,Dennstedt
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- 5-methyl-5-deaza analogues of methotrexate and N10 -ethylaminopterin
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It is disclosed that 5-methyl-5-deazamethotrexate and 5-methyl-5-deaza-10-ethylaminopterin are more than 10 times as potent as 5-deazamethotrexate in the L1210 cell growth inhibition test.
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- Syntheses and Antifolate Activity of 5-Methyl-5-deaza Analogues of Aminopterin, Methotrexate, Folic Acid, and N10-Methylfolic Acid
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Evidence indicating that modifications at the 5- and 10-positions of classical folic acid antimetabolites lead to compounds with favorable differential membrane transport in tumor vs. normal proliferative tissue prompted an investigation of 5-alkyl-5-deaz
- Piper, J. R.,McCaleb, G. S.,Montgomery, J. A.,Kisliuk, R. L.,Gaumont, Y.,Sirotnak, F. M.
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p. 1080 - 1087
(2007/10/02)
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