141580-53-2Relevant academic research and scientific papers
PYRIDINE DERIVATIVE SUBSTITUTED BY HETEROARYL RING, AND ANTIFUNGAL AGENT COMPRISING THE SAME
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Page/Page column 103, (2009/06/27)
The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability. The present invention discloses a compound represented by the following formula I or a salt thereof, and an antifungal agent comprising the compound or the salt: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6-alkoxy-C1-6-alkyl group; R2 represents a hydrogen atom or an amino group; X, Y, Z, and W independently represent a nitrogen atom, an oxygen atom, a sulfur atom, or -CH-, provided that at least two among X, Y, and W are nitrogen atoms; the ring A represents a 5- or 6-membered heteroaryl ring or a benzene ring; Q represents a methylene group, an oxygen atom, -CH2O-, -OCH2-, -NH-, -NHCH2-, or -CH2NH-; and R3 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, or a 5- or 6-membered heteroaryl group, each of which may have one or two substituents.
Synthesis of A-79175: A second generation 5-lipoxygenase inhibitor
Dickman, Daniel A.,Ku, Yi-Yin,Morton, Howard E.,Chemburkar, Sanjay R.,Patel, Hemantkumar H.,Thomas, Albert,Plata, Daniel J.,Sawick, David P.
, p. 1791 - 1795 (2007/10/03)
A convergent, high yielding, and scalable synthesis of A-79175, with a key step involving a mild and efficient Cu-Pd catalyzed coupling reaction of a terminal acetylene with a substituted 2-iodofuran is discussed.
Lipoxygenase and cyclooxygenase inhibiting compounds
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, (2008/06/13)
Compounds having the structure STR1 or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B4, C4, D4, and E4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R1 and R2 are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z--COOH.
ACETYLENE DERIVATIVES HAVING LIPOXYGENASE INHIBITORY ACTIVITY
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, (2008/06/13)
Compounds of the structure where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR1 R2, where R1 and R2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
N-SUBSTITUTED-FURYLALKENYL HYDROXAMIC ACID AND N-HYDROXYUREA COMPOUNDS HAVING LIPOXYGENASE INHIBITORY ACTIVITY
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, (2008/06/13)
Compounds useful in inhibiting the biosynthesis of leukotrienes have the structure where M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group, R4 is alkyl, cycloalkyl or -NR5R6, where R5 and R6 are hydrogen, alkyl, cyclo
