150598-56-4Relevant academic research and scientific papers
Trisubstituted benzene leukotriene B4 receptor antagonists: Synthesis and structure-activity relationships
Konno, Mitoshi,Nakae, Takahiko,Sakuyama, Shigeru,Odagaki, Yoshihiko,Nakai, Hisao,Hamanaka, Nobuyuki
, p. 1649 - 1674 (2007/10/03)
A series of trisubstituted benzenes which demonstrate leukotriene B4 (LTB4, 1) receptor affinity was prepared. Previous trisubstituted benzenes from our laboratory showed high affinity to the LTB4 receptor but demonstrated
CARBOXYLIC ACID LEUKOTRIENE B4 ANTAGONISTS
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, (2008/06/13)
Compounds of the formula STR1 wherein X is O or CH 2 ; Y is O,--CH 2--CH 2,--CH=CH--,--C C--, or--OCH 2 C 6 H 4--;Z is--CH 2--CH 2--,--CH=CH--or--C C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12; R 1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; andA is B or--O--B, wherein B is a mono-, di-or tricyclic aromatic or heteroaromatic moiety substituted by the group--COR 2,--(O) t--(W) s--COR 2 or--(CH=CH) p COR 2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl,--(Q) k--(W) s'--E or--(Q) k--(W) s"--C 6 H 4--(W) s'"--E, provided that no more than one of said substituents is--(Q) k--(W) s'--E or--(Q) k--(W). sub.s"--C 6 H 4--(W) s'"--E, and wherein E is COR 2 or R 2, W is--CR 3 R 4--, Q is O or carbonyl, p is an integer from 1 to 2, s and s', independently, are an integer from 1-12, s" and s'", independently, are an integer from 0 to 12, C 6 H 4 is a 1,2-, 1,3-, or 1,4-phenylene moiety, and R 2 is hydroxy, lower alkoxy or NR 3 R 4, wherein R 3 and R 4, each occurrence, independently, are hydrogen or lower alkyl,their geometric and optical isomers and, when R 2 is hydroxy, pharmaceutically acceptable salts thereof with bases. The compounds of formula I are potent leukotriene B 4 antagonists and are therefore useful in the treatment of inflammatory diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, ischemia/reperfusion injury, and trauma induced inflammation, such as spinal cord injury. "
