- Trisubstituted benzene leukotriene B4 receptor antagonists: Synthesis and structure-activity relationships
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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
- Konno, Mitoshi,Nakae, Takahiko,Sakuyama, Shigeru,Odagaki, Yoshihiko,Nakai, Hisao,Hamanaka, Nobuyuki
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p. 1649 - 1674
(2007/10/03)
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- Phenylalkan(en)oic acid
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The phenylalkan(en)oic acids of the formula: STR1 wherein A is i) --NHCO--, ii) --O-- iii) --NHSO2 --, iv) --CO-- v) --CH2 -- or vi) --CH(OH)--; W is i) C1-13 alkylene, ii) phenylene or iii) STR2 R1 is i) hydrogen, ii) C1-4 alkyl, iii) --COOH, iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 member mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group, v) STR3 vi) --CH2 OH; or A, taken together with W and R1, is i) STR4 ii) STR5 iii) --N--(SO2 R6)2, iv) STR6 or v) STR7 two R2 are, same or different, i) hydrogen, ii) C1-4 alkyl or iii) 4-7 membered saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total, or two R2, taken together with a nitrogen to which they are attached, form saturated or unsaturated, i) 7-14 membered, bi- or tri-cyclic hetero ring containing one nitrogen as a hetero atom, or ii) 4-7 mebered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total; Y is ethylene or vinylene; D is i) --Z--B or ii) STR8 Z is C3-11 alkylene or alkenylene R is STR9 or Z taken together with B, is C3-22 alkyl; R3 is i) hydrogen, ii) halogen, iii) C1-8 alkyl, alkoxy or alkylthio, or iv) C2-8 alkenyl, alkenyloxy or alkenylthio; n is 1-3; R4 is C1-7 alkylene; R5 is i) C1-12 alkyl, ii) C2-12 alkenyl, iii) C5-7 cycloalkyl or pp2 iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy; Two R6 are, same or different, i) C1-7 alkyl, ii) benzyl or iii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; and Two R7 are, same or different, C1-4 alky; with the proviso that i) --A--W--R1 should bind to 3- or 4- carbon in benzene ring, and ii) when W phenylene or STR10 A should not represent --O--, --CO--, --CH2 -- or --CH(OH)--; and non-toxic salts thereof, possess an antagonistic activity on leukotriene B4, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B4.
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