摘要:
Diamidine derivatives of formula (I) and their salts are new. Amidine derivatives of formula (I) and their salts are new. [Image] X : a group of formula (ii) or R 4; Z : -(CH 2) m-; m : 8 - 21; n : 0 or 1; Y : R 3 or a group of formula (iii); R 1 and R' 1H, alkyl, aryl, OH, O-alkyl, O-aryl, OCO-alkyl, OCO-aryl, O-CO-O-(or S or NH)-alkyl, O-CO-O-(or S or NH)-aryl, PO-(O-alkyl or O-aryl) 2, CO-O-CH 2-aryl, or cycloalkyl; R 2 and R' 2H, alkyl, CO-O-CH 2-aryl, CO-O-alkyl, or cycloalkyl; R 3 and R' 3H, alkyl, aryl, CO-O-alkyl, CO-O-aryl, COO-CH(R)-O-CO-alkyl, PO(O-alkyl, or O-aryl, or ONa) 2, or CO-O-CH(R)-aryl; R : H or alkyl; NR 1R 2, NR' 1R' 2, NR 2R 3, NR' 2R' 3a heterocycle, in which R 2 and R 3 and/or R' 2 and R' 3 may be doubly bonded to the nitrogen atom; R 4 and R' 4H or alkyl; R 1R 4, R' 1R' 4-(CH 2) p-; R 4R 2, R' 4R' 2-(CH 2) p; p : 3 - 5; and provided that: (1) when X is a group of formula (ii), then Y is R 3; and (2) when X is R 4, then Y is a group of formula (iii). [Image] Independent claims are also included for the preparation of compounds of formulae (V), (X), (VI) and (VIII). [Image] R anot defined. ACTIVITY : Protozoacide. 1,12-bis(imidazolin-2-yl) dodecane (Ib) was given orally and intraperitoneally to mice infected with Plasmodium vinckei. The dose that cleared 50 % of the infection (ED50) was 3.4 mg/kg i.p and 62 mg/kg p.o. MECHANISM OF ACTION : Not given in source material.
摘要:
PROBLEM TO BE SOLVED: To provide a method for forming guanidine groups not chelate-reacting with metal cations existing in solutions on a carbon nanotube, and to provide a method for forming guanidine groups on a carbon nanotube as a method for more increasing the dispersibility of carbon nanotube. SOLUTION: A method for attaching carbon nanotubes having guanidine groups formed thereon to a substrate comprises a step for coating the substrate with a crown ether-having polymer, a step for drying the crown ether-having polymer layer coated on the substrate in a semi-dry state, and a step for coating the semi-dry polymer layer with a solution containing the carbon nanotubes having the guanidine groups formed thereon. The carbon nanotubes having the guanidine groups formed thereon and produced by the method are uniformly dispersed in solutions by the hydrogen bond of the guanidine groups to the hydrogen bond-formable solvent molecules. The guanidine groups are selectively bound to the crown ether, and the property is utilized to vertically arrange the carbon nanotubes having the guanidine groups formed thereon on the substrate at a constant distance. COPYRIGHT: (C)2006,JPO&NCIPI
摘要:
PROBLEM TO BE SOLVED: To obtain a new compound capable of inhibiting matrix metalloproteinases derived from vertebrates or a tumor necrosis factor-α converting enzyme, and excellent in biological activity such as oral absorptivity. SOLUTION: This compound is represented by formula I [R1 is H, a (substituted) aralkyl or the like; R2 is H, a (substituted) aralkyloxycarbonyl or the like; R3 is H, a (substituted) alkyl or the like; R4 is a (substituted) alkyl or the like; R5 and R6 are each H, a (substituted) alkyl or the like; R7 is H, a (substituted) alkyl or the like; R8 is H, a (substituted) alkyl or the like; R9 is H, OH, amino or the like], e.g. Na-t-butyloxycarbonyl-Ne-benzyloxycarbonyl-L- lysine N-methylamide. The compound represented by formula I is obtained by converting an ester site of a compound represented by formula II into an amide bond-containing site and, as desired, respectively converting groups R11 and R14 (R11 is the same meaning as that of R3 or the like; R12 has the same meaning as that of R4 or the like; R13 has the same meaning as that of R5 or the like; R14 has the same meaning as that of R9 or the like) into the groups R3 to R5 and R9.
摘要:
PROBLEM TO BE SOLVED: To obtain a new compound useful as an organic base precursor having the rapidity of producing a base at the time of heating compatible with the stability during the preservation. SOLUTION: This compound is represented by formula I [R to R are each H, an alkyl, an alkenyl, an aralkyl or an aryl; Z is a substituent group having a value of σ of >=0 when defined by the Hammett's equation; [(i)+(j)] is 3 and (i) is 1 or 2] or formula II (R to R are each same as R to R ), e.g. a compound represented by formula III. The compound represented by formula I is obtained by charging stearylamine, triethylamine and chloroform into a flask equipped with a stirrer, dropping 1.5 g of 1-chloro-2-methyl-2-propyl chloroformate thereinto under cooling with ice, continuing the stirring for 2 hr, then diluting the reactional solution with chloroform, washing the diluted reactional solution with water, dehydrating the washed solution, subsequently distilling off the chloroform under a reduced pressure and recrystallizing the prepared colorless powder from a mixed solvent of an ether with n-hexane.