Agelis, George published the artcileFacile and efficient syntheses of a series of N-benzyl and N-biphenylmethyl substituted imidazole derivatives based on (E)-urocanic acid, as angiotensin II AT1 receptor blockers, Computed Properties of 42074-68-0, the publication is Molecules (2013), 7510-7532, database is CAplus and MEDLINE.
In the present work, a facile and efficient route for the synthesis of a series of N-substituted imidazole derivatives is described. Docking studies have revealed that N-substituted imidazole derivatives based on (E)-urocanic acid may be potential antihypertensive leads. Therefore, new AT1 receptor blockers bearing either the benzyl or the biphenylmethyl moiety at the N-1 or N-3 position, either the (E)-acrylate or the propanoate fragment and their related acids at the C-4 position as well as a halogen atom at the C-5 position of the imidazole ring [I; R = CH:CHCO2H, CH:CHCO2Me, CH2CH2 CO2H, CH2CH2CO2Me] and [II; X = H, R = CH:CHCO2R1 or CH2CH2CO2R1, R1 = H, Me, Q; X = Cl, Br, or iodo, R = CH2CH2R1, R1 = H or Q] were synthesized. The newly synthesized analogs were evaluated for binding to human AT1 receptor. The biol. results showed that this class of mols. possesses moderate or no activity, thus not always confirming high docking scores. Nonetheless, important conclusions can be derived for their mol. basis of their mode of action and help medicinal chemists to design and synthesize more potent ones. An aliphatic group as in losartan seems to be important for enhancing binding affinity and activity.
Molecules published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Computed Properties of 42074-68-0.
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