Synthesis and biological evaluation of novel 2-azido muramyl dipeptide as NOD2 agonistic adjuvants

Piperazine tethered bergenin heterocyclic hybrids: design, synthesis, anticancer activity, and molecular docking studies

“…). 30 In the present study, the lipophilicity of the selected derivatives 5a , 5c , 10f , and 13o was improved as compared with that of the parent molecule (Table S6†).…”

“…of the drug could cause the level of drug administration in animal model (intestinal, blood brain barrier etc.). 30 In the present study, the lipophilicity of the selected derivatives 5a, 5c, 10f, and 13o was improved as compared with that of the parent molecule (Table S6 †).…”

Structure-Activity Relationship in NOD2 Agonistic Muramyl Dipeptides

“…In contrast, thecompound 26, which is the salt form of compound 6, showed diminished NOD2 agonistic activity. 43,44 The compounds having acylation at the C2 position (27-31, Fig. 6)still retained the NOD2 agonist activity two-fold greater than the untreated control.…”

“…7) due to the masking of the hydroxy group by the benzyl group at the C1 axial position as compared to MDP, suggesting that the orientation and substituents at the C1 position might play an important role in NOD2 activity. Also, the compounds with a substituted triazole moiety (42)(43)(44)(45)(46) at the C4 position dramatically weaken the interactions with the NOD2 receptor and thus showed diminished activity.This shows that a substituted triazole moiety causes a significant weakening of NOD2 activity at the C4 position.…”