919088-63-4Relevant academic research and scientific papers
Synthesis of novel monocarbonyl curcuminoids, evaluation of their efficacy against MRSA, including ex vivo infection model and their mechanistic studies
Gagandeep,Kandi, Shamseer Kulangara,Kumar, Prince,Mukhopadhyay, Kasturi,Rawat, Diwan S.
, (2020/04/15)
In continuation of our effort to improve the physiological stability and the antibacterial activity of curcuminoids against drug-resistant bacteria, a series of novel monocarbonyl curcuminoids were synthesized and screened for antibacterial activity against S. aureus and E. coli strains. These curcuminoids showed potent antibacterial activity against both methicillin-sensitive and methicillin-resistant strains of S. aureus with MIC values 2–8 and 4–16 μg/mL, respectively. They also exhibited moderate potency against E. coli strains. The four most active curcuminoids (7d, 7i, 7m, and 7p) were on further investigation found to be very stable under physiological conditions, non-hemolytic, and non-toxic toward mammalian cells up to 150 μg/mL concentration. Mechanistic studies revealed that these curcuminoids displayed potent bactericidal activity by targeting cell membranes. Further, in an ex vivo mammalian co-culture infection model study, remarkably, the curcuminoids 7i and 7p were able to clear the internalized bacteria in mammalian cells and the activity was found to be superior to conventional antibiotics such as vancomycin and linezolid. Therefore, the present study affords us water-soluble, stable, non-toxic curcuminoids that may serve as lead molecules for development as antibacterial agents against MRSA infections.
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands
Lee-Dutra, Alice,Arienti, Kristen L.,Buzard, Daniel J.,Hack, Michael D.,Khatuya, Haripada,Desai, Pragnya J.,Nguyen, Steven,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Breitenbucher, J. Guy
, p. 6043 - 6048 (2007/10/03)
A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H4 receptor.
