1558953-46-0Relevant articles and documents
Aryl-alkyl-lysines: small molecular membrane-active antiplasmodial agents
Ghosh, Chandradhish,Chaubey, Shweta,Tatu, Utpal,Haldar, Jayanta
, p. 434 - 439 (2017)
Due to emerging resistance there is a steady need for new antimalarial drugs. Here, we report a new class of water soluble, non-toxic compounds, aryl-alkyl-lysines, with promising activity against the ring stage of Plasmodium falciparum. The optimal compound perturbed the plasma membrane potential and the digestive vacuole of parasites. In the murine model of malaria (Plasmodium berghei ANKA) the compound was able to increase the survival of mice by at least 5 days by an intra-peritoneal route. Further, the compounds showed no apparent toxicity to mice at the concentration tested.
Small molecular antibacterial peptoid mimics: The simpler the better!
Ghosh, Chandradhish,Manjunath, Goutham B.,Akkapeddi, Padma,Yarlagadda, Venkateswarlu,Hoque, Jiaul,Uppu, Divakara S.S.M.,Konai, Mohini M.,Haldar, Jayanta
, p. 1428 - 1436 (2014/03/21)
The emergence of multidrug resistant bacteria compounded by the depleting arsenal of antibiotics has accelerated efforts toward development of antibiotics with novel mechanisms of action. In this report, we present a series of small molecular antibacterial peptoid mimics which exhibit high in vitro potency against a variety of Gram-positive and Gram-negative bacteria, including drug-resistant species such as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium. The highlight of these compounds is their superior activity against the major nosocomial pathogen Pseudomonas aeruginosa. Nontoxic toward mammalian cells, these rapidly bactericidal compounds primarily act by permeabilization and depolarization of bacterial membrane. Synthetically simple and selectively antibacterial, these compounds can be developed into a newer class of therapeutic agents against multidrug resistant bacterial species.