90389-39-2Relevant academic research and scientific papers
Aryl-alkyl-lysines: small molecular membrane-active antiplasmodial agents
Ghosh, Chandradhish,Chaubey, Shweta,Tatu, Utpal,Haldar, Jayanta
supporting information, p. 434 - 439 (2017/03/08)
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.
ANTIMICROBIAL COMPOUNDS, THEIR SYNTHESIS AND APPLICATIONS THEREOF
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Page/Page column 62; 63, (2014/07/08)
The present disclosure relates to the field of medicinal chemistry and more particularly to the development of antimicrobial compounds. The disclosure relates to the synthesis and characterization of compounds comprising aromatic radical or an aliphatic radical, an alkyl amine and amino acid moiety wherein said compounds exhibit antimicrobial activity against various drug-sensitive and drug-resistant pathogenic 10 microorganisms.
Fluorous scavenger for parallel preparation of tertiary sulfonamides leading to secondary amines
Baslé, Emmanuel,Jean, Micka?l,Gouault, Nicolas,Renault, Jacques,Uriac, Philippe
, p. 8138 - 8140 (2008/03/13)
Alkylation of secondary sulfonamides by alkyl halides or alcohols (Mitsunobu reaction) is an efficient method for secondary amines preparation. However, its application to parallel chemistry is often difficult due to partial reaction. In this Letter, we propose a fluorous technique to bypass this problem. Thus, o-nitrobenzenesulfonamides were prepared and alkylated in parallel (Fukuyama method) with various alkyl halides or alcohols. Depending on the nature of the alkyl halide or alcohol, this step remained incomplete. A reactive fluorous alkyl iodide was then used to trap the unreacted sulfonamide allowing for a rapid and efficient fluorous solid-phase extraction (FSPE). Some examples of the isolated tertiary sulfonamides were converted in parallel to the corresponding secondary amines with good purity.
Mono-N-alkylation of α-Aminoacetonitriles. A Novel Route to Unsymmetrical Secondary Amines
Katritzky, Alan R.,Latif, Muhammad,Urogdi, Laszlo
, p. 667 - 672 (2007/10/02)
Mannich-type condensation products of an aldehyde with an α-aminoacetonitrile and benzotriazole are treated with sodium borohydride or with a Grignard reagent to give unsymmetrical N,N-dialkylaminoacetonitriles, which, on decyanomethylation provide unsymmetrical secondary amines.
The N-Substitution of Aliphatic Primary Amines via 1-benzotriazoles: Preparation of Secondary Amines
Katritzky, Alan R.,Glen, Noble,Pilarski, Boguslaw,Harris, Philip
, p. 1443 - 1446 (2007/10/02)
A new method has been developed for the selective conversion of primary aliphatic amines into unsymmetrical secondary amines by Grignard reaction of 1-benzotriazoles 1.This method employs simple procedures and mild conditions, and is specific in that onyl monoalkylation of the primary amines results.
