50866-56-3Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AND THEIR USE IN PREVENTING OR TREATING BACTERIAL INFECTIONS
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Page/Page column 31-32, (2018/04/17)
The invention relates to a compound of formula (I) and a racemate, an enantiomer, a diastereoisomer, a geometric isomer or a pharmaceutically acceptable salt thereof, and its use as antibacterial agent.
Synthesis and Activity of a New Series of Antileishmanial Agents
Kanwar, Ankush,Eduful, Benjamin J.,Barbeto, Linda,Carletti Bonomo, Piero,Lemus, Andrea,Vesely, Brian A.,Mutka, Tina S.,Azhari, Ala,Kyle, Dennis E.,Leahy, James W.
supporting information, p. 797 - 801 (2017/08/16)
We have determined that tetrahydroindazoles such as 1 show potent activity against Leishmania donovani, the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of 1 have previously been explored, we present here our effort
ANTIMICROBIAL COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT OF INFECTIONS
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Page/Page column 26; 41, (2016/12/22)
The present disclosure provides compositions including a compound (e.g., compounds A-D), pharmaceutical compositions including the compound, methods of treatment of a condition (e.g., an infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7- (naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configurational assignment using infrared and vibrational circular dichroism spectroscopy in combination with ab initio hartree-fock calculations
Huynh, Tri H. V.,Shim, Irene,Bohr, Henrik,Abrahamsen, Bjarke,Nielsen, Birgitte,Jensen, Anders A.,Bunch, Lennart
, p. 5403 - 5412 (2012/08/28)
The excitatory amino acid transporters (EAATs) play essential roles in regulating the synaptic concentration of the neurotransmitter glutamate in the mammalian central nervous system. To date, five subtypes have been identified, named EAAT1-5 in humans, and GLAST, GLT-1, EAAC1, EAAT4, and EAAT5 in rodents, respectively. In this paper, we present the design, synthesis, and pharmacological evaluation of seven 7-N-substituted analogues of UCPH-101/102. Analogue 9 inhibited EAAT1 in the micromolar range (IC50 value 20 μM), whereas analogues 8 and 10 were inactive (IC50 values >100 μM). The diastereomeric pairs 11a/11b and 12a/12b were separated by HPLC and the absolute configuration assigned by VCD technique in combination with ab initio Hartree-Fock calculations. Analogues 11a (RS-isomer) and 12b (RR-isomer) inhibited EAAT1 (IC50 values 5.5 and 3.8 μM, respectively), whereas analogues 11b (SS-isomer) and 12a (SR-isomer) failed to inhibit EAAT1 uptake (IC50 values >300 μM).
Divergent asymmetric synthesis of 3,5-disubstituted piperidines
Olofsson, Berit,Bogar, Krisztian,Fransson, Ann-Britt L.,Baeckvall, Jan-E.
, p. 8256 - 8260 (2007/10/03)
A divergent synthesis of various 3,5-dioxygenated piperidines with interesting pharmacological properties is described. A mixture of the achiral cis- and racemic trans-3,5-piperidine diol could be efficiently obtained from N-benzylglycinate in five steps
