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Replacing the distal sulfonamide moiety with a difluoromethylenesulfonamide group had only a modest effect on inhibitor potency.
Two novel indole-based, bipolar, host materials were designed and synthesized by introducing the triazine unit to the 5-position of indole moiety with a meta-linking strategy.
In contrast, the enantioselectivity is determined by the biomolecular scaffold, which confers the catalytic moiety with a well-defined second coordination sphere, reminiscent of enzymes.
Particularly, derivatives having an N4-alkoxylcarbonyl moiety with a C4 C6 alkyl chain were the most susceptible to the human carboxylesterase.
A series of novel hybrid molecules were designed rationally by connecting an indole moiety with a quinoxaline ring through a linker as potential inhibitors of PDE4.
In the divergent synthesis of DS disaccharide, it is important to prepare the IdoA moiety with a diverse set of protecting groups.
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Lead compound 3, with selective Aβ42-lowering activity, was modified by replacing its imidazolylphenyl moiety with an oxazolylphenyl moiety.
Here we describe a strategy to conveniently obtain metal-based PARP-1 inhibitors with enhanced biological activities by conjugating platinum moiety with an original inhibitor, e.g., benzonaphthyridone.
Comparable activities to 4a were obtained by replacing the anilino nitrogen with an ether linkage 27 or by exchanging the isopropoxy ether moiety with an isopropyl amino group 15.
The emitter, 3- N,N-diphenylamino -7- β,β-dicyanoethenyl)-5,5-spirofluorenyl-5H-dibenzo[a,d]-cycloheptene, was composed of a spirally configured cis-stilbene/fluorene moiety with an ambipolar character, and the matching host was 1-butyl-9,10-naphthalene-anthracene (BANE).
Glycosylation is defined as coupling of a sugar moiety with an aglycone acceptor, which can be achieved by enzymatic, chemical synthesis, and chemoenzymatic approaches (neo-glycosylation).
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