نتایج جستجو برای: benzimidazolone
تعداد نتایج: 55 فیلتر نتایج به سال:
We have investigated the mechanism of action of two benzimidazolone analogs (NS004 and NS1619) on DeltaF508-CFTR using both whole-cell and cell-attached patch-clamp techniques and compared their effects with those of genistein. We conclude that benzimidazolone analogs and genistein act through a common mechanism, based on the following evidence: 1) both act only on phosphorylated CFTR, 2) the m...
A series of novel N-acylated benzimidazolone derivatives, were synthesized from 4-aminobenzoic acid, and their antifungal activities against Botrytis cinerea were evaluated by spore germination assay. Preliminary results indicated that most of the benzimidazolone derivatives had inhibitory effect on spore germination, among which 6-carboxylate substituted derivatives were more effective than it...
The benzimidazolone part of the title mol-ecule, C(17)H(25)N(3)O(3), is almost planar (r.m.s. deviation = 0.016 Å) and its mean plane is aligned at 7.9 (4) ° with respect to the mean plane of the nitro substituent. In the crystal, two mol-ecules are disposed about a center of inversion, generating a N-H⋯O hydrogen-bonded cyclic dimer with a R(2) (2)(8) graph-set motif.
The title compound, C(15)H(13)ClN(2)O(3)S, is one of a series of N(1)-benzyl-1,3-dihydro-2H-benzimidazol-2-one derivatives, a new class of non-nucleoside HIV-1 reverse transcriptase inhibitors. The dihedral angle between the two pharmacophoric groups, the dimethyl-benzene ring and the benzimidazolone ring system, is 88 (1)°, giving a butterfly-like conformation to the mol-ecule. The mol-ecular ...
A series of N-acylated analogues of 1-isopropyl-3-acyl-5-methyl-benzimidazolone were synthesized. Bioassay results indicated that analogues 5-07 and 5-19 exhibited the most potency against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Analogues 5-02, 5-07, 5-12, 5-15, 5-19, 5-20 and 5-25 could effectively inhibit the spore germination of...
The benzimidazolone part of the title mol-ecule, C(13)H(13)ClN(2)O, is almost planar (r.m.s. deviation = 0.006 Å) and its mean plane is aligned at dihedral angles of 62.5 (1) and 78.0 (1)° with respect to the mean planes of the allyl substituents.
The benzimidazolone part of the mol-ecule of the title compound, C(15)H(21)N(3)O(3), is almost planar (r.m.s. deviation = 0.007 Å) with its mean plane aligned at a dihedral angle of 10.4 (3)° with respect to the mean plane of the nitro substituent. In the crystal, two mol-ecules are disposed about a center of inversion, generating an N-H⋯O hydrogen-bonded cyclic dimer with R(2) (2)(8) graph-set...
In the reaction of 7-chloro-1,5-benzodiazepine-2,4-dione with N,N-dimethyl-formamide/dimethyl-acetal, the diazepine seven-membered ring undergoes a contraction to form the five-membered ring. The reaction yields two isomers the title compound, C(13)H(14)ClN(3)O(2); the major component has the chlorine-atom substituent in the 5-position of the benzimidazolone ring and the minor component has the...
several cycline dependent kinase 2 (cdk2) inhibitors with different chemical structures have been introduced. the hinge region of cdk2 (residues 81–84) contains a set of hydrogen bond donor and acceptor sites some of which must be satisfied for potent inhibitor binding. the benzimidazolone skeleton may provide such interactions. accordingly, 3-sulfonamide substituted benzamido-benzimidazolones ...
A piperidinyl-benzimidazolone scaffold has been found in the structure of different inhibitors of membrane glycerolipid metabolism, acting on enzymes manipulating diacylglycerol and phosphatidic acid. Screening a focus library of piperidinyl-benzimidazolone analogs might therefore identify compounds acting against infectious parasites. We first evaluated the in vitro effects of (S)-2-(dibenzyla...
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