PubMed Health⌕ Search

SEARCH · PubMed Health

Results for “Benzophenones”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 325 records · Page 18Linked to original sources
PubMed1977

The metabolism of a substituted aminoacetamido-benzophenone and cyclization to the corresponding benzodiazepine in the rat in vivo.

1. 2-(5-Cyano-N-methyl-3,5-dimethyl-3-aza-pentanamido)-5-nitrobenzophenone, administered orally to the rat, is well absorbed and extensively metabolized with only minimal quantities of parent compound detected in plasma, bile or urine. 2. Urinary t.l.c. metabolite profiles after oral administration of a substituted aminoacetamidobenzophenone, [14C]C 72 0045, and [14C]nimetazepam were qualitatively similar but differed quantitatively. 3. Analysis by t.l.c. of plasma extracts obtained after oral administration of [14C]C 72 0045 demonstrated that nimetazepam and nitrazepam accounted for 20% of the plasma total radioactivity. Nimetazepam and nitrazepam had a combined concentration up to 22 times greater than the concentration of C 72 0045. 4. The presence of nimetazepam in plasma after oral administration of C 72 0045 was confirmed by mass spectrometry. 5. In the liver, [14C]C 72 0045 was rapidly metabolized to polar metabolites. In the same rats, the major brain metabolites were nimetazepam and nitrazepam. 6. It is concluded that [14C]C 72 0045 undergoes metabolic cyclization in the rat to form nimetazepam, which is further metabolized to form nitrazepam.

Animals↗
PubMedDate not supplied

Benzophenone-type photoactivatable derivatives of alpha-neurotoxins and alpha-conotoxins in studies on Torpedo nicotinic acetylcholine receptor.

By chemical modification of different lysine residues, benzoylbenzoyl (BzBz) groups were introduced into neurotoxin II Naja naja oxiana (NT-II), a short-chain snake venom alpha-neurotoxin, while p-benzoylphenylalanyl (Bpa) residue was incorporated in the course of peptide synthesis at position 11 of alpha-conotoxin G1, a neurotoxic peptide from marine snails. Although the crosslinking yields for iodinated BzBz derivatives of NT-II and for Bpa analogue of G1 to the membrane-bound Torpedo californica nicotinic acetylcholine receptor (AChR) are relatively low, the subunit labeling patterns confirm the earlier conclusions, derived from arylazide or diazirine photolabels, that alpha-neurotoxins and alpha-conotoxins bind at the subunit interfaces. Detecting the labeled alpha-subunit with iodinated Bpa analogue of G1 provided a direct proof for the contact between this subunit and alpha-conotoxin molecule.

Animals↗
PubMed1975

Chiral 1,4-benzodiazepine. VII. Cyclization rates of 2-(n-alpha-ammoniumacyl)-amino-5-chloro-benzophenones in the chiral 1,4-benzodiazepin-2-ones.

Cyclisation rates of some S-alpha-amino acid derivatives (I--VII) into chiral 1,4-benzodiazepin-2-ones were determined under physiological-like conditions (pH, temperature) and plotted against pKa values of the corresponding alpha-amino acids. No correlation between k, i.e. t1/2 values, of the acidic precursors, and pharmacodynamic activity, as determined by some standard tests, were observed, however. Unambiguity of cyclisation, and its t1/2 values reveal benefit for physico-chemical properties of the investigated acyclic precursors as transport-forms of the chiral 1,4-benzodiazepin-2-ones with prolonged pharmacological activity.

Aggression↗
PubMed1992

[Antiarrhythmic active amidinohydrazones of substituted benzophenones. 3. The isomerization of (E)-2-amino-5-chlorobenzophenone amidinohydrazones].

The isomerization of the title compound in a preparative scale can be realized by acetylation/deacetylation or by influence of protons in dimethylformamide. The title compound is obtained als main product of the condensation of 2-amino-5-chlorbenzophenone and aminoguanidine if the reaction is carried out in the presence of formaldehyde.

Anti-Arrhythmia Agents↗
PubMed1992

[Antiarrhythmic active amidinohydrazones of substituted benzophenones. 4. The photoisomerization of (Z)- and (E)-2-amino-5-chlorobenzophenone amidinohydrazones and the corresponding (E)-N-phenylamidinohydrazone].

The title compounds undergo a photoisomerization by irradiation. If the E-isomers are irradiated by light of a wavelength of an absorption maximum typical for them, they can be converted quantitatively to the corresponding Z-isomers. In case that the synthesis of analogs of the title compounds give only one configurational isomer, sometimes the missing one can be obtained by photoisomerization.

Anti-Arrhythmia Agents↗