Search results for "Diazepine"
showing 10 items of 108 documents
CCDC 2069303: Experimental Crystal Structure Determination
2021
Related Article: Renè Hommelsheim, Heliana Michaela Núñez Ponce, Khai-Nghi Truong, Kari Rissanen, Carsten Bolm|2021|Org.Lett.|23|3415|doi:10.1021/acs.orglett.1c00874
CCDC 2069304: Experimental Crystal Structure Determination
2021
Related Article: Renè Hommelsheim, Heliana Michaela Núñez Ponce, Khai-Nghi Truong, Kari Rissanen, Carsten Bolm|2021|Org.Lett.|23|3415|doi:10.1021/acs.orglett.1c00874
CCDC 1413502: Experimental Crystal Structure Determination
2016
Related Article: Lei Wang, Sun Li, Marcus Blümel, Arne R. Philipps, Ai Wang, Rakesh Puttreddy, Kari Rissanen, Dieter Enders|2016|Angew.Chem.,Int.Ed.|55|11110|doi:10.1002/anie.201604819
Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
2012
Abstract A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b–h were prepared and tested at 10 μM for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7a–d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a–d,i, showing that the isochromene/chromene isomerism influences the activity.
Behavioural stress reactivity in handling naive and handling-habituated adult male rats prenatally exposed to different benzodiazepine receptor agoni…
2001
Development of Novel Benzodiazepine-Based Peptidomimetics as Inhibitors of Rhodesain from Trypanosoma brucei rhodesiense.
2020
Starting from the reversible rhodesain inhibitors 1 a-c, which have Ki values towards the target protease in the low-micromolar range, we have designed a series of peptidomimetics, 2 a-g, that contain a benzodiazepine scaffold as a β-turn mimetic; they are characterized by a specific peptide sequence for the inhibition of rhodesain. Considering that irreversible inhibition is strongly desirable in the case of a parasitic target, a vinyl ester moiety acting as Michael-acceptor was introduced as the warhead; this portion was functionalized in order to evaluate the size of corresponding enzyme pocket that could accommodate this substituent. With this investigation, we identified an irreversibl…
Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antipr…
2014
Novel papain-family cathepsin L-like cysteine protease inhibitors endowed with antitrypanosomal and antimalarial activity were developed, through an optimization study of previously developed inhibitors. In the present work, we studied the structure-activity relationships of these derivatives, with the aim to develop new analogues with a simplified and more synthetically accessible structure and with improved antiparasitic activity. The structure of the model compounds was significantly simplified by modifying or even eliminating the side chain appended at the C3 atom of the benzodiazepine scaffold. In addition, a simple methylene spacer of appropriate length was inserted between the benzod…
GABAA-receptor Subtypes: Clinical Efficacy and Selectivity of Benzodiazepine Site Ligands
1997
The main inhibitory neurotransmitter receptor of the brain, the gamma-aminobutyric acid type A receptor (GABA[A]), mediates the actions of several classes of clinically important drugs, such as benzodiazepines, barbiturates and general anaesthetics. This review summarizes the current knowledge on how classical benzodiazepines and novel nonbenzodiazepine compounds act on the benzodiazepine site of GABA(A) receptors and on their clinical pharmacology related to anxiolytic, sedative, hypnotic and cognitive effects or side-effects. Partial agonism, receptor subtype selectivity and novel binding sites are discussed as possible strategies to develop new drugs with fewer adverse effects than are s…
Zaleplon displays a selectivity to recombinant GABAA receptors different from zolipdem, zopiclone and benzodiazepines
1999
A chemically heterogeneous group of compounds acts at the benzodiazepine (BZ) recognition site of the γ-aminobutyric acid type A (GABAA) receptor complex. Whereas most 1,4-BZs recognize all GABAA/BZ receptors with similar affinity, other compounds differentiate between the large number of native GABAA receptors which assemble from the more than 14 known subunits. Here we describe the in vitro binding properties of the BZs lorazepam and Ro 15-4513 plus the three hypnotics zaleplon, zolpidem and zopiclone to eight receptors subtypes. Lorazepam fits well into the general shceme for other 1,4-BZs with respect to its receptor subtype selectivity in spite of its clinically different use. Zaleplon…
ChemInform Abstract: 1-Alkyl- and Azeto[1,2-a][1,5]benzodiazepine Derivatives in the Reaction of o-Phenylenediamine with 3-(Dimethylamino)propiopheno…
2001
The reaction of o-phenylenediamine (4) with one, two or three equivalents of p-substituted 3-dimethylaminopropiophenone hydrochlorides 5a−e was studied. 4-Aryl-2,3-dihydro-1H-1,5-benzodiazepine derivatives 6a−e were obtained in good yields, along with the 1:2-adducts 7c−e and the unexpected 1:3-adducts rac-8c−e. The type of adduct formed is determined by the molar ratio of the reactants 4 and 5 and by the nature of the substituent in the para position of the propiophenone 5.