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Design, synthesis and biological evaluation of 1,3,4-oxadiazole derivatives.
3D QSAR analysis for the 21 molecules of 1,3,4-oxadiazoles was carried out by using k-Nearest Neighbor Molecular Field Analysis (kNN-MFA) combined with various selection procedures to evaluate the compounds for their antimicrobial activity against Escherichia coli, Staphylococcus aureus and Staphyllococcus epidermidis. Expand
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
It was concluded that, besides the requirement of a lipophilic substituent in the position para to the methoxy group for antidopamine activity in vivo, the formation of a coplanar six-membered pseudoring involving the amide moiety and the meth oxygen group is a structural requirement for activity in vitro. Expand
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
One compound, S-(-)-3,5-dichloro-N-[(1-ethyl-2-pyrrolidinyl) methyl]-6-methoxysalicylamide (raclopride, FLA 870) (13) had a stereotypy--hyperactivity separation more than twice that of sulpiride while being 100 times more potent in blocking the apomorphine effects. Expand
Potential Neuroleptic Agents. Part 4. Chemistry, Behavioral Pharmacology and Inhibition of [3H]Spiperone Binding of 3,5‐Disubstituted N‐[(1‐Ethyl‐2‐pyrrolidinyl)methyl]‐6‐methoxysalicylamides.
Die Carbonsauren (II) werden in die Amide (III) und (IV) umgewandelt, von denen (III) (R′, R2 = C1) auf Grund der Voruntersu-g chungsergebnisse klinisch gegen Schizophrenie untersucht werden soll.
Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antitumor and antifilarial agents: 1. Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamates, -selenazole-2- carbamates, and
Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamate was the most active compound in this screen, inhibiting the growth of L1210 leukemic cells with an IC50 = 3.2 microM and Mitotic blocking appears to be its primary mechanism of cytotoxic activity. Expand
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds.
The study supports the view that the o-methoxy group may adopt coplanar, as well as perpendicular orientations, and maintain the intramolecular hydrogen bonding required in the bioactive conformation. Expand
Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antifilarial and antitumor agents. 2. 2-Arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and
None of the compounds prepared in this study demonstrated antifilarial activity. Expand
Alkynylation of N-(3-iodopyridin-2-yl)sulfonamide under Pd/C–Cu catalysis: a direct one pot synthesis of 7-azaindoles and their pharmacological evaluation as potential inhibitors of sirtuins
The Pd-mediated alkynylation of N-(3-iodopyridin-2-yl)sulfonamide was investigated in the presence of 2-aminoethanol as a base. The combination of Pd/C–Cu catalysts and 2-aminoethanol facilitated theExpand