2702-58-1Relevant articles and documents
MECHANISM OF THE REACTION OF 3,5-DINITROBENZONITRILE WITH SODIUM METHOXIDE IN METHANOL.
Abe
, p. 1206 - 1213 (1983)
The reaction of 3,5-dinitrobenzonitrile in a methanolic solution containing a low sodium-methoxide concentration has been reinvestigated. The final product has been found to be methoxy (3,5-dinitrophenyl)methanimine, which is produced by a catalytic reaction. The reaction mechanism has been presented for the formation of the Meisenheimer complexes and the final product in the reaction system. The rate and thermodynamic stabilites for their formation have been discussed on the basis of the LUMO coefficients of 3,5-dinitrobenzonitrile and from the relative potential energies of their formation respectively, considering also the solvent effects.
Identification of Monovalent Alcohols with 3,5-Dinitrobenzoic Anhydride
Oelschlaeger, Herbert,Fritsch, Helmut
, p. 759 - 763 (1985)
-
New diarylsulfonamide inhibitors of Leishmania infantum amastigotes
González, Myriam,Alcolea, Pedro José,álvarez, Raquel,Medarde, Manuel,Larraga, Vicente,Peláez, Rafael
, p. 45 - 64 (2021/05/26)
New drugs against visceral leishmaniasis with mechanisms of action differing from existing treatments and with adequate cost, stability, and properties are urgently needed. No antitubulin drug is currently in the clinic against Leishmania infantum, the causative agent of visceral leishmaniasis in the Mediterranean area. We have designed and synthesized a focused library of 350 compounds against the Leishmania tubulin based on the structure-activity relationship (SAR) and sequence differences between host and parasite. The compounds synthesized are accessible, stable, and appropriately soluble in water. We assayed the library against Leishmania promastigotes, axenic, and intracellular amastigotes and found 0, 8, and 16 active compounds, respectively, with a high success rate against intracellular amastigotes of over 10%, not including the cytotoxic compounds. Five compounds have a similar or better potency than the clinically used miltefosine. 14 compounds showed a host-dependent mechanism of action that might be advantageous as it may render them less susceptible to the development of drug resistance. The active compounds cluster in five chemical classes that provide structure-activity relationships for further hit improvement and facilitate series development. Molecular docking is consistent with the proposed mechanism of action, supported by the observed structure-activity relationships, and suggests a potential extension to other Leishmania species due to sequence similarities. A new family of diarylsulfonamides designed against the parasite tubulins is active against Leishmania infantum and represents a new class of potential drugs with favorable cost, stability, and aqueous solubility for the treatment of visceral leishmaniasis (VL). These results could be extended to other clinically relevant species of Leishmania spp.
Synthesis and antimicrobial activity of piperine analogues containing 1,2,4-triazole ring
Kumar, Kottakki Naveen,Amperayani, Karteek Rao,Ummdi, V. Ravi Sankar,Parimi, Uma Devi
, p. 1077 - 1080 (2019/04/05)
A series 1,2,4-triazole piperine analogues (TP1-TP6) were designed and synthesized. The structures were confirmed using 1H NMR and 13C NMR. Antibacterial study was done using Gram-positive (Staphylococcus aureus and Bacillus cereus) and Gram-negative microorganisms (E. coli and Pseudomonas aeruginosa) by disc diffusion method. Compound containing chloro substitution (TP6) showed the highest effect, while compound TP1, TP3, TP4, TP5 showed the moderate activity.
