Synthesis and biological evaluation of new imidazo[1,2-a]pyridine derivatives designed as mefloquine analogues

Synthesis, Antimicrobial, Antiquorum‐Sensing, and Cytotoxic Activities of New Series of Isoindoline‐1,3‐dione, Pyrazolo[5,1‐a]isoindole, and Pyridine Derivatives

“…The pyrazolo[5,1‐ a ]isoindole derivatives were known to possess antihypotensive and antireproductive activities. Moreover, pyridine derivatives were extensively investigated for their pharmacological uses, some of these compounds showed antimicrobial , insecticidal , antimitotic , antitumor , antimalarial , and anti‐inflammatory activities. Considering these published data and in searching for new compounds of potent antimicrobial and antiquorum‐sensing activities, we are reporting herein the synthesis of new series of isoindoline‐1,3‐dione, pyrazolo[5,1‐ a ]isoindole, and pyridine derivatives.…”

Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors

“…20,30 The key step was performed through reduction of the imine adducts formed from treatment of the heterocyclic aldehydes 25a-c, 26a-d, and 27 with functionalized N-phenylpiperazines 28a-e in dry methanol using sodium cyanoborohydride and catalytic amounts of acetic acid, 31 yielding the desired N-phenylpiperazine derivatives 4-21 and 23-24 as shown in Table 1. On the other hand, acetamide derivative 22 was prepared in 88% yield (two steps) from reduction of the nitro compound 21, 32 followed by acetylation of the corresponding aniline intermediate 29 (Scheme 1).…”

“…22 Some of the studies cited above carried on with biarylmethylamine derivatives also describe compounds with considerable affinity for the 5-HT 1A receptors. 22,35,39,42,44 Both NGD-94-1 (30) and FAUC 2020 (31) bind with high affinity to this subtype of serotonin receptor (K i = 180 and 37 nM, respectively). 22,44 Indeed, there is a high molecular similarity between the compounds assayed in present work, NGD-94-1 (30), FAUC 2020 (31), and bifeprunox (3), a mixed D 2 partial agonist (K i = 2.2 nM) and 5-HT 1A agonist Scheme 1.…”

Synthesis, Characterization, and Antiproliferative Activity Studies of Novel Benzimidazole‐Imidazopyridine Hybrids as DNA Groove Binders

“…Another important biologically active heterocyclic compound, namely imidazo[1,2‐ a ]pyridine which was first synthesized by Chichibabin (1925) through a cyclysation reaction between an α‐aminopyridine and α‐halogenatedcarbonyl derivatives . Imidazo[1,2‐ a ]pyridine containing drugs act as antiviral, anti‐inflammatory, anti‐protozoal, anti‐HIV, anti‐malarial, hypnotic, analgesic, tuberculosis, anti‐ulcer, anxiolytic, benzodiazepine receptor agonist and anti‐cancer and also used in materials science, and molecular biology . Among the commercially available imidazo[1,2‐ a ]pyridines, Zolpidem was the first used as a hypnotic and is widely used in the world to treat insomnia .…”