2018
DOI: 10.5530/ijper.52.1.13
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Synthesis, Characterization, Antidepressant Activity and Docking Studies of Some Novel Indole Bearing Azetidinone Derivatives

Abstract: Context: In general, indole bearing azetidinone derivatives are exhibiting various biological activities. The evaluation of pharmacological potential of the indole bearing azetidinone derivatives as antidepressant agent has been relatively less explored. To get insight of the intermolecular interactions, the molecular docking studies are performed at active site of MAO-A enzyme. Aim: In this study, an attempt has been made to generate new molecular template by linking two pharmacophores (indole and azetidinone… Show more

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Cited by 16 publications
(7 citation statements)
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“…We have synthesized new hybrid compounds containing both entities through the reaction of the obtained imino derivative 7 with chloroacetyl chloride and phenacyl bromide to give compounds 8 and 9, respectively. This is in accordance with previous publication [20] (Scheme 3).…”
Section: Introductionsupporting
confidence: 94%
“…We have synthesized new hybrid compounds containing both entities through the reaction of the obtained imino derivative 7 with chloroacetyl chloride and phenacyl bromide to give compounds 8 and 9, respectively. This is in accordance with previous publication [20] (Scheme 3).…”
Section: Introductionsupporting
confidence: 94%
“…From the starting material isatin, compound 2 was synthesized in high yield using the approach reported by Hassan M. et al (Indole-2,3-dione). Compound 2 was condensed with different substituted aromatic aldehydes to get a Schiff base (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22) in the solvent 100 % ethanol. The preparation of pharmacophore, 3-[3chloro-2-substituted-4-oxoazetidin-1-yl]imino-1,3-dihydro-2H-indol-2-one, a pharmacophore was assisted by action of various substituted Schiff bases with chloroacetyl chloride in the presence of triethylamine (23)(24)(25)(26)(27)(28)(29)(30)(31)(32)(33)(34)(35)(36)(37)(38)(39)(40)(41)(42).…”
Section: Chemistrymentioning
confidence: 99%
“…The benzopyrrole scaffold and its analog can be found in a variety of marine and natural plants [4] . The wide range of chemotherapeutic potential of benzopyrrole is very interesting as a lead in the designing of novel agents, effective against microorganisms, [5,6] cancer, [7] convulsion, [8] inflammation, [9,10] depression, [11] HIV, [12] and other bacteria, benzopyrrole, and its derivatives have garnered a lot of attention in recent decades. Furthermore, the various congeners of azetidinone derivatives were found to have antibacterial and antifungal properties [13–17] …”
Section: Introductionmentioning
confidence: 99%
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“…[ 36 ] The available scientific literature is abundant with reports on the development of indole‐based molecules against convulsion shown in Figure 1. [ 37–43 ] However, pyrazoles have proved to be a useful structural motif in medicinal chemistry, having applications in the development of drugs for the treatment of cancer, tuberculosis, inflammation, and so forth. [ 44–46 ] Some studies also prove that 1,3,5‐triphenyl‐2‐pyrazoline derivatives possess antidepressant and anticonvulsant activities.…”
Section: Introductionmentioning
confidence: 99%