New GABA‐Modulating 1,2,4‐Oxadiazole Derivatives and Their Anticonvulsant Activity.

Abstract

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In vitro anti-TB properties, in silico target validation, molecular docking and dynamics studies of substituted 1,2,4-oxadiazole analogues against Mycobacterium tuberculosis

“…These clinical success in parallel gave an impetus to the synthetic chemists to design innovative strategies for the economic, ecofriendly and rapid synthesis of 1,2,4-oxadiazole chemical libraries to accelerate the drug discovery process 32,33 . In the past 40 years, 1,2,4oxadiazole scaffold has been extensively investigated for diverse biological activities 34 including anti-inflammatory 35,36 , analgesic 37 , anaesthetic 38 , anthelmintic 39 , antiallergic 40 , anti-Alzheimer 41 , antibacterial 42,43 , anticancer [44][45][46] , anticonvulsant 47,48 , antidepressant 49 , antifungal 50 , anti-HIV 51 , antiparasitic 52 , antiplatelet and antithrombotic 53 , anti-tubercular 54 , antitussive 55 , antiviral 56,57 , insecticidal 58 , monoamine oxidase inhibition 59 , muscarinic receptor agonists 60 , selective G-protein bile acid receptor 1 (GPBAR1) agonists 61 and selective H 3 receptor antagonists 62 activities.…”

1‐[(2‐Arylthiazol‐4‐yl)methyl]azoles as a New Class of Anticonvulsants: Design, Synthesis, In vivo Screening, and In silico Drug‐like Properties

“…Structure-activity relationship studies reveal the presence of one common pharmacophoric portion in all of these molecules, which is characterized by a lipophilic aryl ring linked by an alkylene bridge to nitrogen of azole ring. The alkylene bridge is often substituted by a small oxygen functional group such as carbonyl, carbamoyl, ethylene dioxy, methoxy, acyloxy, and hydroxy substituents or a electronegative chlorine atom (9,10,13,14).…”

Iron(III) Chloride/l-Proline as an Efficient Catalyst for the Synthesis of 3-Substituted 1,2,4-Oxadiazoles from Amidoximes and Triethyl Orthoformate

“…1 Among oxadiazoles, 1,2,4-oxadiazoles are particularly important (Figure 1). 2,3 They function as hydrolytically stable bioisosteres for esters or amides showing biological properties as antidiabetic, 4 anti-inflammatory, 5 antimicrobial, 6 antitumor, 7 anticonvulsant, 8 and neuroprotective 9 agents. 1,2,4-Oxadiazoles are also found in several drugs including muscarinic receptor agonists for the treatment of Alzheimer's disease, 10 Duchenne muscular dystrophy and potentially other genetic disorders, 11 and helminthiasis 12 ( Figure 2).…”