New quinoxalin‐1,3,4‐oxadiazole derivatives: Synthesis, characterization, in vitro biological evaluations, and molecular modeling studies
Sign Up to like & getrecommendations! Published in 2021 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202000471
Abstract: A new series of quinoxalin‐1,3,4‐oxadiazole (10a–l) derivatives was synthesized and evaluated against some metabolic enzymes including human carbonic anhydrase (hCA) isoenzymes I and II (carbonic anhydrases I and II), cholinesterase (acetylcholinesterase and butyrylcholinesterase), and α‐glucosidase.… read more here.
Keywords: oxadiazole derivatives; new quinoxalin; derivatives synthesis; quinoxalin oxadiazole ... See more keywords
Design, Synthesis, Characterization, and Antimicrobial Screening of Novel Indazole Bearing Oxadiazole Derivatives
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Heterocyclic Chemistry"
DOI: 10.1002/jhet.2540
Abstract: Ethyl 2-(2,6-dioxocyclohexyl)-2-oxoacetate was prepared by reacting cyclohexane-1,3-dione (1) and diethyl oxalate (2) with the help of sodium ethoxide in ethanol at 0–5°C. Subsequent treatment of ethyl 2-(2,6-dioxocyclohexyl)-2-oxoacetate with hydrazine hydrate in ethanol resulted into ethyl… read more here.
Keywords: oxadiazole derivatives; novel indazole; bearing oxadiazole; indazole bearing ... See more keywords
Synthesis of [1,2,4]triazolo[4,3-a]quinoxaline-1,3,4-oxadiazole derivatives as potent antiproliferative agents via a hybrid pharmacophore approach.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104293
Abstract: Imiquimod (1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine) is efficacious in topical therapy for certain types of skin cancers. Structurally similar EAPB0203 (N-methyl-1-(2-phenethyl)imidazo[1,2-a]quinoxalin-4-amine) has been shown higher in vitro potency than imiquimod. Besides, triazole, oxadiazole, and thiadiazole rings are privileged building… read more here.
Keywords: triazolo quinoxaline; oxadiazole derivatives; synthesis triazolo; quinoxaline oxadiazole ... See more keywords
Pharmacokinetic evaluation, molecular docking and in vitro biological evaluation of 1, 3, 4-oxadiazole derivatives as potent antioxidants and STAT3 inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Pharmaceutical Analysis"
DOI: 10.1016/j.jpha.2018.12.002
Abstract: 1, 3, 4-Oxadiazole derivatives (4a–5f) were previously synthesized to investigate their anticancer properties. However, studies relating to their antioxidant potential and signal transducer and activator of transcription (STAT) inhibition have not been performed. We investigated… read more here.
Keywords: pharmacokinetic evaluation; oxadiazole derivatives; evaluation molecular; evaluation ... See more keywords
Syntheses, Biological Evaluations, and Mechanistic Studies of Benzo[c][1,2,5]oxadiazole Derivatives as Potent PD-L1 Inhibitors with In Vivo Antitumor Activity.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00392
Abstract: A series of novel benzo[c][1,2,5]oxadiazole derivatives were designed, synthesized, and biologically evaluated as inhibitors of PD-L1. Among them, compound L7 exhibited 1.8 nM IC50 value in a homogeneous time-resolved fluorescence (HTRF) assay, which was 20-fold… read more here.
Keywords: oxadiazole derivatives; vivo antitumor; syntheses biological; value ... See more keywords
Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02210
Abstract: 1,2,4-Oxadiazole derivatives, a class of Nrf2-ARE activators, exert an extensive therapeutic effect on inflammation, cancer, neurodegeneration, and microbial infection. Among these analogues, DDO-7263 is the most potent Nrf2 activator and used as the core structure… read more here.
Keywords: rpn6; 26s proteasome; oxadiazole derivatives; mechanism ... See more keywords
Characterization of Radioiodinated Diaryl Oxadiazole Derivatives as SPECT Probes for Detection of Myelin in Multiple Sclerosis.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.1c00753
Abstract: Multiple sclerosis (MS) is an intractable disease of the central nervous system that results from destruction of the myelin sheath. Direct measurement of de- and remyelination is required for monitoring the disease stage of MS,… read more here.
Keywords: oxadiazole derivatives; diaryl oxadiazole; podp; multiple sclerosis ... See more keywords
3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00134
Abstract: The human rhinovirus (hRV) is the causative agent of the common cold that often aggravates respiratory complications in patients with asthma or chronic obstructive pulmonary disease. The high rate of mutations and variety of serotypes… read more here.
Keywords: oxadiazole derivatives; derivatives active; hrv; aryl oxadiazole ... See more keywords
Synthesis, characterisation and mesomorphic behaviours of non-symmetrically substituted 1,2,4- and 1,3,4-oxadiazole derivatives
Sign Up to like & getrecommendations! Published in 2017 at "Liquid Crystals"
DOI: 10.1080/02678292.2016.1225837
Abstract: ABSTRACT Two series of non-symmetrically substituted bent-core mesogens derived from the central 3,5 and 2,5 cores of the 1,2,4- and 1,3,4-oxadiazole derivatives, respectively, containing ether and ester linkage have been synthesised by several straightforward synthetic… read more here.
Keywords: oxadiazole derivatives; non symmetrically; synthesis characterisation; mesomorphic behaviours ... See more keywords
New bis 1,3,4-oxadiazole derivatives: syntheses, characterizations, computational studies, and antioxidant activities
Sign Up to like & getrecommendations! Published in 2018 at "Canadian Journal of Chemistry"
DOI: 10.1139/cjc-2018-0101
Abstract: In this study, two new bis oxadiazole derivatives (2a and 2b) were synthesized. The new compounds were characterized by elemental analyses, IR, 1H NMR, 13C NMR, and mass spectral studies and were tested for their… read more here.
Keywords: oxadiazole derivatives; new bis; bis oxadiazole; characterizations computational ... See more keywords
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 1, 3, 4-OXADIAZOLE DERIVATIVES: A REVIEW OF LITERATURE.
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Approximate Reasoning"
DOI: 10.21474/ijar01/6328
Abstract: Baijika P, Akash Marathakam, Midhula C C and Shadiha Saheed K. Department of Pharmaceutical Chemistry, National College of Pharmacy, Manassery, Mukkam, Kozhikode 673602. ...................................................................................................................... Manuscript Info Abstract ......................... ........................................................................ Manuscript History read more here.
Keywords: oxadiazole derivatives; activities oxadiazole; biological activities; derivatives review ... See more keywords