1,3,4-Oxadiazole Derivatives: Synthesis, …
Synthetic Approaches and Pharmacological Activity of 1,3,4-Oxadiazoles: A Review of the Literature from 2000–2012.
Synthesis of 1,2,4-Oxadiazole-, 1,3,4-Oxadiazole-, and 1…
Marina I et al 58 have synthesized a series of 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazole derivatives and screened them all for in vitro activity against Staphylococcus aureus, Trypanosoma cruzi, and Candida albicans. The bioactivity was expressed as minimum inhibitory concentration (MIC) for S. aureus strains, and as fifty-percent inhibitory concentration (IC50) of parasite population growth for T. cruzi.
Juan S et al 34 have synthesized a series of quinoline derivatives and also evaluated their biological activities as potential telomerase inhibitors. Bioassay tests demonstrated that most of the compounds exhibited substantial broad-spectrum of antitumor activity against the three cancer cell lines (HepG2, SGC-7901 and MCF-7). Moreover, all the title compounds were assayed for telomerase inhibition using the TRAP-PCR-ELISA assay. Some compounds from the series displayed the most potent anticancer activities, which were comparable to the positive control.
Synthesis of 1,3,4-oxadiazoles - Organic Chemistry Portal
Keshari K J et al 44 have been synthesized a novel series of 1,3,4-oxadiazole derivatives and screened for their antibacterial activity against E. coli (MTCC 443), S. epidermidis (ATCC12228) and S. aureus (ATCC25923) bacterial strains by disc diffusion method. In all the determinations, tests were performed in triplicate and the results were taken as a mean of three determinations. Some compounds have shown significant inhibition comparable to standard while some of them showed moderate activity [Figure 18].
150. Perez DI, Pistolozzi M, Palomo V, Redondo M, Fortugno C, Gil C. . 5-Imino-1,2-4-thiadiazoles and quinazolines derivatives as glycogen synthase kinase 3 beta (GSK-3 beta) and phosphodiesterase 7 (PDE7) inhibitors: Determination of blood-brain barrier penetration and binding to human serum albumin. 2012;45:677-84
Novel 1,3,4-Oxadiazole Derivatives of …
We have designed and synthesized a series of 1,3,4-oxadiazolethioethers to investigate the effect of the replacement of the anilino moiety with the heterocyclic pyridyl moiety, as well as the replacement of the benzyl group at its 2 position with lipophilic, polar and basic pharmacophores against breast cancer cell line MCF-7. The computer-aided prediction of the biological activity in relation to the chemical structure of the newly synthesized compounds showed that most of these compounds have greater or almost equal % ABS to the reference drug. The antitumor activity revealed that compounds 18 and 22 are almost double the potency of the reference drug, this could be attributed to their chemical structure that allows them to have high topological polar surface area (TPSA) that allow good passive molecular transport through membranes. Also they have more hydrogen bond acceptors (HBA) (8) than the reference drug and they both have (6) NROTB that can form a large number of conformational changes that allow them to fit into the receptor. While compounds 23 and 29 are almost as potent as the reference drug, the other compounds showed moderate anticancer activity. This may be attributed to their high ability to high %ABS. From the Docking studies’ results we may conclude that these biologically active compounds with future further investigations could form a potential lead compounds for enriching the anticancer libraries since they interacted smoothly with EGFR at the ATP binding site.
From these parameters, it is obvious that, all titled compounds exhibited percentage absorption (% ABS) ranging from 55.23 to 91.12%, among them six compounds are supposed to have very high % ABS (85.23–91.12%). Compounds 6, 4, 7–9 and 2 showed greater % ABS than that of the reference drug erlotinib (83.21%). All the newly synthesized compounds showed good membrane permeability since they all exhibited c Log ≤5. Compounds 7 and 9 were similar to that of erlotinib. The number of rotatable bonds (NROTB) ranged from 2–9 which will facilitate the conformational changes required for these compounds to fit inside the receptors.
Synthesis and Pharmacology of 1,3,4-oxadiazole derivatives: ..
Synthesis of substituted 1,3,4-oxadiazole derivatives | …
In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives.
Regioselective Synthesis of 2‑Amino-Substituted 1,3,4-Oxadiazole …
Synthesis of 2‐hydroxycycloalkyl‐substituted 1,3,4‐oxadiazoles, 1,3,4‐thiadiazoles and 1,2,4‐triazoles
Synthesis of some Novel 1,3,4-Oxadiazole derivatives - …
Synthesis of 2‐hydroxycycloalkyl‐substituted 1,3,4‐oxadiazoles, 1,3,4‐thiadiazoles and 1,2,4‐triazoles.
BACHELOR OF PHARMACY (HONS) - AIMST University
Aboraia AS et al 49 reported some novel 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives promising anticancer agents. These seven oxadiazole compounds were selected for a full anticancer screening against a 60-cell panel assay where they showed non-selective broad spectrum and promising activity against all cancer cell lines. As a result of 60-cell panel assay two oxadiazole compounds were identified as promising lead compounds [Figure 23].
Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy …
Schematic diagram of burn-inducedinsulin resistance through the suppression of thephosphoinositide-3 kinase (PI3K)/Akt signaling pathway mediated byinsulin receptor substrate 1 (IRS1) degradation. After burn injury,the blood concentration of tumor necrosis factor (TNF)-α,interleukin (IL) and lipopolysacchride (LPS) is significantlyincreased. TNF-α binds to its receptor and induces inducible nitricoxide synthase (iNOS) production. ILs, IL-6 in particular, bind tocorresponding receptors and promote the expression of suppressor ofcytokine signaling-3 (SOCS3). LPS binds to CD14 with the help ofthe LPS binding protein (LBP) and activates the intracellularsignaling pathway. All the cytokines induce IRS1 proteindegradation, which suppresses the PI3K/Akt signaling pathway, andsubsequently suppresses glucose transporter (GLUT) translocationand glycogen synthesis, which results in burn-induced insulinresistance and hyperglycemia.
Molecules | April 2014 - Browse Articles
Harish R et al 50 reported the synthesis, characterization and antimicrobial properties of novel 2,5-disubstituted 1,3,4-oxadiazoles. All the compounds were screened for their antimicrobial potential using disk diffusion method. Most active compound demonstrated antimicrobial activity against all six microbial strains used with zone of inhibition in disk diffusion method- 18 mm against S. aureus, 15 mm against B. subtilis, 16 mm against P. mirabilis, 17 mm against P. aeruginosa, 16 mm against A. niger and 17 mm against C. albican. In general, compounds bearing the groups like nitro, hydroxy on distant phenyl ring showed high potency in disk diffusion tests. Whereas replacement of these groups with methoxy and chloro groups on the distant phenyl ring has resulted in compounds with decrease in antimicrobial activity.
Molecules, Volume 19, Issue 4 (April 2014), Pages 3851-5458
Kadi AA et al 48 reported the antimicrobial and anti-inflammatory activities of novel 2-substituted-5-(1-adamantyl)-1,3,4-oxadiazolesand 2-substituted-5-(1-adamantyl)-1,3,4-thiadiazoles. Several derivatives showed good or moderate antibacterial activities particularly against the tested Gram-positive bacteria Bacillus subtilis and marked antifungal activity against Candida albicans [Figure 22].
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