Comparative Study of the Synthetic Approaches and Biological Activities of the Bioisosteres of 1,3,4-Oxadiazoles and 1,3,4-Thiadiazoles over the Past Decade

The bioisosteres of 1,3,4-oxadiazoles and 1,3,4-thiadiazoles are well-known pharmacophores for many medicinally important drugs. Throughout the past 10 years, 1,3,4-oxa-/thiadiazole nuclei have been very attractive to researchers for drug design, synthesis, and the study of their potential activity towards a variety of diseases, including microbial and viral infections, cancer, diabetes, pain, and inflammation. This work is an up-to-date comparative study that identifies the differences between 1,3,4-thiadiazoles and 1,3,4-oxadiazoles concerning their methods of synthesis from different classes of starting compounds under various reaction conditions, as well as their biological activities and structure–activity relationship.     

Antioxidant and Gastroprotective Activity of Suaeda fruticosa Forssk. Ex J.F.Gmel

Suaeda fruticosa Forssk. Ex J.F.Gmel is traditionally used for inflammatory and digestive disorders, as a carminative, and for diarrhea. This plant is widely distributed in Asia, Africa, and the Mediterranean region. Aqueous methanolic extract of S. fruticosa (Sf.Cr) was prepared and screened for phytoconstituents through qualitative and GC-MS analysis. Quantification of total phenolic and flavonoid contents was performed, while antioxidant capacity was determined by DPPH, CUPRAC, FRAP, and ABTS assays. The gastroprotective activity was assessed in an ethanol-induced ulcer model. Gastric secretory parameters and macroscopic ulcerated lesions were analyzed and scored for ulcer severity. After scoring, histopathology was performed, and gastric mucus contents were determined. Oral pre-treatment of Sf.Cr demonstrated significant gastroprotection. The gastric ulcer severity score and ulcer index were reduced while the %-inhibition of ulcer was increased dose-dependently. The Sf.Cr significantly elevated the pH of gastric juice, while a decrease in total acidity and gastric juice volume was observed. Histopathology demonstrated less oedema and neutrophil infiltration in gastric mucosa of rats pre-treated with the Sf.Cr in comparison to ethanol-intoxicated animals. Furthermore, the gastric mucus contents were increased as determined by alcian blue binding. Sf.Cr showed marked gastroprotective activity, which can be attributed to antioxidant, antisecretory, and cytoprotective effects.     

Anti‐proliferative activity of newly synthesized Cd(II), Cu(II), Zn(II),Ni(II), Co(II), VO(II), and Mn(II) complexes of 2‐((4,9‐dimethoxy‐5‐oxo‐5H‐furo[3,2‐g]chromen‐6‐yl)methylene) hydrazinecarbothioamide on three human cancer cells

Thiosemicarbazone ligand, 2‐((4,9‐dimethoxy‐5‐oxo‐5H‐furo[3,2‐g]chromen‐6‐yl)methylene) hydrazinecarbothioamide and its Cd(II), Cu(II), Zn(II), Ni(II), Co(II), VO(II), and Mn(II) complexes have been prepared and characterized by various spectroscopic and analytical techniques. Complexes molar conductance measurements displayed that all complexes (2–8) are non‐electrolyte. With general composition [M(H₃L)(CH₃COO)₂H₂O].nH₂O, where M = Cd(II), Cu(II), Zn(II), Ni(II), Co(II) and Mn(II) while complex (8) has [VO(H₃L)(SO₄)H₂O].2H₂O formula. Based on analytical and spectral measurements, the octahedral or distorted octahedral geometries suggested for complexes. Ligand and complexes anti‐proliferative activities were assessed against three various human tumor cell lines including breast cancer (MCF‐7), liver cancer (HepG2) and lung cancer (A549) using SRB fluorometric assay and cis‐platin as positive control. The anti‐proliferative activity result indicated that the ligand and its complexes have considerable anti‐proliferative activity analogous to that of ordinarily utilized anti‐cancer drug (cis‐platin). They do their anti‐cancer activities by modifying free radical's generation via raising the superoxide dismutase activity and depletion of intracellular reduced glutathione level, catalase, glutathione peroxidase activities, escorted by highly generation of hydrogen peroxide, nitric oxide and other free radicals leading to tumor cells death, as monitoring by decreasing the protein and nucleic acids synthesis.     

Synthesis,Spectral Characterization,and In Vitro Biological Evaluation of Some Novel Isoquinolinone‐based Heterocycles as Potential Antitumor Agents

A series of new N‐substituted isoquinolin‐1,3‐dione derivatives were prepared, starting from reaction of (Z)‐4‐((E)‐3‐phenylallylidene)isochromane‐1,3‐dione 4 with different nitrogen nucleophiles. The assigned structures of the prepared compounds were elucidated by spectral methods (IR, ¹H NMR, ¹³C NMR, and mass spectroscopy). Some of the newly prepared compounds were tested in vitro against a panel of three human tumor cell lines, namely, hepatocellular carcinoma (liver) HepG2, colon cancer HCT‐116, and mammary gland breast MCF‐7. Also, they were tested as antioxidants. Some of the tested compounds showed very strong cytotoxic activity with respect to the standard.     

Blue‐Emissive Cobalt(III) Complexes and Their Use in the Photocatalytic Trifluoromethylation of Polycyclic Aromatic Hydrocarbons

Room‐temperature luminescent Co^III complexes ( 1 and 2 ) are presented that exhibit intense ligand‐to‐metal and ligand‐to‐ligand charge transfer absorption in the low‐energy UV region (λ_abs≈360–400 nm) and low‐negative quasi‐reversible reduction events (E^1/2_(red)=?0.58 V and ?0.39 V vs. SCE for 1 and 2 , respectively). The blue emission of 1 and 2 at RT is due to the large bite angles and strong σ‐donation of the ligands, the combined effect of which helps to separate the emissive ³LMCT (triplet ligand‐to‐metal charge transfer) and the non‐emissive ³MC (triplet metal‐centered) states. 1 and 2 were found to be powerful photo‐oxidants (E =2.26 V and 2.75 V vs. SCE of 1 and 2 , respectively) and were used as inexpensive photoredox catalysts for the regioselective mono(trifluoromethylation) of polycyclic aromatic hydrocarbons (PAHs) in good yields (ca. 40–58 %).     

A Lagrangian Relaxation Heuristic for Capacitated Facility Location with Single-Source Constraints

Facility location models are applicable to problems in many diverse areas, such as distribution systems and communication networks. In capacitated facility location problems, a number of facilities with given capacities must be chosen from among a set of possible facility locations and then customers assigned to them. We describe a Lagrangian relaxation heuristic algorithm for capacitated problems in which each customer is served by a single facility. By relaxing the capacity constraints, the uncapacitated facility location problem is obtained as a subproblem and solved by the well-known dual ascent algorithm. The Lagrangian relaxations are complemented by an add heuristic, which is used to obtain an initial feasible solution. Further, a final adjustment heuristic is used to attempt to improve the best solution generated by the relaxations. Computational results are reported on examples generated from the Kuehn and Hamburger test problems.     

Mesoporous cadmium sulfide nanoparticles derived from a new cadmium anthranilato complex: Characterization and induction of morphological abnormalities in pathogenic fungi

A cadmium complex of the general formula Cd(C₁₃H₉O₂NCl)₂(H₂O)₂ {C₁₃H₉O₂NCl = 2-(4-chlorophenylamino)benzoate} was synthesized and characterized regarding its CHN data, solution molar conductivity and spectroscopic (UV–Vis. and IR) properties. Cadmium sulfide nanoparticles (CdS NPs) were grown form the microcrystalline complex and thiourea via a hydrothermal route. The as-prepared NPs were assigned based on X-ray powder diffraction (PXRD), transmission electron microscopy (TEM), field emission scanning electron microscopy (FE-SEM) and Brunauer – Emmett – Teller (BET) surface area measurements. The CdS absorption and emission spectra were also recorded that revealed an energy gap of 2.47 eV and large Stokes shift of 130 nm. For the as-prepared NPs, the measurements have also indicated a mesoporous structure and an average particle size of 20–28 nm associated with an average pore diameter of 11.21 nm. The as-synthesized CdS NPs acted as antifungal controlling agent against human and plant pathogenic fungi of serious environmental and health concerns. The NPs at concentration of 200 ppm inhibited several fungi with inhibition efficiency of 100% against Aspergillus ustus Au-28. The nanoparticles induced morphological abnormalities in fungal mycelia, conidia and vesicle. Additionally, they inhibited the conidia septum formation, accelerated the chlamydospores generation and enlarged the yeast cells.     

V2O5 based quadruple nano‐perovskite as a new catalyst for the synthesis of bis and tetrakis heterocyclic compounds

In this article, we presented a novel, efficient and facile approach for using strontium titanate supported catalyst in organic synthesis. Bis and tetrakis of coumarin, indole and xanthene derivatives can effortlessly have prepared using V₂O₅/perovskite nanoparticles (NPs) under solvent‐free condition. V₂O₅/perovskite in (NPs) was prepared and identified using Fourier transform infrared spectroscopy (FTIR), X‐ray diffraction (XRD) and scanning electron microscope supported with energy dispersive X‐ray (SEM/EDAX). Calculated crystal size was from the intense XRD peaks was found to range between 50–60 nm in agreement with that obtained from the transmission electron microscopic investigation. EDAX analysis and mapping images reveal a homogenous distribution of all constituents with their calculated ratios in the synthesized catalyst.