SYNTHESIS, IN VITRO ANTIMICROBIAL, ANTI-LIVER CANCER EVALUATION OF SOME NOVEL BIS-CYANOACRYLAMIDE AND BIS-AZOLES DERIVATIVES

Objective: Synthesis of some novel bis [3-(aryl)-2-cyanoacrylamide], bis-pyrazole, bis-thiazole and bis-triazole derivatives starting from N,N'-ethane-1,2-diylbis(2-cyanoacetamide) (1) to evaluate for their in-vitro antibacterial, antifungal and anticancer activities.Methods: Reaction of N, N'-ethane-1,2-diylbis(2-cyanoacetamide) (1) with different aromatic and heteroaromatic aldehydes yielded the corresponding bis[3-(aryl)-2-cyanoacrylamide] derivatives, which reacted with hydrazine hydrate to give N,N'-ethane-1,2-diylbis[3-amino-5-(4-aryl)-1H-pyrazole-4-carboxamide] derivatives. Compound 1 reacted with each of thioglycolic acid, Phenyl isocyanate and elemental sulfur in presence triethylamine to give bis-thiazole derivatives. Diazotization of 1 with the desired diazonium chloride yielded the bis-hydrazone derivatives. The latter compounds refluxed with hydroxylamine hydrochloride and chloro- acetonitrile to give bis-triazole and bis-pyrazole derivatives respectively.Results: The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H NMR, [13]C NMR and mass spectral data. A total fourteen new synthesized compounds were evaluated for their in-vitro antibacterial, antifungal and anticancer activities against human liver cancer cell line (HEPG-2).Conclusion: The results obtained indicated that some of such compounds showed promising activities against Gram-positive, Gram-negative bacteria, fungi and anticancer activity in relation to the reference drugs ampicillin, gentamicin, Amphotericin B and vinblastine respectively.Â

Synthesis and Characterization of Some New Bis-Pyrazolyl-Thiazoles Incorporating the Thiophene Moiety as Potent Anti-Tumor Agents

A new series of 1,4-bis(1-(5-(aryldiazenyl)thiazol-2-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-3-yl)benzenes 3a–i were synthesized via reaction of 5,5′-(1,4-phenylene)bis(3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide) (1) with hydrazonoyl halides 2a–i. In addition, reaction of 1 with ethyl chloroacetate afforded bis-thiazolone derivative 8 as the end product. Reaction of compound 8 with methyl glyoxalate gave bis-thiazolone derivative 10. The structures of the newly synthesized compounds were established on the basis of spectroscopic evidences and their alternative syntheses. All the synthesized compounds were evaluated for their anti-tumor activities against hepatocellular carcinoma (HepG2) cell lines, and the results revealed promising activities of compounds 3g, 5e, 3e, 10, 5f, 3i, and 3f with IC50 equal 1.37 ± 0.15, 1.41 ± 0.17, 1.62 ± 0.20, 1.86 ± 0.20, 1.93 ± 0.08, 2.03 ± 0.25, and 2.09 ± 0.19 μM, respectively

Performance of Statistical and Intelligent Methods in Estimating Rock Compressive Strength

This research was conducted to forecast the uniaxial compressive strength (UCS) of rocks via the random forest, artificial neural network, Gaussian process regression, support vector machine, K-nearest neighbor, adaptive neuro-fuzzy inference system, simple regression, and multiple linear regression approaches. For this purpose, geo-mechanical and petrographic characteristics of sedimentary rocks in southern Iran were measured. The effect of petrography on geo-mechanical characteristics was assessed. The carbonate and sandstone samples were classified as mudstone to grainstone and calc-litharenite, respectively. Due to the shallow depth of the studied mines and the low amount of quartz minerals in the samples, the rock bursting phenomenon does not occur in these mines. To develop UCS predictor models, porosity, point load index, water absorption, P-wave velocity, and density were considered as inputs. Using variance accounted for, mean absolute percentage error, root-mean-square-error, determination coefficient (R2), and performance index (PI), the efficiency of the methods was evaluated. Analysis of model criteria using multiple linear regression allowed for the development of a user-friendly equation, which proved to have adequate accuracy. All intelligent methods (with R2 > 90%) had excellent accuracy for estimating UCS. The percentage difference of the average of all six intelligent methods with the measured value was equal to +0.28%. By comparing the methods, the accuracy of the support vector machine with radial basis function in predicting UCS was (R2 = 0.99 and PI = 1.92) and outperformed all the other methods investigated

Dendrimers: A New Race of Pharmaceutical Nanocarriers

Dendrimers are nanosized, symmetrical molecules in which a small atom or group of atoms is surrounded by the symmetric branches known as dendrons. The structure of dendrimers possesses the greatest impact on their physical and chemical properties. They grow outwards from the core-shell which further reacts with monomers having one reactive or two dormant molecules. Dendrimers’ unique characteristics such as hyperbranching, well-defined spherical structure, and high compatibility with the biological systems are responsible for their wide range of applications including medical and biomedical areas. Particularly, the dendrimers’ three-dimensional structure can incorporate a wide variety of drugs to form biologically active drug conjugates. In this review, we focus on the synthesis, mechanism of drug encapsulations in dendrimers, and their wide applications in drug delivery

Employing Sisko non-Newtonian model to investigate the thermal behavior of blood flow in a stenosis artery: Effects of heat flux, different severities of stenosis, and different radii of the artery

In this paper, a numerical investigation is carried out to study the blood flow behavior within the stenosis artery. An artery is under applying a constant heat flux on the boundary walls in this simulation. Lumen model is employed for simulation of the artery and the Sisko model is used to indicate properties of blood as non-Newtonian fluid. Also, the cone geometry of stenosis with different severities and radii are simulated. Then, effects of heat flux, different severities of stenosis, and different radii of the artery are studied on the blood flow behavior. It is reported that before stenosis, velocity is increasing and heat transfer rate is also increasing which cause temperature to be decreased in stenosis position. But after stenosis, velocity is decreased. Consequently, heat transfer rate is decreased which leads to reduction in blood temperature. Also, since the blood particles adhere to the arterial wall, with increasing radial distance from the walls, velocity is increased, which causes maximum velocity to be found in the central region. Moreover, the thermal driving force is damped in the lateral region of the artery and does not affect velocity. On the other side, as the severity increases step by step, the temperature decreases, respectively. In fact, the cross-sectional area decreases with increasing severity of stenosis. Consequently, velocity increases and causes heat transfer enhancement, which leads to a reduction in blood temperature. Therefore, the highest temperatures are related to the artery with an intensity of 20%. Although the cross-section area of the artery can change blood temperature, but its role can be ignorable in temperature enhancement and body healthy in this regard

Curcumin Nanoparticles as Promising Therapeutic Agents for Drug Targets

Curcuma longa is very well-known medicinal plant not only in the Asian hemisphere but also known across the globe for its therapeutic and medicinal benefits. The active moiety of Curcuma longa is curcumin and has gained importance in various treatments of various disorders such as antibacterial, antiprotozoal, cancer, obesity, diabetics and wound healing applications. Several techniques had been exploited as reported by researchers for increasing the therapeutic potential and its pharmacological activity. Here, the dictum is the new room for the development of physicochemical, as well as biological, studies for the efficacy in target specificity. Here, we discussed nanoformulation techniques, which lend support to upgrade the characters to the curcumin such as enhancing bioavailability, increasing solubility, modifying metabolisms, and target specificity, prolonged circulation, enhanced permeation. Our manuscript tried to seek the attention of the researcher by framing some solutions of some existing troubleshoots of this bioactive component for enhanced applications and making the formulations feasible at an industrial production scale. This manuscript focuses on recent inventions as well, which can further be implemented at the community level