Integration of sensor vision capabilities on UAV flight route optimization: A linear model and a heuristic algorithm proposal

Nowadays countries provide great resources for the research and development activities to develop Unmanned Air Vehicle technologies. The most important problem encountered in efficient use of these technologically intensive systems is to determine the minimum cost route plan which can observe the maximum number of targets. Unmanned Air Vehicle Route Optimization Problem is considered as the integration of Traveling Salesman Problem and Vehicle Routing Problem in the literature. Unmanned Air Vehicle Route Models can be developed by incorporating the vision capabilities of the sensors into the route plan. In this study, taking into account the sensor capabilities an integrated linear model and a two-phased heuristic routing algorithm are proposed for the route planing process of Unmanned Air Vehicle. A generic scenario related to surveillance and reconnaissance activities on southern borderline of Turkey has been developed in order to test the proposed models. The test results show that integrating sensor vision capabilities on Unmanned Air Vehicle flight route model is effective in minimization of total flight distance and the proposed two-phased heuristic routing algorithm can be effectively used in the Unmanned Air Vehicle route planing process

Antipsychotic agents screened as human carbonic anhydrase I and II inhibitors

WOS: 000334916900004PubMed: 24289818The antipsychotic drugs currently used to treat schizophrenia can be divided into two distinct classes, typical and atypical antipsychotics. Many drug molecules are enzyme inhibitors that bind reversibly or irreversibly to their target through intermolecular interactions. That's why enzyme inhibition studies are an important issue for drug design and biochemical applications. In this study, in vitro inhibition effect of some antipsychotic drugs on the purified carbonic anhydrase (CA) I and II isoenzymes were investigated by using CO2 as a substrate. CA I and II were purified from human erythrocytes by a simple one step procedure using Sepharose 4B-L-tyrosine-sulfonamide affinity column. The results showed that all the drugs inhibited the cytosolic carbonic anhydrases enzyme activity in a concentration-dependent fashion. Among the studied drugs, aripiprazole and pramipexole were found to be the most active one for hCA I (IC50: 3.64 and 5.37 mu M) and hCA II (IC50: 4.16 and 4.81 mu M) activity, respectively

Comparative experimental study on the modification of microstructural and mechanical properties of friction stir welded and gas metal arc welded EN AW-6061 O aluminum alloys by post-weld heat treatment

In this paper, the effects of post-weld heat treatment on modification of microstructures and mechanical properties of friction stir welded and gas metal arc welded AA6061-O plates were compared with each other. Gas metal arc welding and friction stir welding were used as the applicable welding processes for AA6061-O alloys. The applied post-weld heat treatment consisted of solution heat treatment, followed by water quenching and finally artificial aging. The samples were classified as post-weld heat treated and as-welded joints. The microstructural evolution, tensile properties, hardness features and fracture surfaces of both as-welded and post-weld heat treated samples were reported. The results clearly showed that friction stir welding process demonstrated better and more consistent mechanical properties by comparison with the gas metal arc welding process. The weld region of as-welded samples exhibited a higher hardness value of 80 HV0.1 compared to the base material. In addition, the feasibility of post-weld heat treatment in order to enhance the mechanical properties and to obtain more homogeneous microstructure of 6061-O aluminum alloys was evaluated

The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes

Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the in vitro effects of 35 frequently used cardiac drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined with both the hydratase and esterase methods. The most potent inhibitors observed were propafenone (hCA I: 2.8 µM and hCA II: 3.02 µM) and captopril (hCA I: 1.58 µM and hCA II: 6.25 µM). Isosorbide mononitrate, propranolol, furosemide, and atorvastatin were also potent inhibitors. The inhibitor constant, Ki, value from the Lineweaver–Burk plot for propafenone was 2.38 µM for hCA I and 2.97 µM for hCA II. The tested cardiac drugs showed potent in vitro inhibition of the hCA I and II isozymes. Especially, in patients with atherosclerotic heart disease, these drugs may be preferred primarily due to the beneficial effects of carbonic anhydrase inhibition on atherosclerosis

Synthesis and Evaluation of New Phthalazine Urea and Thiourea Derivatives as Carbonic Anhydrase Inhibitors

A new series of phthalazine substituted urea and thiourea derivatives were synthesized, and their inhibitory effects on the activity of purified human carbonic anhydrases (hCAs I and II) were evaluated. 2H-Indazolo[2,1-b]phthalazine-trione derivative (1) was prepared with 4-nitrobenzaldehyde, dimedone, and phthalhydrazide in the presence of TFA in DMF, and nitro group was reduced to amine derivative (2) with SnCl2·2H2O. The compound was reacted with isocyanates and isothiocyanates to get the final products (3a–p). The results showed that all the synthesized compounds inhibited the CA isoenzymes activity. 3a (IC50 = 6.40 µM for hCA I and 6.13 µM for hCA II) has the most inhibitory effect. The synthesized compounds are very bulky to be able to bind near the zinc ion, and they much more probably bind as the coumarin derivatives

Development of carbazole-bearing pyridopyrimidine-substituted urea/thiourea as polyphenol oxidase inhibitors: synthesis, biochemistry, and theoretical studies

Polyphenol oxidase (Tyrosinase, PPO) has received considerable attention, since it is the key enzyme in melanin biosynthesis. In this study, we investigated prepared novel carbazole-containing pyridopyrimidine-substituted with urea and thiourea derivatives and their PPO activities on the diphenolase activity of banana tyrosinase. The structures of the compounds synthesized were confirmed by 1 H NMR, 13 C NMR, FTIR and elemental analysis. PPO enzyme was purified from banana on an affinity gel comprised of Sepharose 4B-L-tyrosine-p-amino benzoic acid. For evaluating the enzyme activity, the synthesised compounds were subjected to tyrosinase inhibition assay using catechol as substrate. While some of the compounds (6, 7, 8f, 8h, 8i, 8j) showed enzyme inhibitor effect, some of them (8a, 8b, 8c, 8d, 8e, 8g, 8k) activated the PPO enzyme activity. Gaussian software was used for the molecular calculations to explain the results for the prepared compounds

In vitro effects of estrogen and progesterone containing drugs on human erythrocyte carbonic anhydrase I and II isozymes in women smokers and nonsmokers

Background: Carbonic anhydrases (CAs), a group of metalloenzymes, are involved in numerous physiological and pathological processes such as acid–base balance, gluconeogenesis, lipogenesis, ureagenesis, electrolyte secretion in various tissues, bone resorption and calcification, and tumorigenicity. In the current study, we aimed to determine and compare possible alterations in the activity of carbonic anhydrase I (CA I) and carbonic anhydrase II (CA II) isozymes by using estrogens and progestagens in female smokers and nonsmokers. Methods: Blood samples from 30 smoker and 30 nonsmoker volunteers were drawn after obtaining informed consent. The blood samples were centrifuged to separate the plasma and erythrocytes. Thereafter, hemolysate was prepared from the red cells. CA I and CA II were purified from human erythrocytes with a simple one-step procedure using Sepharose 4B-l-tyrosine-sulfonamide affinity column. CAI and CA II isozymes were treated with estrogen and progesterone-containing drugs, after which the inhibition or activation of the enzyme was determined. Results: CA I and CA II enzyme activity was observed to be increased in female smokers. The results of this study show that dienogest is the most effective inhibitor for human erythrocytes CA I when compared with micronized progesterone, hydroxyprogesterone caproate, estradiol valerate, and estradiol hemihydrate in both female smokers and nonsmokers. All active ingredients have been shown to have a stronger inhibition in smokers than nonsmokers for CA I activity. Additionally, estradiol valerate and hydroxyprogesterone caproate have stronger inhibition against CA II enzyme activity in women who smoke. Conclusion: The results of the current study provide important information to clinicians about how to consider the possible adverse effects of these drugs which are produced as a result of inhibition of CA I and CA II enzyme. Clinicians should take into consideration the side effects caused by CA I and CA II enzyme inhibition when prescribing these drugs in the treatment of different clinical conditions, especially in women who smoke

INHIBITION OF CARBONIC ANHYDRASE I AND II WITH TOTAL ANTHOCYANINS EXTRACTED FROM SWEET CHERRY CULTIVARS

Total anthocyanins were extracted from six sweet cherry cultivars grown in Sakarya, Turkey. In vitro inhibition effects of the extracted total anthocyanins on purified carbonic anhydrase I and II were investigated using CO2 as a substrate. All the extracted total anthocyanins inhibited the activity of the human carbonic anhydrase (hCA) I and II enzymes. Among all the cultivars, 'Karakiraz' was found to be the most active on both hCA I (IC50 = 30.59 mu g/mL) and hCA II activity (IC50 = 44.52 mu g/mL). Additionally, all the cultivars have higher inhibitory activity on hCA I than hCA II

Synthesis and evaluation of new phthalazine substituted beta-lactam derivatives as carbonic anhydrase inhibitors

A new series of phthalazine substituted beta-lactam derivatives were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA I and II) were evaluated. 2H-Indazolo[2,1-b]phthalazine-trione derivative was prepared with 4-nitrobenzaldehyde, dimedone, and phthalhydrazide in the presence of TFA in DMF, and the nitro group was reduced to 13-(4-aminophenyl)-3,3-dimethyl-3,4-dihydro-2H-indazolo[1,2-b]phthalazine-1,6,11(13H)-trione with SnCl2 center dot 2H(2)O. The reduced compound was reacted with different aromatic aldehydes, and phthalazine substituted imines were synthesized. The imine compounds undergo (2+2) cycloaddition reactions with ketenes to produce 2H-indazolo[2,1-b]phthalazine-trione substituted beta-lactam derivatives. The beta-lactam compounds were tested as inhibitors of the CA isoenzyme activity. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. 1-(4-(3,3-dimethyl-1,6,11-trioxo-2,3,4,6,11,13-hexahydro-1H-indazolo[1,2b]phthalazin-13-yl)phenyl)-2-oxo-4-p-tolylazetidin-3-yl acetate (IC50 = 6.97 A mu M for hCA I and 8.48 A mu M for hCA II) had the most inhibitory effect