Sinteza i anthelmintičko djelovanje novih 2-supstituiranih-4,5-difenil imidazola

A series of 2-substituted-4,5-diphenyl imidazoles 1a-j were synthesized by refluxing benzil with different substituted aldehydes in the presence of ammonium acetate and glacial acetic acid. Structures of the synthesized compounds were confirmed on the basis of IR, 1H NMR and mass spectral data. Compounds 1a-j were screened for anthelmintic activity. Test results revealed that compounds showed paralysis time of 0.24 to 1.54 s and death time of 0.39 to 4.40 s while the standard drugs albendazole and piperazine citrate showed paralysis time of 0.54 and 0.58 s and death time of 2.16 and 2.47 s, respectively, at the same concentration of 1 % (m/V). Five compounds, 2-[2-hydroxyphenyl]-4,5-diphenyl imidazole (1b), 2-[3-methoxyphenyl]-4,5-diphenyl imidazole (1c), 2-[2-phenylethenyl]-4,5-diphenyl imidazole (1e), 2-[4-fluorophenyl]-4,5-diphenyl imidazole (1g) and 2-[3-nitrophenyl]-4,5-diphenyl imidazole (1h) showed significant anthelmintic activity compared to the standard drugs.Refluksiranjem benzila s različitim supstituiranim aldehidima u prisutnosti amonijeva acetata i ledene octene kiseline sintetizirana je serija 2-supstituiranih-4,5-difenil imidazola (1a-j). Strukture sintetiziranih spojeva potvrđene su IR, 1H NMR i masenom spektroskopijom. U testovima na anthelmintičko djelovanje određeno je vrijeme paralize 0,24 do 1,54 min i vrijeme smrti 0,39 do 4,40 min, dok standarni lijekovi albendazol i piperazin citrat imaju vrijeme paralize 0,54 i 0,58 min, a vrijeme smrti 2,16, odnosno 2,47 min pri istim koncentracijama (1 % m/V). Pet spojeva, 2-[2-hidroksifenil]-4,5-difenil imidazol (1b), 2-[3-metoksifenil]-4,5-difenil imidazol (1c), 2-[2-feniletenil]-4,5-difenil imidazol (1e), 2-[4-fluorofenil]-4,5-difenil imidazol (1g) i 2-[3-nitrofenil]-4,5-difenil imidazol (1h) pokazuju značajno anthelmintičko djelovanje u odnosnu na standardne lijekove

Synthesis of Some New Isoxazoline Derivatives of Chalconised Indoline 2-one as a Potential Analgesic, Antibacterial and Anthelmimtic Agents

A series of novel 1[5”-(2”’-substituted phenyl)-4”,5”’-dihydro isoxazole-3”-yl]-3-[(4 substituted phenyl)imino]1-3-dihydro-2H-indole-2-one were synthesized from different substituted chalconised indole-2,3-dione was prepared from the different chalconised Isatin. The structures of the compounds were elucidated by elemental and spectral (IR, 1H NMR, and MS) analysis. The synthesized compounds were screened for their analgesic activity by the acetic acid induced Writhing method and in vitro antimicrobial activity against the Gram-positive bacteria—Staphylococcus aureus and the Gram-negative bacteria—Pseudomonas auroginosa, Pseudomonas mirabilis, and E. coli by the cup plate agar diffusion method. Compounds 6a1, 6a3, 6b3, and 6b2 were found to be active against bacteria. The compounds 6a1, 6b3, and 6a3 show a significant analgesic activity. Synthesized compounds also screened for anthelmintic activity against Pheretima posthuma. Compounds 6a1, 6b1, and 6b3 show significant anthelmintic activity

Sarcophine-Diol, a Skin Cancer Chemopreventive Agent, Inhibits Proliferation and Stimulates Apoptosis in Mouse Melanoma B16F10 Cell Line

Sarcodiol (SD) is a semi-synthetic derivative of sarcophine, a marine natural product. In our previous work, we reported the significant chemopreventive effects of SD against non-melanoma skin cancer both in vitro and in vivo mouse models. In this investigation, we extended this work to study the effect of sarcodiol on melanoma development, the more deadly form of skin cancer, using the mouse melanoma B16F10 cell line. In this study we report that SD inhibits the de novo DNA synthesis and enhances fragmentation of DNA. We also evaluated the antitumor effect of SD on melanoma cell viability using several biomarkers for cell proliferation and apoptosis. SD inhibits the expression levels of signal transducers and activators of transcription protein (STAT-3) and cyclin D1, an activator of cyclin-dependent kinase 4 (Cdk4). SD treatment also enhances cellular level of tumor suppressor protein 53 (p53) and stimulates cleavage of the nuclear poly (ADP-ribose) polymerase (cleaved-PARP). SD also enhances cellular levels of cleaved Caspase-3, -8, -9 and stimulates enzymatic activities of Caspase-3, -8 and -9. These results, in addition to inhibition of cell viability, suggest that SD inhibits melanoma cell proliferation by arresting the cell-division cycle in a Go quiescent phase and activates programmed cell death (apoptosis) via extrinsic and intrinsic pathways. Finally, these studies demonstrate that SD shows a very promising chemopreventive effect in melanoma B16F10 tumor cells

Synthesis and Biological Evaluation of Substituted Thiazolo(4,5-d)Pyrimidines and Substituted Pyrimidines as Corticotropin Releasing Factor (CRF) Receptor Antagonists

Corticotropin releasing factor (CRF) is a neuropeptide hormone produced from the hypothalamus that coordinates behavioral, endocrine and autonomic functions in stress response and its dysregulation has been implicated in stress disorders, depression, anxiety, irritable bowel disorder, alcohol and addictive drug withdrawal symptoms. New drugs that can target the CRF function may represent a new development of neuropsychiatric medicines to treat various stress-related disorders. Several classes of small molecule non-peptide CRF receptor antagonists have been developed and, in this study, two series of new pyrimidines and thiazolo[4,5-d]pyrimidines were designed based on the structural features of the basic pharmacophore and prominent CRF antagonists. A total of 79 compounds were synthesized including all intermediates and final target compounds. A multi-step synthesis was used to prepare each group of the target compounds. The detailed synthesis of all compounds is described and the structures of all the synthesized compounds are characterized and confirmed by spectral data including 1H NMR, 13C-NMR, mass spectroscopy and also micro-elemental analysis for all the final compounds. The 50 final target compounds were screened for their binding affinity to CRF1 receptors on two stages. The first stage was screening the compounds for their ability to inhibit the [125I]Tyr0-Savaugine binding to the CRF1 receptors in HEK 293 cells at 500- 1000 nM concentration. Based on initial screening studies, in the second stage, derivatives that showed 50% or more inhibition were selected for competition binding studies to further determine their IC50 values. Comparison with Antalarmin, a potent CRF1 antagonist, were also carried out in competition binding study. None of the 22 substituted thiazolo[4,5-d]pyrimdines showed 50% or more inhibition at 1000 nM, and thus were not considered for the second evaluation protocol. On the other hand, four new pyrimidines showed 50% or more inhibition of binding of [125I]Tyr0-Savaugine to the CRF1 receptors and thus passed on to the second protocol. These four compounds showed -log IC50 values of 6.61-6.27 compared to -log IC50 value of 7.73 for Antalarmin used as a standard CRF1 receptor antagonist. It was concluded that further structural modifications of these four lead compounds may lead to compounds with superior CRF1 antagonist activity and a potential for development as new antidepressant and anti-anxiety agents

ANTI-DIARRHOEAL ACTIVITY OF CARDIOSPERMUM HALICACABUM AND DODONEA VISCOSA

Objective: The present study to carry out the anti-diarrhoeal activity of leaf extracts of Cardiospermum halicacabum and Dodonea viscosa in different experimental models of diarrhoea. Methods: The acute toxicity of the extracts were determined, LD50was calculated according to the Up and down method†following OECD guidelines No. 425 of CPCSEA. The anti-diarrhoeal potential was assessed by castor oil induced diarrhea. Gastro-intestinal motility test and Prostaglandin-E2 induced enteropooling in experimental animals. Results: The alcoholic and aqueous extracts of Cardiospermum halicacabum and Dodonea viscosa have exhibited the dose dependant antidiarrhoeal activity in all the three experimental models by reducing the frequency of defecation as well as total weight of wet faeces, decreased the propulsion of charcoal meal through the gastrointestinal tract and also decrease in the oedema volume in the intestine (intestinal secretion) of the drug treated animals with the respective models of diarrhea. Conclusion: Cardiospermum halicacabum and Dodonea viscosa shows to have a potential value for the development of a phytomedicine for diarrhoea. Further comprehensive chemical and pharmacological investigations are needed to elucidate the exact mechanism accountable for the exhibited activity

A Review on Methods of Noise Attenuation in Engineering Design Applications

Nose is an unwanted sound that causes annoyance. It has been proved that the noise has an adverse effect on living things including human beings. Noise pollution norms have been laid down by OSHA (Occupational Safety and Health Administration) and Euro Norms. It is apparent that there exists a scope for the research in the design and development of noise attenuation methods and materials. In present review, the contributions of the researchers in design, testing and implementation of noise engineering in attaining the attenuation is focussed. Application of numerical, finite element analysis and experimentation analysis to study and to investigate acoustic materials in achieving noise attenuation are discussed. It also provides useful information in extending these studies and approaches with respect to macro and micro level material analysis in engineering design applications and thin film noise attenuation as well

Finite element analysis of Spiral bevel gears pair used in an Automobile Differential gear box

This paper covers the static, fatigue, modal and harmonic analysis of Spiral bevel gears pair used as drive pinion and crown wheel in the differential gearbox of Tata Ace vehicle, using a popular commercial finite element analysis software ANSYS. The main goals are to estimate the life and early detection of failure of the spiral bevel gears pair, during operation. The solid models of gears are created by using the widely used solid modeling software CATIA V5. The goals are achieved by comparing the results of FEA of new gears pair with the results of gears pair having a crown pinion with one tooth broken. A review of work done so far on Finite element analysis of bevel gears is also presented

<b style="">Wound healing activity of <i>Cordia dichotoma</i> Forst. f. fruits</b><b style=""></b>

99-102The extraction of fruits of Cordia dichotoma Forst. f. was carried out using ethanol. This extract was further fractionated using petroleum ether (40-60%), solvent ether, ethyl acetate, butanol and butanone in succession. These fractions were screened for wound healing activity using three different models, viz. excision, incision and dead space wound models on either sex of albino rats of Wistar strain. All the fractions showed significant (P<0.001) activity on the chosen models