The present series of compounds were synthesized with the aim to develop newer anticonvulsant agents that are comparatively more efficacious and safer than the currently used anticonvulsant agents. Various thiazolyl coumarins were synthesized by the reaction of 3-(bromoacetyl)-2H-chromen-2-one with different substituted aryl thiourea. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing Pen Tylenetetra Zoleinduced seizure (PTZ) and Maximal Electroshock Seizure (MES) tests at 30, 100 and 300 mg kg −1 dose level. Neurotoxicity and ethanol potentiation test of the compounds were also assessed at the same dose level. Two compounds of the series 3g and 3j exhibited significant anticonvulsant activity at 30 mg kg −1 dose level with lesser neurotoxicity than the standard drug phenytoin.
Background:In most African and Arabic countries tuberculosis (TB) causes great economic losses in bovine species and constitutes serious zoonotic problem. As the traditional diagnostic method delay the research because of low sensitivity and specificity, a rapid method of diagnosis is of outmost importance.Aim:The study was designed to evaluate the two rapid diagnostic methods of TB in cattle, further to differentiate between infected and bacillus Calmette-Guerin (BCG) vaccinated animals.Materials and Methods:Intradermal tuberculin test was applied to 300 cattle. Of these cattle, 15 cattle were vaccinated from cattle negative to tuberculin test with BCG. Blood samples were taken for lymphocyte separation to apply polymerase chain reaction (PCR) upon and for serum preparation for the enzyme-linked immunosorbent assay (ELISA) application, this blood collected from 65 cattle classified into three groups, viz. positive tuberculin test (35 animals), negative tuberculin test (15 animals), and vaccinated cow with BCG (15 animals). From blood samples lymphocytes were separated and the isolated lymphocytes were subjected to PCR and serum for ELISA application. Blood samples, specimens from lymph nodes and specific tissues were taken for PCR and for cultivation and isolation of Mycobacterium bovis.Results and Conclusions:The results of this study revealed that PCR can be used as rapid efficient and accurate diagnostic test in detection of ruminant TB. Moreover, cattle's ELISA reading showed higher sensitivity in positive tuberculin animals. However, the differentiations between vaccinated and infected animals not clear by using a single antigen only.
A series of dihalosubstituted thiocarbamide derivatives (5a-e, 6a-e, 7a-e, and 8a-e) were synthesized as antitubercular agents. The structures of dihalosubstituted thiocarbamide derivatives were established on the basis of IR, 1 H, 13 C NMR, and mass spectral data. All the compounds were tested in vitro for antimycobacterial activity against Mycobacterium tuberculosis (ATCC-25177) by well-diffusion method and MIC by serial dilution method. Results of the antitubercular screening revealed that some of the compounds showed moderate to good antitubercular activity. Of all the compounds tested, two derivatives viz., 8d and 8e expressed MIC of 25 lg/ml, and one compound 7e showed MIC of 12.5 lg/ml against M. tuberculosis (ATCC-25177).
A mucoadhesive microemulsion of lipophilic silymarin (SLMMME) was developed to treat Parkinson’s disease (PD). Optimization of the SLM microemulsion (ME) was performed using Central Composite Design (CCD). The composition of oil, surfactant, co-surfactant, and water was varied, as per the design, to optimize their ratio and achieve desirable droplet size, zeta potential, and drug loading. The droplet size, zeta potential, and drug loading of optimized SLMME were 61.26 ± 3.65 nm, −24.26 ± 0.2 mV, and 97.28 ± 4.87%, respectively. With the addition of chitosan, the droplet size and zeta potential of the developed ME were both improved considerably. In vitro cell toxicity investigations on a neuroblastoma cell line confirmed that SLMMME was non-toxic and harmless. In comparison to ME and drug solution, mucoadhesive ME had the most flow through sheep nasal mucosa. Further, the in vitro release showed significantly higher drug release, and diffusion of the SLM loaded in MEs than that of the silymarin solution (SLMS). The assessment of behavioral and biochemical parameters, as well as inflammatory markers, showed significant (p < 0.05) amelioration in their level, confirming the significant improvement in neuroprotection in rats treated with SLMMME compared to rats treated with naïve SLM.
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