Validated, Ultra Violet Spectroscopy Method for the Dissolution Study of Mycophenolate Mofetil Immediate Release 500mg Tablets

A simple, selective and precise dissolution method was developed and validated for the Mycophenolate mofetil immediate release tablets. The method employed dissolution medium 0.1N HCl (pH1.2) and volume 900ml with USP-II apparatus (Paddle). Detection was made by measuring the absorbance on UV at the λ~max~ 250nm. The method show the linearity in the range of conc. 5[mu]g/ml to 40[mu]g/ml with r^2^=0.999. The method is also validated as per International Conference of Harmonization guidelines. The method showed the specificity with standard deviation 0.00. The method is repeatable, selective and accurate for the dissolution study of Mycophenolate mofetil immediate release tablets

Anticonvulsant activity of Bacopa monniera in rodents

Bacopa monniera, da família Scrophulariaceae, e comumente denominada Brahmi, é bem conhecida na Índia por sua atividade no Sistema Nervoso Central, mas seu efeito neurofarmacológico não foi, ainda, explorado. No presente estudo, investigaram-se os efeitos antiepilépticos da planta. O extrato etanólico da Bacopa monniera foi testado quanto à atividade anticonvulsivante em ratos albinos, utilizando-se diferentes modelos de convulsão. O extrato etanólico das folhas produziu atividade anticonvulsivante significativa para todos os diferentes modelos estudados. O presente estudo mostra provável mecanismo de ação semelhante ao dos benzodiazepínicos (agonista do GABA). Assim sendo, esses resultados enfatizam a necessidade de diversificar, utilizando-se abordagens terapêuticas alternativas da medicina natural, em que uma planta facilmente disponível pode fornecer soluções para vários desafios terapêuticos, como o observado na ação anticonvulsivante do extrato etanólico de Bacopa monniera.Bacopa monnieri (L), belonging to the Scrophulariaceae family and commonly known as Brahmi, is well known in India for its CNS activity but its neuropharmacological effect has not yet been explored. In the present study, the antiepileptic effects of the plant were investigated. The ethanolic extract of Bacopa monniera was tested for anticonvulsant activity in albino rats, using different convulsive models. The ethanolic extract of leaves produced significant anticonvulsant activity for all the different models studied. The present study shows a probable mechanism of action similar to that of benzodiazepines (GABA agonist). Thus, these results emphasize the need to diversify by using alternative therapeutic approaches pertaining to herbal medicine, where a single easily available plant may provide solutions to several therapeutic challenges, as observed in the anticonvulsant action of ethanolic extract of B. monniera

Sinteza i preliminarna ispitivanja antikonvulzivnog djelovanja derivata benzotiazol-2-il tiadiazola

Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N\u27-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100 % indicative of the promising nature of the compounds against the seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.U radu je opisano dizajniranje i sinteza različitih N-(5-klor-6-supstituiranih-benzotiazol-2-il)-N\u27-(supstituiranih fenil)-[1,3,4]tiadiazol-2,5-diamina (5a-t) polazeći od odgovarajućih acetofenona. Strukture spojeva određene su na temelju spektroskopskih podataka i elementarne analize. Ispitano je antikonvulzivno djelovanje svih novosintetiziranih spojeva i uspoređeno s djelovanjem natrijeve soli fenitoina. Spojevi 5b i 5c pružaju potpunu zaštitu od konvulzija uzrokovanih MES-om, a svi spojevi štite od konvulzija u rasponu od 50 do 100 %

Recent thiazolidinediones as antidiabetics

99-109Thiazolidinediones, a class of oral insulin sensitizing agents that improve insulin resistance, are agonists of peroxisome proliferator activated receptor-ϒ (PPAR-ϒ). Two clinically used drugs pioglitazone (ACTOS) and rosiglitazone (AVANDIA) have made a great contribution to therapy for type 2 diabetes. However, weight gain and hepatotoxicity are side effects of thiazolidinediones. For thiazolidinediones with lesser side effects, researchers are focusing on modification of side chain at C-5 of thiazolidinedione nucleus and its derivatization. Netoglitazone possesses both PPAR-⍺/ϒ dual agonistic activity. More thiazolidinedione derivatives like DRF-2189, PHT46, PMT13, DRF-2519 can be utilized as potent antidiabetic agents in future

QSAR Optimization of Benzofuran and Benzothiophene Sulfono Biphenyl as Potent PTPase-1B Inhibitors

ABSTRACT: Insulin resistance is associated with a defect in protein tyrosine phosphorylation in the insulin signal transduction cascade. Protein tyrosine phosphatase (PTPase) enzyme dephosphorylates the active form of insulin receptor and thus attenuates its tyrosine kinase activity, therefore the need of potent PTPase inhibitor is there with that intention the Quantitative structure-activity relationship QSAR was performed. QSAR has been established on a series of compounds of novel sulfono biphenyl analogs using SYSTAT (Version 7.0) software, for their PTPase-1B inhibitor activity, in order to understand the essential structural requirement for binding with the receptor. Among several 2D QSAR models, one for a series was selected on the basis of high correlation coefficient, least standard deviation, & high value of significance for maximum no. of subject was considered. The interpreted data signify the essentiality of Benzofuran ring in the designing of the new PTPase-1B inhibitors and any substitution on the biphenyl and sulfonyl phenyl is going to decrease its activity. Key words: QSAR, PTPase-1B inhibitor, Sulfono biphenyl analog

Benzothiazole incorporated thiazolidin-4-ones and azetidin-2-ones derivatives: Synthesis and in vitro antimicrobial evaluation

In this study, a series of novel thiazolidin-4-ones (5a–g) and azetidin-2-ones (6a–g) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl)hydrazine carboxamide derivatives of the benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (−) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5–200 μg/mL in DMSO. It has been observed that azetidin-2-ones derivatives are found to be more active than thiazolidin-4-ones derivatives against all pathogenic bacterial and fungal strains

Synthesis, anti-inflammatory, analgesic, COX1/2-inhibitory activity, and molecular docking studies of hybrid pyrazole analogues

This article reports on the design, synthesis, and pharmacological activity of a new series of hybrid pyrazole analogues: 5a-5u. Among the series 5a-5u, the compounds 5u and 5s exhibited potent anti-inflammatory activity of 80.63% and 78.09% and inhibition of 80.87% and 76.56% compared with the standard drug ibuprofen, which showed 81.32% and 79.23% inhibition after 3 and 4 hours, respectively. On the basis of in vivo studies, 12 compounds were selected for assessment of their in vitro inhibitory action against COX1/2 and TNF alpha. The compounds 5u and 5s showed high COX2-inhibitory activity, with half-maximal inhibitory concentrations of 1.79 and 2.51 mu M and selectivity index values of 72.73 and 65.75, respectively, comparable to celecoxib (selectivity index = 78.06). These selected compounds were also tested for TNF alpha, cytotoxicity, and ulcerogenicity. Docking studies were also carried out to determine possible interactions of the potent compounds (\(5u and 5s), which also showed high docking scores of -12.907 and -12.24 compared to celecoxib, with a -9.924 docking score. These selective COX2 inhibitors were docked into the active site of COX2, and showed the same orientation and binding mode to that of celecoxib (\(selective COX2 inhibitor). Docking studies also showed that the SO2NH2 of 5u and 5s is inserted deep inside the selective pocket of the COX2-active site and formed a hydrogen-bond interaction with His90, Arg513, Phe518, Ser353, Gln192, and Ile517, which was further validated by superimposed docked pose with celecoxib