The stability studies is one of the very important evaluation parameter of pharmaceutical products. Stability assessment and shelf-life prediction is usually a major focus of a pharmaceutical scientist’s attention in the development of all dosage forms. It is important in the development of small molecule drug products as well, particularly given the importance of the physical state of the drug in determining stability characteristics. Stability testing is utilized for formulated product to prediction of shelf life, determine proper storage conditions and suggest labeling instructions.
In this study, synthesis of dihydro-5-substituted-2-thioxopyrimidine derivatives has been described. The route of preparation involved the use of thiobarbituric acid as starting material and treated with substituted aldehyde compounds (aromatic and aliphatic) to give the required derivatives. A total of six derivatives were synthesized and the compounds were purified by chromatographic methods and identified by spectroscopic methods; FTIR, H1 NMR and also by measuring its melting point. The synthesized compounds were tested for antibacterial activity against two bacterial strains, of them one is gram positive strain Staphylococcus aureus and one gram negative strain Bacillus subtilis. The compounds were also evaluated for antifungal activity against two fungal strains Rhizopus andAsperigillus. The phenolic compounds viz., benzyl (3), 2-hydroxy (4), 4-dimethylamino (5), 4-dimethylaminocinnamyl (6) derivatives were found to be active against both the fungal and bacterial strains. The non-phenolic compounds viz., formyl (1), glutryl (2) derivatives exhibited significant activity against the gram negative bacteria Bacillus subtilis revealing that substitution by aromatic nuclei than aliphatic nuclei enhances the antimicrobial activity.
K. Padmini*, M. Lohita, S. Sumakala, M. Vishnupriya, Y. Gowtham Kumar, E. M. Ramyasudha.
Ocimum sanctum, is locally called as “Tulsi” belongs to the family Lamiaceae. The present study was carried out to identify the phytocomponents present in the methanolic extract of the leaves of Ocimum sanctumby GC-MS analysis. From the GC-MS results three compounds were identified as major constituents, they are Benzene, 1, 2-dimethoxy-4-(2-propenyl)-, Isocaryophyllene and Eugenol.
S. Balasubramanian*, D. Ganesh, P. Shridhar Reddy, V. V. S. Surya Narayana.
The current aim of our research work is to prepare methotrexate azo adduct with alanine for colon targeting. We synthesized alanine methotrexate azo adduct and examine the effect of enzyme azo reductase on the release characteristics of alanine and methotrexate in the gastrointestinal contents of rats. By using this approach two drugs can be targetted at the same time in the colon so as to treat the various diseases of colon such as colitis and colorectal cancer.The azo adduct did not release drug in acidic environment of stomach, but when drug reaches to colon the enzyme azo reductase acts on azo bond and releases the methotrexate and alanine simultaneously. By using this approach dual drugs can be released at same time. The azo adduct was evaluated for its color, solubility, Rf value, melting point, IR, 1HNMR and Mass spectral analysis. It was further subjected for evaluating its colon targeting property by in-vitromethod using rat fecal matter. The cytototoxic and acute toxicity studies of the compound were also performed which reveals that the alanine methotrexate azo adduct is safe for use to colon for the treatment of colorectal cancer.
Rajeev Kumar Sharma*, N. V. Satheesh Madhav, A. K. Sharma.
A new series of 2-hydrazino-quinazolinone (III) and 3-amino-triazolo-quinazolinones (VIIa-g) were prepared upon hydrazinolysis of 2-mercapto-quinazolinone intermediates (II,VIa-g) respectively. These compounds were condensed with aromatic aldehydes, for its confirmation; where compound (III) gives rise 2-(2-substitutedarylidenehydrazinyl)-3-(phenylamino) quinazolin-4(3H)-one (IVa-f) and compound (VIIa) gives rise 3-(4-chloro benzylideneamino)-2-phenyl-[1,2,4] triazolo[5,1-b]quinazolin-9(3H)-one (X). The biological testing of the target compounds (IVe, IVf, VIIa,VIIf) showed moderate anti-inflammatory activity with low ulcerogenic index compared with diclofenac sodium and celecoxib.
Samy M. Ibrahim*, M. Abo-Kul, Moustafa K.Soltan, Ahmed S. Helal.