Journal of Pharmaceutical and Medicinal Chemistry

 Pharmaceutical industries are now focused towards research and development of new drug delivery technologies to fulfill the needs of the modern world. Innovations with lipid based drug delivery have become a vital component of development in dosage form. Many formulations and innovations in controlled and targeted drug delivery have been attempted for the release of drug at the right place in a safe and reproducible manner. Liposomal drug delivery systems has become successful and has led to many development in liposome based formulations like niosomes, ethosomes, transferosomes, bilosomes, etc. Bilosomes are colloidal novel drug delivery systems similar to other liposomal delivery systems but prepared by incorporating bile salts into the lipid bilayer membrane. This present article focuses on the bilosomal drug delivery systems.

Heterocyclic compounds containing sulphur, nitrogen and oxygen atoms in the core structure shows number of pharmacological and biological activities. So, various heterocyclic systems were synthesized, studied in the past decade and found to possess remarkable pharmacological activities and are employed in the treatment of commonly occurring diseases. This has been back bone for the chemists to impart interest for the synthesizing some novel derivatives. In the last few decades, the chemistry of five membered heterocyclic rings has received considerable attention owing to their synthetic and biological importance. Among that one such class of compound is thiazolidinediones. The synthesis of novel thiazolidinedione derivatives and investigation of their chemical and biological behaviour have gained much more importance in recent decades. The thiazolidinediones chemistry has been developed extensively and is still developing. Presently there are a few number of drugs used clinically which comprises thiazolidinedione moiety in association with various heterocyclic rings. The present review deals with the structural features, synthesis, mechanism of action associated with thiazolidinedione derivatives and special emphasis is given on recently reported thiazolidinedione analogues possessing various biological activities.

Keywords: Solid lipid nanoparticles, Nanostructured lipid carriers, lipid matrix, drug carriers. 

Keywords: Orodispersible, Ondansetron HCL, Crospovidone, Croscarmellose sodium,  

Keywords: Hydrazones, Anticonvulsant, Epilepsy. 

 The synthesis of a peptide containing an oxime bridge performed on solid-phase is described. The strategy used takes advantage of selective acidolytic removal of Boc and acetal protecting while minimally cleaving a PAL anchor, as well as compatibility of PEG-PS resin supports with aqueous conditions for oxime formation.

Keywords: cyclic peptide, oxime bond, on-resin, intramolecular bridge. 

Objective:  The aim of present work is to synthesize a novel series of (Isatin) 1H-indole-2, 3-diones derivatives and evaluate its antioxidant activity. The structure of these compounds was established on basis of NMR data and IR data. Introduction: Isatin (1H-indole-2, 3-dione) is a synthetically versatile substrate, where it can be used for the synthesis of large variety of heterocyclic compounds, such as Indoles and quinolones. Isatin modify can considered as an important pharmacophore in the field of medicinal chemistry which can be used for conjugating it with other bioactive molecules such as antibacterial, antifungals, anticonvulsants and antiviral agents due to its potent pharmacological activity. Looking at the pharmacological potential of isatin we thought it worthwhile to synthesize and characterize some Schiff’s and Mannich bases of isatin.   Isatin and its derivatives undergo nucleophilic attack at position C-3. The chemo selectivity of these reactions depends on the nature of the substituents attached to the isatin nucleus, and especially of those bonded to the nitrogen atom, as well upon solvent and temperature employed. Chemistry:   Isonitrosoacetanilide was prepared from aniline by treating aniline with chloral hydrate and hydroxylamine hydrochloride and from Isonitrosoacetanilide, indole-2, 3-dione was prepared in presence of conc. Sulphuric acid. Then various derivatives of indole-2, 3-diones were prepared by treating indole-2, 3-dione with various amines in presence of glacial acetic acid and formaldehyde to yield Schiff’s and Mannich bases. The structure of synthesized compounds were confirmed by chromatographic and spectral analysis Antioxidant activity: The synthesized compounds were then evaluated for their Free radical scavenging activity by the DPPH assay method at 10, 20, 30, 40, 50 µg/ml concentrations of ligands & standard. Ascorbic acid was used as the standard. The data obtained were analyzed and results were expressed as mean absorbance ± standard error mean for each compound. The results of the pharmacological screening indicated that Compound ISS-2 shows more significant Free radical scavenging activity in comparison to other ligands and compounds ISS-1, ISS-5 shows moderate antioxidant activity and compounds ISS-4 and ISS-3 shows less antioxidant activity.  Conclusion: The compounds synthesized were then characterized using various spectroscopic techniques i.e.IR, 1H-NMR. The spectroscopic studies showed spectral data confirmed the formation of new compounds. The synthesized compound possesses significant antioxidant activity.

Keywords: Isatin, antioxidant, Manichh and Schiff base, DDPH assay, ascorbic acid. 

Context: Although Colocasia esculenta Linn. (Araceae) commonly known as patarveliya in Guajarati possesses several medicinal properties, a little is known about its antioxidant activity. Objective: The current research was designed to examine the antioxidative potential of hydroalcoholic extract of leaves of Colocasia esculenta (HECE) for the first time using several in-vitro analytical methods. Materials and methods: The antioxidant activity of HECE was evaluated using reducing power ability, nitric oxide scavenging assay and the estimation of total phenolic contents. Results and Discussion: The HECE gave an IC50 value of 45.75±0.38 µg/ml. The reducing power was investigated by Fe3+-Fe2+ transformation in the presence of extract tested using ascorbic acid as standard. The HECE showed increase in reducing ability with increase in concentration at 700nm. The total antioxidant capacity by nitric oxide scavenging method is expressed as curcumin equivalents. The content of total phenolics in HECE was found to be 49.21 ìg gallic acid equivalent/mg. Conclusions: Based on the above results, the higher the phenolic content, the higher the antioxidant capacity was very well