Journal of Pharmaceutical and Medicinal Chemistry

 Triazoles are five-member nitrogen containing heterocyclic compounds. Triazole derivatives have great importance in the field of chemical synthesis, agriculture and pharmaceutical industries due to their wide range of applications. Over the past few decades, researchers have focused their research on the synthesis of novel triazole derivatives. The 1,2,4- triazole heterocyclic ring is an integral part of various synthetic compounds with wide range of therapeutic and pharmacological potentials like antiinflammatory, antibacterial, anticancer, antifungal, antiviral, anticonvulsant, anti-tubercular, etc. Many marketed drugs are triazoles derivatives like antifungal drugs which include fluconazole, ravuconazole, itraconazole, and voriconazole. Due to the wide scope of pharmacological potentials of triazole derivatives, research community has shown great interest to discover triazoles having potent bioactivities with lesser side effects. This review summarizes the recent developments on the synthetic approaches, mechanism of action, and pharmacological properties of latest and novel triazole derivatives.

Keywords:Nitrogen Heterocycles; Azole; Synthesis; Antimicrobial. 

 Peptides are excellent biomolecular receptors and interactions between peptide and nanoparticle have played a major role in controlled drug delivery. Peptide-based nanoparticles (pep-NPs) are emerging as promising imaging and therapeutic agents against cancer due to their biocompatibility and tunability. This mini review dealt with development of new peptide-incorporated nanoparticles for imaging and drug delivery applications for detection and treatment of brain cancer.

Keywords: Peptides; Nanoparticles; Biodegradable; Imaging; Drug Delivery.

 Aims: The present study is to evaluate the in vitro Anti-diabetic activity of the various extracts of Adhatoda vasica Nees on glucose uptake by isolated rat hemi-diaphragm. Methods: The Adhatoda vasica Nees was extracted by using n-hexane, chloroform, ethyl acetate, methanol, and aqueous. The different extracts were then used to study on in vitro glucose uptake by isolated rat hemi-diaphragm. Results: The ethyl acetate and methanol extracts of the plant extracts showed significant glucose uptake when compared with control. The result strongly suggest that Adhatoda vasica nees will be alternative choice for treatment of diabetes mellitus. Conclusion: In the in vitro uptake assay in rat hemi diaphragm, Ethyl acetate and Methanol extract and the isolated compound showed significant of glucose uptake (41.3653±0.657188, and 27.26±0.88) respectively. The results suggested that the extracts and compound enhanced the uptake of glucose by isolated rat hemi diaphragm which was more effective than insulin.

Keywords: Adhatoda Vasica Nees; Glucose Uptake by Isolated Rat Hemi-Diaphragm; Diabetes Mellitus, Nilgiris.

 Pyrazline derivatives (3a-3i) were synthesized by using microwave irradiation i.e. by involving green chemistry. These compounds were taken for in vitro antimalarial activity using schizont maturation inhibition assay, using chloroquine as the standard against chloroquine sensitive, 3D7 strain of P. falciparum. Activity of the compounds was reported in terms of IC50 values. Compound 3h with dimethylamino substitution was found to be most active with IC50 value of 13.765 ìg/mL. From the results, it can be easily inferred that the bulky groups favoured antimalarial activity.

Keywords: Pyrazoline; Antimalarial; Microwave.

 In this paper, an attempt has been made to develop a quantitative structure–activity relationship 2DQSAR study on 30 analogues of 4-(anilino) pyrrole- 2-carboxamide, non steroidal non anilide molecules as androgen antagonist, to simulate a mathematical relation and to estimate the contributing descriptors. A statistically validated 2D QSAR model was obtained through k-nearest neighbour (kNN) simulated annealing with statistical data (q2 =0.792; pred r2 = 0.862) method using Vlife molecular design suits (MDS) 4.3. Positive and negative correlation of the various descriptors have been discussed.

Keywords: Androgen Antagonists; Bicalutamide; Flutamide; Non Steroidal; Prostate Cancer; 2D-QSAR.