Letters in Drug Design & Discovery - Volume 15, Issue 5, 2018

Background: A new series of substituted 1,2,4-triazoles derivative were synthesized and characterized by IR, 1HNMR, 13CNMR spectra, mass spectroscopy and elemental analysis. Methods: The isonicotinic acid hydrazide (INH) was used as starting material. These synthesized compounds were screened for antitubercular activities by Luciferase Reporter Phase (LRP) assay against drug sensitive reference strain (H37RV) an Read More

Background: Cancer is a major health problem worldwide, the relative mortality rate caused by cancer is still very high even in developed countries. Although the remarkable success has been achieved: some small molecule anticancer agents have been approved by the U.S. Food and Drug Administration (FDA) in clinics and some are currently in clinical trials, cancer chemotherapy is still highly inadequate. It is essential to fin Read More

Background: A novel series of 4-[(4,5-diphenyl-2-substituted phenyl/heteryl)-1H-imidazole- 1-yl]pyrimidine-2(1H)-one derivatives 5 (a-o) were synthesized using Green protocol. Methods: The structures of the synthesized derivatives were established by IR, NMR, Mass spectra and elemental analysis. The synthesized coupled derivatives 5 (a-o) were evaluated for their in vitro antifungal activity against six fungi strains. Compo Read More

Background: Head and neck squamous cell carcinoma (HNSCC) is one of the most common malignancies in humans and the average 5-year survival rate is one of the lowest among aggressive cancers. Protein kinase C zeta (PKCZ) is highly expressed in head and neck tumors, and the inhibition of PKCZ reduces MAPK activation in five of seven head and neck tumors cell lines. Considering the world-wide HNSCC problem Read More

Background: Diabetes mellitus, a chronic disease, has grown wide concern in today's world. Majority of the world's population is affected by this disease. All the existing drugs have some side effects such as weight gain, risk of liver disease, skin problems etc. This situation demands the need of more and more potent drugs. Demand for new and faster acting drugs is great and as such it necessitated search for new drug targe Read More

Background: High rate of bacterial infection potentiates scientists to search natural products for new antimicrobial agents. Methods: This research determines the antimicrobial activity of tannins isolated from Pimenta dioica leaves on Gram-positive and Gram-negative infectious organisms using agar diffusion method. Results: All tested compounds were effective against Staphylococcus epidermidis, particularly pedunculagin Read More

Background: Pyrazoline scaffold is a key structural motif found among pharmaceutically active molecules including synthetic and natural products. The molecules with pyrazoline backbone from natural as well as synthetic origin are investigated worldwide for the development of efficient and potent drugs. Over the past few years, pyrazoline derivatives are used for the treatment of diverse dreadful diseases including malaria, Read More