Recent Drug-Repurposing-Driven Advances in the Discovery of Novel Antibiotics.

Drug repurposing is a safe and successful pathway to speed up the novel drug discovery and development processes compared with de novo drug discovery approaches. Drug repurposing uses FDA-approved drugs and drugs that failed in clinical trials, which have detailed information on potential toxicity, formulation, and pharmacology. Technical advancements in the informatics, genomics, and biological sciences account for the major success of drug repurposing in identifying secondary indications of existing drugs.

Novel hybrid biosorbents of agar: Swelling behaviour, heavy metal ions and dye removal efficacies.

Agar based hybrid biosorbents were synthesized by free radical copolymerization of acrylamide, NN'-methylenebisacrylamide (NN'MBAAm) on the agar backbone in presence of free radical initiator (ceric ammonium nitrate (CAN)) via oxidation, grafting and crosslinking reactions. The resultant hybrid materials have been characterized by FTIR spectroscopy, elemental analysis, thermal analysis (TGA/DTA), X-ray diffraction (XRD) and scanning electron microscopy (SEM) taking agar as a reference. The swelling responses of hybrid materials have been extensively studied with various pH, time, temperature and ionic strength [NaCl] of the solution.

Antiproliferative Activity of Crocin Involves Targeting of Microtubules in Breast Cancer Cells.

Crocin, a component of saffron spice, is known to have an anticancer activity. However, the targets of crocin are not known. In this study, crocin was found to inhibit the proliferation of HCC70, HCC1806, HeLa and CCD1059sk cells by targeting microtubules.

Synthesis and anti-HCV determinant motif identification in pyranone carboxamide scaffold.

Hepatitis C Virus exhibits high genetic diversity. The current treatment for genotype-1 with ∼80% sustained virologic responses is a combination of pegylated interferon, ribavirin and boceprevir/telaprevir/simeprevir which is associated with several side effects and need close monitoring. Therefore, novel therapies are invited for safer and more efficient treatment.

Synthesis and Anti-HCV Activity of 4-Hydroxyamino α-Pyranone Carboxamide Analogues.

High genetic variability in hepatitis C virus (HCV), emergence of drug resistant viruses and side effects demand the requirement for development of new scaffolds to show an alternate mechanism. Herein, we report discovery of new scaffold I based on 4-hydroxyamino α-pyranone carboxamide as promising anti-HCV agents. A comprehensive structure-activity relationship (SAR) was explored with several newly synthesized compounds.

Synthesis and applications of polyacrylamide grafted agar as a matrix for controlled drug release of 5-ASA.

Agar has been modified by microwave assisted grafting with acrylamide monomer, resulting in poly acrylamide grafted agar (Ag-g-PAM). The synthesized grades of Ag-g-PAM were characterized by standard physico-chemical characterization techniques (FTIR spectroscopy, elemental analysis, scanning electron microscopy (SEM)) to ascertain the intended grafting. The synthesized graft copolymer (Ag-g-PAM) has been investigated (in vitro) for controlled and colon targeted release of 5-amino salicylic acid (5-ASA).

Skeletal hybridization and PfRIO-2 kinase modeling for synthesis of α-pyrone analogs as anti-malarial agent.

The pharmacophoric hybridization and computational design approach were applied to generate a novel series of α-pyrone analogs as plausible anti-malarial lead candidate. A putative active site in flexible loop close to wing-helix domain of PfRIO2 kinase was explored computationally to understand the molecular basis of ligand binding. All the synthesized molecules (3a-g) exhibited in vitro antimalarial activity.