Objective: To synthesize, evaluate and performing the docking studies of novel formazan derivatives as enoyl-ACP reductase inhibitors.Materials: In the present investigation, a series of formazans (Ia-d) were synthesized by stirring aryl diazonium salts solution with Schiff's base at 0-5˚C for 2 h. The intermediate azomethine (Schiff base) itself was synthesized by condensation of para aminobenzoic acid with dimethylamino benzaldehyde in presence of a glacial acetic acid as a catalyst. The antimicrobial activity was done for these synthesized compounds by cup plate method. Moreover, the antimicrobial activity was further confirmed by its molecular docking approach study by using Molecular Operating Environment (MOE) 2009.10 software.Results: In the present study all the synthesized compounds (Ia-Id) showed the enhanced zone of inhibition against S. aureus, B. subtilis, E. coli and S. typhi (5±0.12 to 12±0.45) whereas, the antifungal activity against A. niger and C. albicans were showed the zone of inhibition in the range of 9±0.51 to 12±0.43 when compared to that of the standard drug.Further the docking study reveals that, only three of the formazan compounds under observation (Ia, Ib and Ic) have higher binding affinity with the receptors enzymes enoyl-ACP reductase, which is in the narrow range of binding energy for the protein PDB: 1C14 is-24.4598 to-23.9377 kcal/mol, which shows the further confirmation of these formazan compounds as better microbial inhibitor.Conclusion: Therefore our present report shows that formazans could be the potential drug candidate that inhibits the microbial activity by interacting and inhibiting the enoyl-ACP reductase enzyme which is confirmed by its both in vitro antimicrobial study and as well as from its docking study.

The marine bacterium was widely recognized as a natural manufacturer of novel bioactive secondary metabolites during the last decades, making the marine ecosystems a huge treasure of novel isolates. Marine coastal areas of the southern part of India have huge varieties of ecosystems that produce many marine microbes and organisms which are considered as a perennial source of many potential drug leads. This study focuses on the isolation of marine soil samples collected from the shores of the Bay of Bengal at Kanyakumari, Tuticorin, and Mandapam and followed by the characterization of the novel marine bacterium from that soil sample for the secondary metabolites production with   potential pharmacological  importance. The isolated  pure  culture  from  colonies  was  cultured  and  taxonomically  characterized  by  gram  staining  and  other  supported biochemical tests. Further, from the genetic analysis results through 16s rDNA sequencing and by comparing the nucleotide homology  and  phylogenetic  analysis  of  the  organisms  it  was  confirmed  as  “Paenibacillus  dendritiformis  and  Paenibacillus thiaminolyticus”.  Moreover, it was found that the bacterial isolates produced the inhibitory activity to other bacterial strains including both gram-positive and gram-negative bacteria at a concentration of 32 µl/ml. Thus, the bacterial isolates were found to produce secondary metabolites that comprise antimicrobial components and enzymes of commercial importance. Henceforth, this preliminary study looks promising and may lead to the discovery of potential antibiotics and other bioactive compounds.

The objective of this study is to develop a passive targeting of multilayered nanoparticles encountering multiple obstacles on the way to their target due to the mucosal barrier, nonspecific uptake of the drug. To prevent the nonspecific drug toxicity and combination chemotherapy for synergistic effect, multifunctional ferromagnetic properties were successfully fabricated by the layer-by-layer assembly (LBL) technique. The drug-loaded magnetic chitosan nanospheres were coated alternatively with sodium alginate and chitosan up to 3 layers incorporated with melphalan and methotrexate. The core-shell type  composites  consisting  of  magnetic  nanoparticles  decorated  with  biological  substances  are  interesting  for  various biomedical applications. The magnetic property investigation reveals that drug-loaded nanomaterials exhibit superparamagnetic behavior. The uniformly distributed magnetic nanoparticles were also observed in scanning electron microscopic images to characterize the synthesized product. The thin film consisting of chitosan nanospheres was coated alternatively with sodium alginate and magnetic nanoparticles had a conductivity of two formulations F1a and F2a were 35.2 emu/g and 43.4 emu/g respectively. The formulation was evaluated for its particle size, size distribution, zeta potential, and in-vitro drug release in the pH of 1.2 and 7.0 fitted in kinetic release studies. The developed magnetic nanoparticles showed promising results with better- delayed drug action and will be an enhanced therapeutic means in combating the infections of cancer therapy.

This abstract was not presented at the conference. Citation Format: Lin C-Y, Hazar-Rethinam M, Thangavelu P, Dray E, Duijf PH. Not presented [abstract]. In: Proceedings of the 2018 San Antonio Breast Cancer Symposium; 2018 Dec 4-8; San Antonio, TX. Philadelphia (PA): AACR; Cancer Res 2019;79(4 Suppl):Abstract nr P1-04-02.