22^nd International Conference on Medicinal Chemistry, Drug Discovery & Drug Delivery December 06-07, 2019 Singapore City, Singapore

Biography:

Dr.M.Madhavi has completed her PhD at the age of 35 years from Osmania  University. She has published more than 25 papers in reputed journals and has been awarded as Fellow of Academy of Emvironmental Biology, INDIA(FAEB) . Associate Fellow of Telangana Academy of SCIENCES  (AFTAS) and AP Academy of Sciences (APAS)        
 

Abstract:

Sitophilus oryzae  is one of the dangerous serious pests in stored grain and related products. The attack of stored products of agricultural and animal origin by more than 600 species of beetle pests causing quantitative and qualitative losses, as well as insect  contamination in food commodities, is an important quality control problem that is of great concern to food industries. It is reported that insect damage in stored grains and pulses may amount to 10-40% in countries where modern storage technologies have not been introduced . It is therefore  necessary to reduce such losses by controlling pests in stored products. The essential oil from Vitex negundo leaves repels Sitophilus zeamais Motsch. . Oil of the leaves   and acetone   extracts of black pepper seeds are toxic to Sitophilus oryzae (L.) and  Rhyzopertha dominica (F.)  It is considered a Primary pest, which can easily infest damaged or broken kernels and apart from grain, it is particularly destructive to Rice  and other processed grain products. During the last two decades phytochemicals from plant bioresources have been heralded as desirable alternative to synthetic chemical insecticides for pest management because they pose little threat to the environment or human health. In our earlier studies, we reported the effect of commercial glycoalkaloid, Vitex negundo  on Corcyra cephalonica larvae. The treatment prevented the normal development of the last instar larvae. Increase in dosage of Vitex negundo  resulted in interference in ecdysis, inhibition of pupation, formation of mosaics (larval-pupal, pupal-adult intermediates), deformed pupae and deformed adults. However, the molecular mechanism of the phytochemical effect on the larvae is yet to be studied. Lindsey C. Perkin corresponding and Brenda Oppert in recently reported the list of genes that are altered during developmental stages (PMID: 31198628). We planned to isolate the RNA from the different growth stages of the food pest and study their expression pattern after the treatment of Vitex negundo.

Key Words: Vitex negundo, Sitophilus oryzae,  Ecdysis, RNA, Gene Expression.

Biography:

Ziyuan Zhou has completed his PhD at the age of 28 years from University of Kentucky, USA and postdoctoral studies from Peking University, Shenzhen CHINA. He has published more than 24 papers in reputed journals.

Abstract:

Antimicrobial resistance (AMR) is gravely threatening modern health care system. The traditional antimicrobials themselves are the catalyst for AMR. Thus, novel antimicrobial strategies are desperately needed. The targeting of bacterial RecA represents an alternative approach to combat AMR, as RecA inhibitors could block RecA mediated SOS response, while not inhibit bacteria growth, presumably impose less selective pressure for AMR. A series of naphthalene polysulfonated compounds, represented by suramin, were reported to be RecA inhibitors. However, the specific interaction between these compounds and RecA is still unclear. We identified the binding site on RecA and predict the binding details of the naphthalene polysulfonated compounds with RecA by multiple theoretical approaches. Taken together, this work dedicates to correlate the inhibitor-RecA interactions and inhibitory activities at the molecular level, and to provide theoretical and experimental foundations for the screening of novel compounds as RecA targeting antibiotic adjuvants. We have elucidated a proposed molecular interaction mechanism for the previously observed, but molecularly uncharacterized naphthalene polysulfonated compounds as the bacterial RecA inhibitors. These computational and experimental results suggest this scaffold design is a promising strategy for the developing novel compounds with improved adjuvants against RecA proteins from a broad spectrum of bacterial pathogens. Conclusions of this work can be included in a drug discovery pipeline as a way to optimize drug leads and increase the successful rate in the future RecA targeting inhibitors discovery.

Biography:

László Kollár received his diploma in 1979 and the doctoral degree in 1983 at the University of Veszprém, Hungary. He is now the Head of the Institute of Chemistry at the University of Pécs, Hungary. The main efforts of his current research are focused on the synthetic application of transition metal complexes regarding the functionalization of steroids and N-heterocycles of pharmacological importance, as well as PARP inhibitors. He is the author of more than 300 papers published in international journals and co-author of 9 basic patents on 5-reductase inhibitors and agrochemicals.

Abstract:

The functionalization of the androstane, estrane and pregnane skeletons, as well as the stereoselective formation of the steroidal framework by homogeneous catalytic reactions proved to be highly attractive synthetic methods [1]. Among the functional groups of pharmacological importance, the carboxamido functionality, especially in the distinguished position-3 and 17, plays an important role due to its presence in steroids with 5-reductase inhibitor properties. [2-5]

In the present contribution we report on the efficient synthesis of host compounds (cavitand–steroid conjugates) with chiral inlet bearing steroidal moieties at the upper rim of the cavitand ‘basket’. The unexpectedly high selectivity regarding the formation of tetracarboxamide, as well as the characterization and potential pharmacological applications of these compounds in ‘host-guest’ interactions will be discussed.

Biography:

Ruby Kharwar is presently working as Research fellow at ARIBAS in the department of Pharmaceutical chemistry. She has completed her masters in Pharmaceutical Chemistry and worked on six months project entitled “Development of transdermal patches by varying plasticizers”.  After that she served as a technical assistant at ARIBAS for more than a year. Presently she is doing her research on synthesis, characterization and biological evaluation of sulphonamide substituted derivatives of 8-Hydroxyquinoline and its metal chelates.

Abstract:

With vast potential biological activities and metal chelating ability, the utilization of 8-Hydroxyquinoline (8HQ) as a pharmacophore for preparing drugs and coordination compounds has been increased exponentially. The work endeavours synthesis of new sulphonamide substituted derivative of 8HQ which is N-(8-hydroxyquinolin-5-yl)-2,4,6-trimethylbenzenesulfonamide (8HQTMBS) and its metal complexes with metal salts such as Cu(II), Ni(II), Zn(II), Co(II), Fe(II) and Mn(II) have been synthesized. The ligand 8HQTMBS is further characterized by FT-IR, MASS, ¹H-NMR, ¹³C-NMR. Study of physiochemical properties, elemental analysis, FT-IR, and thermal analysis like TGA and DSC were used to confirm the structure of synthesized metal chelates. The ligand and central metals have been coordinated through O and N electron donar sites which are evident from infrared spectra. The antibacterial activity was carried out by agar plate method, the result suggested that the metal chelates increases the efficacy of parent moiety. Also, interaction of Ligand (8HQTMBS) and its metal chelates with calf thymus DNA (CT-DNA) were investigated by UV-Visible spectroscopy, viscosity measurement and gel electrophoresis which showed that the binding of complexes with DNA occurs through intercalation mode. Moreover, molecular docking study was performed using Autodock 4.2 tools to emphasize the experimental behaviour and to investigate antibacterial activities of 8HQTMBS and its metal chelates on proteins of microorganisms such as Bacillus subtilis (5h67), Escherichia coli (3t88), Proteus vulgaris (5i39) and Staphylococcus aureus (3ty7). Further, molecular docking of 8HQTMBS and its metal chelates with double stranded BDNA (PDB ID: 1BNA) confirms the intercalation mode of binding.