alexa Abstract | STRUCTURE ACTIVITY RELATIONSHIP STUDIES OF CONJUGATED DIAMIDES OF VARIABLE ATOMIC ELECTRONEGATIVITY FOR SLEEPING TIME SYNERGISTIC ACTIVITY

International Journal of Drug Development and Research
Open Access

OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Abstract

The idea has been generated for CNS depression from the rational drug design from the structure of benzodiazepines and barbiturates in which there are closed chain urea moiety having two nitrogens in heterocyclic rings. Our objective was to synthesis such molecule in which this type of linkage must be in closed chain as well as in side chain. The synthesised molecule has three variables of three hetero atoms O/S/N and the CNS depression study has been done with respect to the standard sedative drug and found that the CNS depression activity persists in only urea moiety and there was no CNS depression activity in thiourea and guanidine linkage, but the sleeping time potentiation has been found in all the three compounds are as follows: Compound-A: X=O (urea derivative) > Compound-C: X=NH (guanidine derivative) > Compound-B: X=S (thiourea derivative) because electronegativity of oxygen for urea X:O=3.5 and of sulfur for thiourea X:S=2.4 and of nitrogen for guanidine X:NH=3.1. So the X=O shows the maximum electronegativity with two lone pair of electrons whereas X=S has also two lone pairs but X=NH has one lone pair of electrons, but in case of NH moiety the electronegativity of hetero element (N) is in between the hetero elements (O) for X:O and (S) for X:S. So, the affinity for GABA receptor binding capacity for urea is maximum to block the chloride channel.

To read the full article Peer-reviewed Article PDF image | Peer-reviewed Full Article image

Author(s): HARDIK ARVINDBHAI PATEL KIRAN MANUBHAI PATEL DHRUBO JYOTI SEN AND DILIPKUMARRAMJIBHAI CHAVDA

Keywords

Conjugated Diamides, electronegativity, CNS depression, GABA receptor, Synergistic Activity *Corresponding

 
Peer Reviewed Journals
 
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us