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Pharma Chem Congress 2019

Journal of Pharmaceutical Chemistry & Chemical Science | Volume 3

June 12-13, 2019 | Bangkok, Thailand

OF EXCELLENCE

IN INTERNATIONAL

MEETINGS

YEARS

PHARMACEUTICAL

CHEMISTRY AND DRUG DISCOVERY

International Conference on

DESIGN, SYNTHESIS, PHARMACOLOGICAL SCREENING, MOLECULAR DOCKING AND

TOXICITY STUDIES ON 7-(2-(BENZO[D]THIAZOL-2-YLAMINO) ETHOXY)-4-METHYL-2H-

CHROMEN-2-ONE DERIVATIVES FOR ATYPICAL ANTIPSYCHOTIC ACTIVITY

Ashish A Gawai

Anuradha College of Pharmacy, India

ypical antipsychotics are used to treat a mental, baffling, severe disorder called Schizophrenia. The present

study focuses on design and synthesis of some novel derivatives. The novel series 7-(2-(benzo[d]thiazol-2-yl-

amino)ethoxy)-4-methyl-2H-chromen-2-one (4a-4k) was designed and synthesized by refluxing 2-amino ben-

zothiazole substituted derivatives (3a-3k) with 7-(2-chloroethoxy)-4-methyl-2H-chromen-2-one(2) in dry pyri-

dine. All the synthesized compounds were screened and evaluated for their dopamine D2 and serotonin 5HT2

antagonistic activity as a measure of typical antipsychotic property. Compounds 4b, 4c, 4e, 4g and 4i have

shown good preliminary pharmacological activity. Some of the better activity compounds were selected for

determination of acute toxicity (LD50) studies by OECD guidelines and also for effective dose (ED50) determi-

nation by probit log scale method. The therapeutic index (TI) of the selected compounds was determined for

selection of safer and better compounds. These synthesized derivatives were screened by molecular docking

method. The compounds were sketched using ChemBioDraw Ultra 12 and subjected for all possible confor-

mation of compounds interacting with receptors. Molecular docking was performed with the Glide 7.6, Mae-

stro 11.3 of Schrodinger 2017. PDB for Dopamine receptor 6CM4 and for serotonin 5TUD were obtained from

Brookhaven Protein database. The ligand-protein hydrogen bond network was obtained and total energy was

minimized by employing OPLS 2005 force field. The docking poses were ranked according to GlideScore. From

all above data results, compounds with electron withdrawing substitution like 4e and 4b has shown better

atypical antipsychotic profile.

Ashish A Gawai, J Pharm Chem Chem Sci 2019, Volume 3

Ashish A Gawai is an Associate Professor at Department of Pharmaceutical Chemistry at Anuradha College of Pharmacy, India. He

had completed his Master of Pharmacy in Pharmaceutical Chemistry from Bharti Vidyapeeth University, Poona College of Pharmacy,

India and PhD in Pharmaceutical Sciences at Department of Pharmaceutical Sciences, Dibrugarh University, India. He has 12 years

of teaching, 1.5 years of industrial experience and having more than 30 research papers and 50 research publications. He has also

crashed Maharashtra Public Service Commission and Union Public Service Commission examination for Pharmacy post. He has

attended to the invited conference at South Korea as well as several in India also. He has one published book entitled“A TEXTBOOK

OF MEDICINAL CHEMISTRY”in his credit also. He is a potential reviewer for prestigious research journals like

Bentham Science, Indian

Journal of Pharmaceutical Sciences

and many more. 24 students were completed Post-Graduation under his guidance. His research

area is drug synthesis, drug design (Molecular modeling and docking study), toxicity studies and quality assurance.

BIOGRAPHY