EUROPEAN JOURNAL OF
PHARMACEUTICAL AND MEDICAL RESEARCH

( An ISO 9001:2015 Certified International Journal )

An International Peer Reviewed Journal for Pharmaceutical, Medical & Biological Sciences

An Official Publication of Society for Advance Healthcare Research (Reg. No. : 01/01/01/31674/16)

European Journal of Pharmaceutical and Medical Research (EJPMR) has indexed with various reputed international bodies like : Google Scholar , Indian Science Publications , InfoBase Index (In Process) , SOCOLAR, China , Research Bible, Fuchu, Tokyo. JAPAN , International Society for Research activity (ISRA) , Scientific Indexing Services (SIS) , Polish Scholarly Bibliography , Global Impact Factor (GIF) (Under Process) , Universal Impact Factor , International Scientific Indexing (ISI), UAE  , Index Copernicus , CAS (A Division of American Chemical Society) USA (Under Process) , Directory of Open Access Journal (DOAJ, Sweden, in process) , UDLedge Science Citation Index , CiteFactor , Directory Of Research Journal Indexing (DRJI) , Indian citation Index (ICI) , Journal Index (JI, Under Process) , Directory of abstract indexing for Journals (DAIJ) , Open Access Journals (Under Process) , Impact Factor Services For International Journals (IFSIJ) , Cosmos Impact Factor , Jour Informatics (Under Process) , Eurasian Scientific Journal Index (ESJI) , International Innovative Journal Impact Factor (IIJIF) , Science Library Index, Dubai, United Arab Emirates , Pubmed Database [NLM ID: 101669306] (Under Process) , IP Indexing (IP Value 2.40) , Web of Science Group (Under Process) , Directory of Research Journals Indexing , Scholar Article Journal Index (SAJI) , International Scientific Indexing ( ISI ) , Scope Database , Academia , 

 ISSN 2394-3211

Impact Factor: 7.065

 ICV - 79.57

Abstract

DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF ANTI-TUBERCULAR AGENTS TARGETING MTFAB D, MALONYL COA - ACYL CARRIER PROTEIN TRANSACYLASE

Parakkot Ramakrishnan Surya and Ayyadurai Jerad Suresh*

ABSTRACT

Mycobacterium tuberculosis MTB, or TB (tubercle bacillus), is a common, and in many cases lethal, infectious disease caused by various strains of mycobacteria, usually Mycobacterium tuberculosis. Over the past 200 years, tuberculosis has been responsible for the death of over 100 million people. Moreover due to the emergence and reemergence of multi-drug resistant tuberculosis (MDR-TB), extremely - drug resistant tuberculosis (XDR-TB), totally -drug resistant tuberculosis (TDR-TB) and also because of the co-infection of TB with HIV there is an urgent need for new Anti-TB agents. Today hetero cyclic compounds have attained wide attention in the discovery of new drug candidates because of their diverse biological activity. Heterocyclic ring system encompasses the core of the active moiety as pharmacophore. For a period of decade’s heterocyclic therapeutic agents plays a pivotal role in chemotherapy. In view of the above facts, this research work deals with the designing of chalcones containing heterocyclic moiety and synthesizing it for potential anti-tubercular activity. So molecules were designed and docked against MTB enzyme mtFab D, malonyl CoA - acyl carrier protein transacylase The screened molecules were synthesized by condensation method, purified by chromatographic techniques, characterized by various spectral analytical techniques and evaluated for in-vitro anti mycobacterial activity against tuberculosis H37RV strain by Microplate Alamar Blue Assay (MABA) method. The experimental results show that Compound Y possesses better anti-tubercular activity with an MIC below 1.6 mcg/mL while NA, and PW showed moderate anti tubercular activity with an MIC below 6.25mcg/Ml, and Compound X exhibited good anti tubercular activity with an MIC below 12..5mcg/Ml.

Keywords: Mycobacterium tuberculosis, Chalcones, Docking, MABA.


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