EUROPEAN JOURNAL OF
PHARMACEUTICAL AND MEDICAL RESEARCH

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 (Under Process) , 

 ISSN 2394-3211

Impact Factor: 4.897

 ICV - 79.57

Abstract

DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF NOVEL BENZIMIDAZOLE, PYRIDINE AND OXADIAZOLE DERIVATIVES AS ANTITUBERCULAR AGENTS AGAINST MYCOBACTERIAL TARGET ENZYME INH A

Ayyadurai Jerad Suresh*, Jesu Robert Dilton, Sundaraiah Suresh Kumar, Durga Rjendran , Parakkot Ramakrishnan Surya

ABSTRACT

Tuberculosis is the communicable disease. InhA the enoyl-ACP reductase in Mycobacterium tuberculosis is an attractive target. Benzimidazole, Oxadiazoles and Pyridine derivatives exhibit pharmacological activities such as antimicrobial, antiviral, anticancer, anti-inflammatory, analgesic, etc. Hence decided to develop novel Benzimidazole, Oxadiazoles and Pyridine derivatives as potent anti-tubercular agents against InhA enzyme (Enoyl acyl carrier protein reductase).Compounds were designed and docked against inh A enzyme by using online docking Software Argus lab 4.0.1®. The molecules screened for best docking score and protein interaction. The selected molecules were synthesized in good yield by simple reflux condensation. Synthesized compounds were purified and characterized and biologically evaluated for their Anti tubercular activity by Microplate Alamar Blue Assay (MABA techenique). The research work concludes that the synthesized anti-tubercular molecules effectively inhibit target enzyme Enoyl acyl carrier protein reductase (inh A). The benzimidazole derivatives were active at concentrations of 1.6mcg/ml “b” and 3.125mcg/ml “a”. The synthesized pyridine derivatives “c” and “d” showed good anti tubercular activity at 1.6mcg/ml. whereas oxadiazole derivatives “ e” and “f “were active at 1.6mcg/ml. Further structural modifications of the synthesized compounds will aid in the development of potential anti tubercular molecule. The cytotoxic evaluation of all the synthesized compounds was performed. The IC50 for Rifampicin is 113 μg/ml on vero cell line. Two compounds “a” and “b” shows decreased IC50 values of 37.63 and 111.2 μg/ml. Compounds “c” and “d “ showed increased IC50 values 389.7 and 319.3. Compounds “e” and “f” also showed increased IC50 values of 299.3 and 520.

Keywords: Mycobacterium tuberculosis; MABA; Oxadiazole; Benzimidazole; Rifampicin.


[Full Text Article]

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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 (Under Process)