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Title: Synthesis Study of Some Novel and#946; carboline Derivatives as Potential Agents Against HIV and Associated Infections
Researcher: ASHOK P
Guide(s): S. MURUGESAN
Keywords: quotNovel and#946;-carboline, Potential Agents, HIV, Associated Infectionsquot
University: Birla Institute of Technology and Science
Completed Date: 
Abstract: xiii newlineAbstract newlineAcquired Immuno Deficiency Syndrome (AIDS) is the advanced stage of the infection newlinecaused by Human Immunedeficiency Virus (HIV). According to UNAIDS-2014 report, it is newlineestimated that, 35.3 millions are currently living with HIV infection, 2.3 million new newlineinfections and 1.5 million deaths are reported in the year 2013. AIDS mortality rate, newlinedecreased continuously in the last decade, due to the availability of Highly Active Anti newlineRetroviral Therapy (HAART). HAART is the combination of three or more anti-HIV drugs, newlineused to reduce the emergence of resistance and side effects. HAART turned fatal AIDS newlineinto chronic manageable disease. Non-Nucleoside Reverse Transcriptase Inhibitors newline(NNRTIs) are the key components of HAART due to their high potency, selectivity and newlineless toxicity. Developed resistance to first generation NNRTIs and high mutation rate of newlinethe virus increases the need of novel anti-HIV agents. newlineIn the present, we have designed novel and#946;-carboline derivatives based on butterfly shape newlinepharmacophore as non-nucleoside inhibitors of HIV-1 reverse transcriptase. The newlinedesigned and#946;-carboline derivatives were synthesized from DL-tryptophan/tryptamine in newlineseries of reactions. Synthesized compounds were characterized by IR, 1H NMR, Mass and newlineelemental analysis. All the synthesized derivatives were evaluated for cytotoxicity newlineagainst healthy vero cell line using MTT assay method. In-vitro HIV-1 reverse newlinetranscriptase inhibition activity of these compounds was evaluated using colorimetric newlineassay method and first generation NNRTI efavirenz was used as reference drug. newlineMolecular modeling studies were performed to study the molecular interactions and newlineexact binding mode analysis in Non-nucleoside inhibitory binding pocket (NNIBP) using newlineSchr√∂dinger 2014. These anti-HIV and#946;-carboline derivatives were also evaluated for their newlineinhibitory potentialagainstAIDSopportunistic infections like leishmaniasis andtuberculosis. Standard drugs miltefosine (anti-leishmanial), isoniazid, rifampicin (antitubercular) newlinewere used as reference dru
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Appears in Departments:Pharmacy

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