Synthesis and Testing of New MTN Inhibitors as Novel Antibiotics

Romaric Mukuna; Hank Dossett; Necia Hunter; John H. Thurston; Ken Cornell

Synthesis and Testing of New MTN Inhibitors as Novel Antibiotics

Romaric Mukuna
, Hank Dossett
, Necia Hunter
, John H. Thurston
, Ken Cornell

Chemistry Department

Research output: Contribution to conference › Poster

Abstract

In the last decade, a new epidemic of antibiotic resistant microbes has swept the globe. With few new FDA approved antibiotics in the past 20 years, there is a need for new and novel antibiotics to treat drug resistant microbes. Methylthioadenosine nucleosidase (MTN) an important metabolic enzyme for microbes that is absent from humans. Drugs that inhibit MTN, while not inhibiting mammalian Methylthioadenosine phosphorylase (MTAP), could be valuable new antibiotics. In this study, potential inhibitors identified by in silico screening were tested for anti-MTN activity. Several urea-base compounds with tighter binding to MTN than MTAP were found. In addition, a urea-based analog was synthesized and fully characterized showing correct structure and activity against E. coli MTN.

Original language	American English
State	Published - 1 Jul 2015
Event	Idaho Conference on Undergraduate Research 2015 - Boise State University, Boise, United States Duration: 1 Jul 2015 → … https://scholarworks.boisestate.edu/icur/2015/

Conference

Conference	Idaho Conference on Undergraduate Research 2015
Abbreviated title	ICUR 2015
Country/Territory	United States
City	Boise
Period	1/07/15 → …
Internet address	https://scholarworks.boisestate.edu/icur/2015/

EGS Disciplines

Chemicals and Drugs
Enzymes and Coenzymes
Medicinal-Pharmaceutical Chemistry

Cite this

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title = "Synthesis and Testing of New MTN Inhibitors as Novel Antibiotics",

abstract = " In the last decade, a new epidemic of antibiotic resistant microbes has swept the globe. With few new FDA approved antibiotics in the past 20 years, there is a need for new and novel antibiotics to treat drug resistant microbes. Methylthioadenosine nucleosidase (MTN) an important metabolic enzyme for microbes that is absent from humans. Drugs that inhibit MTN, while not inhibiting mammalian Methylthioadenosine phosphorylase (MTAP), could be valuable new antibiotics. In this study, potential inhibitors identified by in silico screening were tested for anti-MTN activity. Several urea-base compounds with tighter binding to MTN than MTAP were found. In addition, a urea-based analog was synthesized and fully characterized showing correct structure and activity against E. coli MTN.",

author = "Romaric Mukuna and Hank Dossett and Necia Hunter and Thurston, \{John H.\} and Ken Cornell",

year = "2015",

month = jul,

day = "1",

language = "American English",

note = "Idaho Conference on Undergraduate Research 2015, ICUR 2015 ; Conference date: 01-07-2015",

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TY - CONF

T1 - Synthesis and Testing of New MTN Inhibitors as Novel Antibiotics

AU - Mukuna, Romaric

AU - Dossett, Hank

AU - Hunter, Necia

AU - Thurston, John H.

AU - Cornell, Ken

PY - 2015/7/1

Y1 - 2015/7/1

N2 - In the last decade, a new epidemic of antibiotic resistant microbes has swept the globe. With few new FDA approved antibiotics in the past 20 years, there is a need for new and novel antibiotics to treat drug resistant microbes. Methylthioadenosine nucleosidase (MTN) an important metabolic enzyme for microbes that is absent from humans. Drugs that inhibit MTN, while not inhibiting mammalian Methylthioadenosine phosphorylase (MTAP), could be valuable new antibiotics. In this study, potential inhibitors identified by in silico screening were tested for anti-MTN activity. Several urea-base compounds with tighter binding to MTN than MTAP were found. In addition, a urea-based analog was synthesized and fully characterized showing correct structure and activity against E. coli MTN.

AB - In the last decade, a new epidemic of antibiotic resistant microbes has swept the globe. With few new FDA approved antibiotics in the past 20 years, there is a need for new and novel antibiotics to treat drug resistant microbes. Methylthioadenosine nucleosidase (MTN) an important metabolic enzyme for microbes that is absent from humans. Drugs that inhibit MTN, while not inhibiting mammalian Methylthioadenosine phosphorylase (MTAP), could be valuable new antibiotics. In this study, potential inhibitors identified by in silico screening were tested for anti-MTN activity. Several urea-base compounds with tighter binding to MTN than MTAP were found. In addition, a urea-based analog was synthesized and fully characterized showing correct structure and activity against E. coli MTN.

UR - https://scholarworks.boisestate.edu/icur/2015/Poster_Session/97/

M3 - Poster

T2 - Idaho Conference on Undergraduate Research 2015

Y2 - 1 July 2015

ER -

Synthesis and Testing of New MTN Inhibitors as Novel Antibiotics

Abstract

Conference

EGS Disciplines

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