JOFOC 2001907.pdf

Justification for Other than Full and Open Competition at or Below the Simplified Acquisition Threshold

Project Title: Glycomimetic library screening

I . Identification of the agency and contracting activity

DHHS, NIH, NIAID, LCIM, TRS

Address of the requesting lab/office: Tuberculosis Research Section, LCIM/NIAID/NIH, 9000 Rockville pike, Bethesda, MD 20892.

II. Description of the project, and supplies or services required to meet the agency’s needs (including the estimated value) A. Type of action. Check the appropriate box:

☒ New requirement B. Project Background

The Tuberculosis Research Section (TBS) of the Laboratory of Clinical Immunology and Microbiology (LCIM) Focuses on the development of novel chemotherapeutics and immunotherapeutics for the treatment of tuberculosis and related diseases; because much of the inherent drug resistance of Mycobacterium tuberculosis is due to their highly impermeable cell wall, important targets for new drug development lie in the enzymatic pathways responsible for cell wall biosynthesis and assembly and conducts studies to understand the pathways responsible for the synthesis and modification of mycolic acids, the major component of mycobacterial cell walls, using tools from both biochemistry and molecular genetics to foster a deeper understanding of the interactions between the various molecular components of the cell wall and create genetically engineered strains which are defective in cell wall synthesis and have utility as new improved vaccine strains; targets chemotherapeutic enzymes involved in the modification of such molecules through the construction of directed combinatorial libraries of known inhibitors of similar chemical reactions and by construction of libraries of analogs of known antituberculars.

Glycomimetic are compounds that have structures similar to carbohydrates and have modified biological activities.

Our laboratory is seeking to acquire a diverse molecule library of this class of compounds to screen against M.

tuberculosis to look for novel compounds with anti-tuberculosis activity.

The ordered compounds need to be provided at 0.2 ul and 5mM. We need a large diversity of library compounds (>2000). Fluorescent M. tuberculosis will be incubated with these compounds and fluorescence will be read off after a few days of incubation. We will determine the minimal inhibitory concentration with the plate reader’s data and determine if there are compounds in the library with anti-tuberculosis activity. The compounds need to be made assay ready 384-well plates.

III. Identification of the statutory authority permitting other than full and open competition (SELECT ONE) ☒ 41 USC 253(c) (1) a n d F A R P a r t 6 . 3 0 2 - 1 : Only one responsible source

IV. Demonstration that the proposed contractor(s) unique qualifications or the nature of the acquisition requires use of the authority cited.

The ordered compounds need to be provided at 0.2 ul and 5mM. We need a large diversity of library compounds (>2000).

Fluorescent M. tuberculosis will be incubated with these compounds and fluorescence will be read off after a few days of incubation. We will determine the minimal inhibitory concentration with the plate reader’s data and determine if there are compounds in the library with anti-tuberculosis activity. The compounds need to be made assay ready 384-well plates.

The glycomimetic compound library from Enamine is the only one that could fulfill the requirements for the number of compounds, diversity, and flexibility to adapt to our established screening protocol in our laboratory.

Vendor Information:

Enamine LTD 3940 Glendale Milford Rd Cincinnati, OH, 45241-3131