Saturday, July 5, 2025 7/5/2025

Development of novel anti-Neisseria gonorrhoeae therapeutic agents

Award Number: R01AI153264
ORGANIZATION: NATIONAL INSTITUTE OF ALLERGY & INFECTIOUS DISEASES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 08/12/2022
PERIOD OF PERFORMANCE END DATE: 07/31/2026

Group Awards By:

View Award Description

Development of novel anti-Neisseria gonorrhoeae therapeutic agents - Project Abstract: Gonorrhea is a sexually transmitted disease caused by the bacterial pathogen Neisseria gonorrhoeae that colonizes urogenital, anal, and nasopharyngeal tissues. Locally in the United States the Centers for Disease Control and Prevention (CDC) reported a 67% increase of gonorrhea cases between 2013 – 2017 with >550,000 cases in 2017 alone. N. gonorrhoeae wreaks havoc on world health care systems causing pelvic inflammatory disease, infertility and ectopic pregnancies. The bacteria can also be transmitted from mother to child during birth and lead to blindness. If left untreated N. gonorrhoeae can cause gonococcemia resulting in skin infection, arthritis or endocarditis. Pathogenic gonorrhea strains are increasingly resistant to common front-line antibiotics. The WHO surveillance program reports resistance to most available antibiotics. Rampant resistance has caused the CDC and the World Health Organization each to classify N. gonorrhoeae as a superbug and a future with an untreatable gonococcal infection is a real possibility. Thus, there is significant unmet need to identify novel targets and molecules with therapeutic potential. Studies proposed in this application build upon discoveries that FDA- approved carbonic anhydrase inhibitors (CAIs), such as acetazolamide and ethoxzolamide, display potent antimicrobial activity, in an applicable clinical range, against N. gonorrhoeae. CAIs, and analogs we have designed, also have no antimicrobial effect on commensal bacteria reducing the potential for problematic dysbiosis caused by antibiotic treatment. We have shown that the molecules exhibit their antibiotic effect by inhibiting the carbonic anhydrase from N. gonorrhoeae and have validated N. gonorrhoeae carbonic anhydrase (NgCA) as a viable anti-gonococcal therapeutic target. Our team has improved the potency of the CAI-based inhibitors from 4 µg/mL to 0.5 µg/mL. This proposal will continue lead optimization of CAI-based analogs using structure-based design while incorporating modifications to improve permeability into the Gram-negative cell. Molecules will be assessed in in vitro antimicrobial assays and prioritized analogs will progress to in vitro pharmacokinetic (PK) and pharmacologic profiling. Finally, top performing analogs will be assessed for in vivo efficacy in various gonorrhea mouse models as well evaluated the in safety and pharmacokinetic assay to support future lead selection and investigational new drug enabling studies.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2024 ( Subtotal = $757,023 )
2024	2024	PURDUE UNIVERSITY	2550 NORTHWESTERN AVE # 1100	WEST LAFAYETTE	IN	47906	TIPPECANOE	USA	Allergy and Infectious Diseases Research	000	3	7/15/2024	NON-COMPETING CONTINUATION	$757,023
														Subtotal = $757,023

Issue Date FY: 2023 ( Subtotal = $764,773 )
2023	2023	PURDUE UNIVERSITY	2550 NORTHWESTERN AVE STE 1900	WEST LAFAYETTE	IN	47906	TIPPECANOE	USA	Allergy and Infectious Diseases Research	000	2	7/6/2023	NON-COMPETING CONTINUATION	$764,773
														Subtotal = $764,773

Issue Date FY: 2022 ( Subtotal = $780,073 )
2022	2022	PURDUE UNIVERSITY	2550 NORTHWESTERN AVE STE 1900	WEST LAFAYETTE	IN	47906	TIPPECANOE	USA	Allergy and Infectious Diseases Research	000	1	8/12/2022	NEW	$780,073
														Subtotal = $780,073

Grand Total All Awards = $2,301,869

Top

All Categories

About

Search

Reports

Data Submission

Award Information

Development of novel anti-Neisseria gonorrhoeae therapeutic agents

Award Number: R01AI153264

ORGANIZATION: NATIONAL INSTITUTE OF ALLERGY & INFECTIOUS DISEASES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 08/12/2022

PERIOD OF PERFORMANCE END DATE: 07/31/2026

Federal Websites

Department of Health & Human Services

HHS Operating Divisions

HHS Staff Divisions

Download A Document Viewer