Novel Selective Anti-chlamydial Compounds and Use

Invention Summary:

Chlamydia trachomatis is the most common sexually transmitted pathogenic bacterium worldwide. If left untreated in women, this infection often leads to serious complications including infertility, pelvic inflammatory syndrome, ectopic pregnancy, and abortion. Several broad-spectrum antibiotics are used to treat diagnosed chlamydia. However, they also kill beneficial bacteria in the reproductive as well as the gastrointestinal tract, leading to dysbiosis. In addition, C. trachomatis may develop resistance to antibiotics. Thus arose the need to develop new selective antichlamydial compounds.

Rutgers researchers have developed five new selective antichlamydial ‘acylpyrazoline’ compounds with minimal inhibitory concentration. These compounds have about 2- to 5-fold higher potency in comparison to similar compounds and were designed to have better drug properties. Certain structural modifications show that these compounds are highly tolerated by bacteria colonized in humans. Studies show that all the five novel antichlamydial compounds are well tolerated by lactobacilli found in human vagina, E. coli in human gastrointestinal tract and other human pathogens including Klebsiella and Salmonella. These compounds inhibit chlamydia through a GrgA (General regulator of genes A) dependent mechanism..

Market Applications:

• Compounds have beneficial selective antichlamydial activity and are useful as new pharmaceutical compositions preferably administered through oral, or intravenous injection or infusion route.
• Sexually transmitted infections

Advantages:

• New selective antichlamydial leads for evaluations of its therapeutic applications
• Compounds can be modified to improve properties and potency
• Further development scope for the in-vivo test, preclinical and testing in humans

Intellectual Property & Development Status:

Patent pending. Available for licensing and/or research collaboration.