Building Blocks

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

3-Chloro-N-methyl-2-nitroaniline is an antibiotic that belongs to the group of quinolone antibiotics. It has a broad spectrum against Gram-positive and Gram-negative bacteria, including methicillin resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa. 3-Chloro-N-methyl-2-nitroaniline binds to bacterial DNA gyrase and topoisomerase IV, as well as human DNA gyrase and topoisomerase II, inhibiting their activity. This leads to cell death by interfering with the production of proteins vital for cell division. The optimal parameters for this drug have been found using isothermal titration calorimetry on the enzyme gyrase in the presence of different concentrations of 3CMA. Pharmacological targets for this drug include DNA gyrase and topoisomerase IV.

Versatile small molecule scaffold

2-Chloro-5-nitronicotinamide is a synthetic drug that has been used as an antileprosy, antimycobacterial, and chemotherapeutic agent. It is a dithiocarbamate that inhibits the synthesis of mycolic acids in mycobacteria. The interaction between 2-chloro-5-nitronicotinamide and mycolic acid is synergistic. This drug can be used to investigate the role of mycolic acids in the pathogenesis of leprosy and tuberculosis. 2-Chloro-5-nitronicotinamide is also active against footpad infections caused by erythromycin resistant strains of Mycobacterium smegmatis. It has been shown to be effective in mice when applied topically as an antimicrobial agent or when injected intravenously as an antimicrobial chemotherapy agent.

6,7-Dimethoxy-2-(piperazin-1-yl)quinazolin-4-amine dihydrochloride (DMPQ) is a piperazine derivative that is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5). This drug has been shown to be useful in the treatment of the symptoms of benign prostatic hyperplasia. DMPQ inhibits the hydrolysis of cyclic adenosine monophosphate (cAMP), which leads to an increase in intracellular levels of cAMP. This drug also exhibits antihypertensive effects, as it inhibits the activity of nitric oxide synthase.

2-(5-Oxooxolan-2-yl)acetic acid is a fluorophore that emits light upon excitation. It binds to the kappa opioid receptor and has been shown to inhibit leukocyte chemotaxis in vivo. 2-(5-Oxooxolan-2-yl)acetic acid has also been shown to function as an acetylcholinesterase inhibitor, which is important for maintaining the stability of the neurotransmitter dopamine. The fluorescence intensity of 2-(5-Oxooxolan-2-yl)acetic acid increases when it is reacted with amines or other functional groups.

Versatile small molecule scaffold