Zuma, Nonkululeko H.; Smit, Frans J.; Seldon, Ronnett; Aucamp, Janine; Jordaan, Audrey; Warner, Digby F.; N’Da, David D. published the article 《Single-step synthesis and in vitro anti-mycobacterial activity of novel nitrofurantoin analogues》. Keywords: nitrofurantoin preparation antimycobacterial antitumor human drug toxicity; Analogues; Drug resistance; Nitrofurans; Nitrofurantoin; Nitroreductase; Tuberculosis.They researched the compound: 1-Bromoundecane( cas:693-67-4 ).Quality Control of 1-Bromoundecane. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:693-67-4) here.
To improve TB efficacy of nitrofurantoin (NFT), a series of NFT analogs I [R = Me, Et, Bn, etc.] was synthesized and evaluated in vitro for anti-mycobacterial activity against the laboratory strain, Mtb H37Rv and for potential cytotoxicity using human embryonic kidney (HEK-293) and Chinese hamster ovarian (CHO) cells. The NFT analogs showed good safety profiles, enhanced anti-mycobacterial potency, improved lipophilicity, as well as reduced protein binding affinity. Analog I [R = n-Bu] which contains an eight carbon aliphatic chain was the most active, equipotent to isoniazid (INH), a major front-line agent, with MIC90 = 0.5μM, 30-fold more potency than the parent drug, nitrofurantoin (MIC90 = 15μM), and 100-fold more selective towards mycobacteria. Therefore, compound I [R = n-Bu] was identified as a validated hit for further investigation in the urgent search for new, safe and affordable TB drugs.
Compounds in my other articles are similar to this one(1-Bromoundecane)Quality Control of 1-Bromoundecane, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.
Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem