Adamec Jan, Waisser Karel, Kunes Jirí, Kaustová Jarmila
Department of Inorganic and Organic Chemistry, Charles University, Faculty of Pharmacy, Hradec Králové, Czech Republic.
Arch Pharm (Weinheim). 2005 Aug;338(8):385-9. doi: 10.1002/ardp.200400967.
A set of 32 1-phenyl-5-benzylsulfanyltetrazoles substituted on the phenyl ring as well as on the benzyl moiety was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis. The activity against M. tuberculosis becomes higher with increasing electron-accepting properties of the substituents on the phenyl ring. On the other hand, any substitution on the benzylic moiety decreases the activity.
合成了一组在苯环以及苄基部分上被取代的32种1-苯基-5-苄基硫烷基四唑。对这些化合物针对结核分枝杆菌的体外抗分枝杆菌活性进行了评估。随着苯环上取代基吸电子性质的增加,其对结核分枝杆菌的活性变得更高。另一方面,苄基部分上的任何取代都会降低活性。