Anti-tubercular agents. Part 5: synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners.
In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and in vivo study of recently reported potent molecule 4 (MIC = 1 microg/mL) is also discussed.
Kamal
Ahmed
A
Division of Organic Chemistry-I, Indian Institute of Chemical Technology, Tarnaka, Hyderabad-500 607, India. ahmedkamal@iict.res.in
Shetti
Rajesh V C R N C
RV
Azeeza
Shaik
S
Ahmed
S Kaleem
SK
Swapna
P
P
Reddy
A Malla
AM
Khan
Inshad Ali
IA
Sharma
Sandeep
S
Abdullah
Sheikh Tasduq
ST
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D001419:Bacteria / Q000187:drug effects; D001581:Benzothiadiazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D005260:Female; D005658:Fungi / Q000187:drug effects; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D014376:Tuberculosis / Q000188:drug therapy*
D000995:Antitubercular Agents; D001581:Benzothiadiazines