Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl)phenothiazine-[1,2,3]triazole hybrids

1H‐1,2,3‐Triazole‐tethered Isatin–coumarin Hybrids: Design, Synthesis and In Vitro Anti‐mycobacterial Evaluation

“…Obviously, the favorable properties of 1,2,3‐triazole motif like moderate dipole character, hydrogen bonding capability, and rigidity and stability under in vivo conditions are responsible for the enhanced biological activities . 1,2,3‐Triazole‐based anti‐TB agents may be regarded as a new class providing effective lead candidates, and numerous of 1,2,3‐triazole‐tethered derivatives have been synthesized for this purpose, and some of them showed promising potency . It is notable that 1,2,3‐triazole‐tethered derivative I‐A09 is in clinical trials currently, which may be approved to treat TB patients in the near future .…”

“…1,2,3‐Triazole‐based anti‐TB agents may be regarded as a new class providing effective lead candidates, and numerous of 1,2,3‐triazole‐tethered derivatives have been synthesized for this purpose, and some of them showed promising potency . It is notable that 1,2,3‐triazole‐tethered derivative I‐A09 is in clinical trials currently, which may be approved to treat TB patients in the near future .…”

Synthesis of novel 5-[(1,2,3-triazol-4-yl)methyl]-1-methyl-3H-pyridazino[4,5-b]indol-4-one derivatives by click reaction and exploration of their anticancer activity

“…Triazole is a core structural moiety found in some important drugs like tazobactam, cefatrizine, carboxyamidotriazole and rufinamide. The most significant and current studies have discovered that 1,2,3-triazole derivatives exhibit a broad spectrum of pharmacological activity such as antimicrobial (Kushwaha et al, 2014), anti-inflammatory (Shafi et al, 2012), anticonvulsant (Ulloora et al, 2013), antituberculosis (Addla et al, 2014;Patpi et al, 2012;Yempala et al, 2014) and, in particular, anticancer (Akselsen et al, 2012;Howell et al, 2009;Pagliai et al, 2006) activity. Owing to the drug-like properties of 1,2,3-triazole derivatives and also based on the preliminary structure-activity information (Güven and Jones, 1993), we have planned to incorporate 1,2,3-triazole unit into the pyridazino [4,5-b]indole structure with an expectation that the amalgamation of these two active pharmacophores in a single molecular framework would enhance the efficacy of the hybrid molecule.…”

Synthesis and bio-evaluation of phenothiazine derivatives as new anti-tuberculosis agents

“…However, comparison of SARs of anti-59 tuberculosis and anti-psychotic obtained from limited phenothia-60 zine derivatives suggests that anti-TB activity is mainly from the 61 scaffold of phenothiazine, since there is no obvious SAR trend can 62 be concluded from the side chain and substituents of related 63 phenothiazine derivatives [16,17]. It is revealed that the terminal 64 amine group in the 10-side chain as well as C-2 substitution 65 determines the optimal neuroleptic activity on central nervous 66 system [18].…”