38002-61-8Relevant articles and documents
Inhibitory effect of phenothiazine- and phenoxazine-derived chloroacetamides on Leishmania major growth and Trypanosoma brucei trypanothione reductase
Marcu, Ana,Schurigt, Uta,Müller, Klaus,Moll, Heidrun,Krauth-Siegel, R. Luise,Prinz, Helge
supporting information, p. 436 - 443 (2015/12/24)
A number of phenothiazine-, phenoxazine- and related tricyclics-derived chloroacetamides were synthesized and evaluated in vitro for antiprotozoal activities against Leishmania major (L. major) promastigotes. Several analogs were remarkably potent inhibitors, with antileishmanial activities being comparable or superior to those of the reference antiprotozoal drugs. Furthermore, we explored the structure-activity relationships of N-10 haloacetamides that influence the potency of such analogs toward inhibition of L. major promastigote growth in vitro. With respect to the mechanism of action, selected compounds were evaluated for time-dependent inactivation of Trypanosoma brucei trypanothione reductase. Our results are indicative of a covalent interaction which could account for potent antiprotozoal activities.
Conventional as well as microwave assisted synthesis of some new N 9-[hydrazinoacetyl-(2-oxo-3-chloro-4-substituted aryl azetidine)]-carbazoles: Antifungal and antibacterial studies
Srivastava,Nema,Srivastava
, p. 606 - 612 (2008/09/19)
Carbazole on reaction with chloroacetyl chloride afford N 9-(chloroacetyl)-carbazole, 1 which on treatment with hydrazine hydrate has yielded N9-(hydrazinoacetyl)-carbazole, 2. Condensation of 2 with various aromatic aldehydes afforded N9-(arylidene hydrazinoacetyl)-carbazoles, 3 which on cycloaddition with chloroacetyl chloride in the presence of triethylamine yielded N9-[hydrazinoacetyl-(2-oxo- 3-chloro-4-substituted aryl azeitidine)]-carbazoles 4. All the above reactions are also performed by microwave assisted synthetic method. The structures of all the products are characterized by microanalytical data and spectroscopic techniques. All the synthesized products are screened for their antibacterial activity against Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and antifungal activity against Aspergillus nigar, Aspergillus flavus, Fusarium oxisporium and Trichoderma viride.