Chebolu Naga Sesha Sai Pavan Kumar

Synthesis and biological evaluation of tetrazole containing compounds as possible anticancer agents

A series of new tetrazole derivatives are synthesized from Baylis–Hillman allyl amines in a clean, efficient and straightforward manner. The stereochemistry of the double bond is confirmed by X-ray diffraction data. These compounds are evaluated for in vitro anticancer activity against five cancer cell lines. Most of the compounds exhibited good anticancer activity in micro molar concentration out of 16 compounds synthesized and screened. Furthermore, the compound 5o has good binding affinity to calf thymus DNA (ct DNA), as assayed by UV-vis absorption and fluorescence spectroscopic methods.

AlCl3/PCC-SiO2-Promoted Oxidation of Azaindoles and Indoles

Abstract A simple and efficient method is described for the oxidation of 7-azaindoles and indoles to 7-azaisatins and isatins using pyridinium chlorochromate–silica gel (PCC-SiO2) with the aid of Lewis acid catalyst aluminium chloride (AlCl3) in dichloroethane. Simplicity of the reaction conditions, easy workup procedure, and good yields are the key features of this protocol. GRAPHICAL ABSTRACT

Synthesis and antimalarial activity of Baylis-Hillman adducts from substituted 2-chloroquinoline-3-carboxaldehydes

Abstract Various quinoline carboxaldehydes were prepared from corresponding anilides using classical Vilsmeier-Haack reaction conditions and transformed into their Baylis-Hillman adducts. The synthesized Baylis-Hillman adducts were screened for their in vitro antimalarial activity against Plasmodium falciparum. Most of the compounds out of 21 compounds synthesized and screened exhibited substantial antimalarial activity.

A facile route for the synthesis 1,4-disubstituted tetrazolone derivatives and evaluation of their antimicrobial activity

A facile route for the synthesis of 20 new 1,4-disubstituted tetrazolone derivatives from allyl bromides of Baylis–Hillman adducts and various 1-substituted tetrazolones is described. All the synthesized compounds were screened for in vitro antibacterial and antifungal activity. Out of 20 newly synthesized compounds 16 compounds showed very good activity against the Gram-positive bacteria Bacillus subtilis compare to the standard drug ciprofloxacin. The compounds 7b, 7n and 7o showed remarkable activity against both the Gram-positive bacteria B. subtilis and Staphylococcus aureus. Two compounds 7l and 7o showed very good activity against the Gram-negative bacteria Escherichia coli. The compounds, when tested for antifungal activity four compounds— 7b, 7l, 7o and 7s— showed very good activity against the strain Aspergillus niger, whereas seven compounds— 7e, 7g, 7h, 7l, 7o and 7s— display good activity against Candida albicans. Compounds 7b, 7e, 7g, 7l and 7o exhibited very good-to-high activity towards all the strains tested.

Efficient Synthesis of N -Allylated 2- Nitroiminoimidazolidine Analogues From Baylis-Hillman Bromides

ABSTRACT Various Baylis–Hillman–derived new N-allylated 2-nitroiminoimidazolidine analogs were efficiently prepared using potassium carbonate as base. Simple workup procedure, excellent yields, and mild reaction conditions are the salient features of this method. All the synthesized compounds are screened for their larvicidal activity on fourth instar mosquito larvae, Culex quinquefasciatus. GRAPHICAL ABSTRACT