Plant-based larvicidal agents: An overview from 2000 to 2018.

Current review aims to systematically segregate, analyze and arrange the key findings of the scientific reports published on larvicidal plants including larvicidal formulations. The investigation was carried out by analyzing the published literature in various scientific databases, subsequently, the key findings of the selective scientific reports having larvicidal potency (LC50) of extract or isolated oil<100 µg/mL were tabulated to provide the concise and crucial information. Special emphasis was given on reports in which LC50 of extract or isolated oil was reported to be < 10 µg/mL, genus or species documented in multiple independent studies, advancement in larvicidal formulations and activity of isolated phytoconstituents. Extensive analysis of published literature revealed that the larvicidal potency of herbal resources varied from sub-microgram/ml to practically insignificant. Overall, this unprecedented summarized and arranged information can be utilized for design, development and optimization of herbal based formulation having potential larvicidal activity.

Hit optimization studies of 3-hydroxy-indolin-2-one analogs as potential anti-HIV-1 agents.

In the current study, twenty-two compounds based upon 3-hydroxy-3-(2-oxo-2-phenylethyl)indolin-2-one nucleus were designed, synthesized and in vitro evaluated for HIV-1 RT inhibition and anti-HIV-1 activity. Compounds 3d, 5c and 5e demonstrated encouraging potency against RT enzyme as well as HIV-1 in low micromolar to nanomolar concentration with good to excellent safety index. Structure activity relationship studies revealed that halogens such as bromo or chloro at 5th the position of oxindole ring remarkably enhanced the potency against RT. Moreover, methoxy or chloro groups at the ortho position of phenyl ring also significantly favored RT inhibition activity. Seven compounds (3b, 3c, 3d, 3e, 5b, 5c and 5e) with better anti-HIV-1 potency were tested against the mutant HIV-1K103N strain. The putative binding mode, as well as interaction patterns of the best active compound 5c with wild HIV-1 RT were studied via docking studies.