Efficient syntheses of some new substituted pyrazoline derivatives linked to substituted benzimidazole scaffold were performed by multistep reaction sequences. All the synthesized compounds were characterized using elemental analysis and spectral studies (IR, 1D/2D NMR techniques and mass spectrometry). The synthesized compounds were screened for their antimicrobial activity against selected Gram-positive and Gram-negative bacteria, and fungi strain. The compounds with halo substituted phenyl group at C5 of the 1-phenyl pyrazoline ring (15, 16 and 17) showed significant antibacterial activity. Among the screened compounds, 17 showed most potent inhibitory activity (MIC = 64 µg mL -1 ) against a bacterial strain. The tested compounds were found to be almost inactive against the fungal strain C. albicans, apart from pyrazoline-1-carbothiomide 21, which was moderately active.

Background: Aristolochia indica L. of the family Aristolochiaceae is a twining perennial herbs with an ancient history of medicinal use. In the Indian Ayurvedic system, it is mentioned for the treatment of snake venom, scorpion venom, pimple, fever and worm infection. Objective: To make accessible the current information that is existing on the traditional uses, phytochemistry, pharmacology and toxicology of Aristolochia indica . Additionally, to emphasize the potential uses of this plant to treat various diseases and to bring in a foundation for further research. Methods:: The present review is carried out by compiling literature from 1935 to 2020, concerning the morphology, tradional uses, phytochemistry, pharmacological activities and toxicological aspects of Aristolochia indica. Results:: Diverse chemical compounds including Aristolochic acids, aristolactam, Phenanthrenes, alkaloids, lignans, steroids and terpenes have been isolated from this plant. Mostly in-vivo models indicated several evidence in the use of this plant particularly to regulate fertility. Few in-vivo studies also proved usefulness of this plant in inflammation and diabetis. In some in-vitro studies the anti-snake venom, larvicidal, and anti-oxidant potential has been proved. Conclusion: Preclinical studies have demonstrated remarkable activity which support the conventional use of the plant as an antivenum, antifertility, antimicrobial and anti-inflammatory agent. Although few phytochemicals isolated (Aristolic acid, (12S)-7,12-secoishwaran-12-ol, Aristololactam-I N-β-D-glucoside, Aristolochic acids, β-sitosterol, (-) Hinokinin and Aristolactam-I) from the plant exhibited remarkable biological activity, it was only confined to preclinical study. Even though, the isolated aristolochic acids showed significant anti-snake venom activity but it was found to be nephrotoxic and mutagenic. More detailed safety data pertaining to dose of crude extracts or pure compounds needs to be generated.

Spathodea campanulata P. Beauv., belonging to the family Bignoniaceae, is a big erect tree with an ancient history of medicinal use in Africa. In the traditional system, it is mentioned for the treatment of malaria, diabetes, stomach ulcers, wounds, skin infections and viral diseases. The aim of the review is to make available the current information that exists on the traditional uses, phytochemistry, pharmacology, and toxicology of S. campanulata. Additionally, the potential uses of this plant to treat various diseases and to bring in a foundation for further research are emphasized. The present review is carried out by compiling literature from 1972 to 2021, concerning the morphology, traditional uses, phytochemistry, pharmacological activities, and toxicological aspects of S. campanulata. Literatures were collected from various online search engines, viz. Google Scholar, PubMed, Science Direct, Core, and Semantic Scholar. Diverse chemical compounds including iridoids, terpenoids, steroids, cinnamic acid derivatives, cerebrosides, flavonoids, and carotenoids have been isolated from this plant. Mostly in-vivo models have indicated several evidences of the use of this plant particularly to cure malaria. Few in-vivo studies have also proved the usefulness of this plant in inflammation, wound healing, diabetes, and convulsion. In some in-vitro studies, the anticancer, antibacterial, antiviral insecticidal, larvicidal, and anti-oxidant potential has been proved. Preclinical studies have demonstrated remarkable activity which supports the conventional use of the plant as an antimalarial, wound healing, antidiabetic, antimicrobial, and anti-inflammatory agent for years without any adverse effects. Based on the results obtained from a combination of in vivo and in vitro potency and toxicity studies reported, S. campanulata is a promising agent in the development of nutraceuticals against malaria and diabetes. Although few phytochemicals isolated (ursolic acid, tomentosolic acid, 20β-hydroxyursolic acid, verminoside, specioside, spathoside, kaempferol, and β-sitosterol-3-acetate) from the plant exhibited remarkable biological activity, it was only confined to preclinical study. The only clinical study documented is for curing malaria, but with crude extract only. With its current extensive traditional use, there is a need for additional studies of the isolated compounds, clinical trials, and product development to take full advantage of this widely distributed medicinal plant.

Background: Emergence of resistance to accessible anticancer drugs became a threat to human lives in the recent time. To address this issue, discovery of novel anticancer agents becomes very essential. Benzimidazoles and pyrimidines have been reported to possess potent anticancer activity. Materials and Methods: A hybrid approach has been used, in which core structure of potentially active N-benzyl benzimidazole and pyrimidine derivatives are brought together in to a single molecule. The desired compounds were prepared by the condensation of N-benzyl benzimidazole chalcones with guanidine hydrochloride. The synthesized compounds were characterized using spectral studies (IR, 1 H, 13 C-NMR techniques and mass spectrometry). All the compounds were screened for their anticancer activity against human breast cancer cell line MDA-MB-231. Results: The spectral data's are in well agreement with the synthesized compounds 5a-e. Compounds 5b (GI 50 = 39.6 μM) and 5a (GI 50 =84.0 μM) exhibited significant anticancer activity. Conclusion: Owing to the anticancer activity, compound 5b can be used as lead structure in the development of yet more potent anticancer agents.

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