Design, Synthesis, Anti-Proliferative, and Apoptotic Assessment of Spirocyclopropyl Oxindole-Isatin Hybrids on Triple-Negative Breast Cancer.

A series of 1H-1,2,3-triazole-tethered spirocyclopropyl oxindole-isatin hybrids were synthesized using a copper-promoted click reaction and evaluated for their anti-proliferative activities against triple-negative breast cancer cell lines. The most potent compound in the series outperformed tamoxifen and 5-fluorouracil, with selectivity indices of 1.60 and 1.

Cu-promoted synthesis of triclosan-Mannich and Glaser adducts: anti-mycobacterial evaluation with validations.

 The WHO, Global tuberculosis report 2022 estimated number of tuberculosis (TB) cases reached 10.6 million in 2021, reflecting a 4.5% increase compared with the 10.

Chemical constituents from rhizomes of Cautleya spicata (Sm.) Baker (Zingiberaceae).

The chemical investigation of ethanolic extract from rhizomes of Cautleya spicata (Sm.) Baker (Zingiberaceae) has resulted in the isolation of eight compounds which were characterised as β-sitosterol (1), β-sitosterol β-D-glucoside (2), bergapten (3), zerumin A (4), (E)-labda-8(17),12-diene-15,16-dial (5), kaempferol (6), quercetin (7) and astragalin (8). All compounds were identified by spectroscopic and chemical methods.

Synthesis and structure-activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2.

Following a structure-based virtual screening, a series of 2,4 thiazolidinediones was synthesized in order to explore structure activity relationships for inhibition of the Plasmodium falciparum cysteine protease falcipain-2 (FP-2) and of whole cell antiparasitic activity. Most compounds exhibited low micromolar antiplasmodial activities against the P. falciparum drug resistant W2 strain.

Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives.

The synthesis and antiplasmodial and antimycobacterial evaluation of two new series of nitroimidazole and nitroimidazooxazine derivatives is described. The majority of these compounds, especially hybrids 9d, 9f, and 14b, exhibited potent activity against the chloroquine-resistant K1 strain of Plasmodium falciparum. Furthermore, a notable number from the tetrazole series were significantly more active against M.

Antibacterial sesquiterpene lactone glucoside from seed pods of Bauhinia retusa.

From the seed pods of Bauhinia retusa, a new eudesmane sesquiterpene glucoside, 1-O-β-D-glucopyranosyl-9β,15-dihydroxy-5α,6βH-eudesma-3-ene-6α,12-olide (1), has been isolated together with three known compounds, 4'-hydroxy-7-methoxy flavane (2), β-sitosterol (3), and stigmasterol (4). The structures of isolated compounds were verified with the help of 1D, 2D NMR, and HR-ESI-MS spectroscopies. Compound 1 showed moderate antibacterial activity against Pseudomonas aeruginosa and Escherichia coli when a disc diffusion method is used.

Chemical and antibacterial constituents of Skimmia anquetelia.

Investigation of the leaves of Skimmia anquetelia (Rutaceae) led to the isolation of a new coumarin glucoside 7,8-dihdroxy-6-[3'-beta- D-glucopyranosyloxy-2'(xi)-hydroxy-3'-methylbutyl]-coumarin ( 1) together with five known coumarins: 6-(2,3-dihydroxy-3-methylbutyl)-7-methoxycoumarin ( 2), skimmin ( 3), osthol ( 4), esculetin ( 5) and scopuletin ( 6). The antibacterial activity of compounds 1 and 3 was also investigated against the plant bacterial pathogens Agrobacterium tumifaciens, Pseudomonas syringae and Pactobacterium carotovorum. Structures were determined on the basis of analyses of spectral evidence including 1D, 2 D NMR (COSY, HMQC, HMBC and NOESY) and mass spectroscopy.