Synthesis of narrow-spectrum anti-mycobacterial molecules without effect on the diversity of gut microbiota in mice based on the structure of rifampicin.

Rifampicin (RIF) is a broad-spectrum antimicrobial agent that is also a first-line drug for treating tuberculosis (TB). Based on the naphthyl ring structure of RIF this study synthesized 16 narrow-spectrum antimicrobial molecules that were specifically anti-Mycobacterium tuberculosis (Mtb). The most potent candidate was 2-((6-hydroxynaphthalen-2-yl) methylene) hydrazine-1-carbothioamide (compound 3c) with minimum inhibitory concentration (MIC) of 1 μg/mL against Mtb.

19 Schiff bases as antimycobacterial agents: synthesis, molecular docking and a plausible mechanism of action.

To discover novel anti- () drugs, 19 compounds were synthesized; their anti- effects were evaluated and mechanisms of action were preliminarily explored. The compounds were synthesized and their anti- activity was elucidated using resazurin microtiter assays. The plausible target of the potential compound was investigated by microimaging techniques, gas chromatography-mass spectrometry analysis and molecular docking.

Synthesis, antimycobacterial evaluation, and molecular docking study of 1,2,4-triazole derivatives.

Fifteen 1,2,4-triazole derivatives were synthesised in this study and their MIC values against () ranged from 2 to 32 μg/mL. Furthermore, their antimycobacterial activity was positively correlated with the KatG enzyme docking score. Among the 15 compounds, compound showed the strongest bactericidal activity with an MIC of 2 μg/mL.

Antimycobacterial Compound of Cynoglossum lanceolatum Forsk.: Bioassay Guided Isolation, Molecular Docking, Synthesis of Analogs, and a Plausible Mechanism of Action.

Tuberculosis (TB) remains a major threat to human health. Due to the prevalence of drug-resistant Mycobacterium tuberculosis (Mtb), it is urgent to discover drugs with new mechanisms of action (MOA) to ensure effectiveness against strains that are resistant to existing TB drugs. Cynoglossum lanceolatum Forsk was used to treat TB in Traditional Chinese Medicine.

Quinoline derivatives as potential anti-tubercular agents: Synthesis, molecular docking and mechanism of action.

Development of new drugs with novel mechanisms of action is required to combat the problem of drug-resistant Mycobacterium tuberculosis. The present investigation is aimed at combining two pharmacophores (quinoline or isoquinolines and thiosemicarbazide) to synthesize a series of compounds. Seven compounds were synthesized based on combination principle in this study.

Bioassay-guided isolation of a Mycobacterium tuberculosis bioflim inhibitor from Arisaema sinii Krause.

Mycobacterium tuberculosis biofilms harbour drug-tolerant bacteria. Identification of drugs that inhibit biofilm formation could enable the dramatic shortening of tuberculosis treatments using standard antibiotics. Arisaema sinii Krause is used to treat pulmonary and lymphatic tuberculosis by Dong People of China.

[Studies on flavonoids from Derris eriocarpa].

Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before.

A novel franchetine type norditerpenoid isolated from the roots of Aconitum carmichaeli Debx. with potential analgesic activity and less toxicity.

Further investigation on the phytochemistry of the plant Aconitum carmichaeli Debx. led to isolate a new franchetine type C(19)-diterpenoid alkaloid, guiwuline 1. Its structure was established on the basis of the spectroscopic data (1D and 2D NMR, HRESIMS, UV, IR).

[Study on skin toxicology and penetration enhancement of skin absorption of volatile oil extracted from tender branchers of Camellia oleifera].

Objective: To study the toxicity on skin and penetration effect of volatile oil from tender branchers of Camellia oleifera on nitrendipine, baicalin, nimesulide for percutaneous obsorption.

Method: Acute skin toxicity, irritation and allergy on rats were tested, and mouse skin in vitro was applied for studying the effects of different concentrations of volatile oil in nitrendipine, baicalin, nimesulide on drug permeation.

Result: Different dosage volatile oil had no acute toxicity, irritation or hypersensitive effects.

[Structure-activity relationships of salicylic acid and its analogs in the inhibitory action on beta-lactamase].

Aim: Nineteen compounds related to salicylic acid were evaluated for their in vitro activity of inhibiting beta-lactamase isolated from a resistant strain of Pseudomonas aeruginosa, and their structure-activity relationships were examined.

Methods: Nitrocefin method was used.

Results: The 50% inhibitory concentration (IC50) of salicylic acid inhibiting beta-lactamase was 22 mmol x L(-1); four analogs had IC50 lower than that of salicylic acid; fifteen analogs had IC50 higher than that of salicylic acid.

Chemical composition of the volatile oil from Cynanchum stauntonii and its activities of anti-influenza virus.

The volatile oil of the roots of Cynanchum stauntonii was examined by gas chromatography-mass spectrometry (GC-MS). Thirty-eight constituents were identified. (E,E)-2,4-Decadienal, 3-efhyl-4-methypentanol, 5-pentyl-3H-furan-2-one, (E,Z)-2,4-decadienal and 2(3H)-furanone,dihydro-5-pentyl were found to be the major components.

The synergistic activity of antibiotics combined with eight traditional Chinese medicines against two different strains of Staphylococcus aureus.

The ethanolic extracts of eight traditional Chinese medicines and four antibiotics were investigated for their combined effects on the resistance of Staphylococcus aureus (S. aureus) in vitro. Methicillin resistant S.