Patent classifications
C07J73/00
SMALL MOLECULES ACTIVE AGAINST GRAM-NEGATIVE BACTERIA
Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
Azasteroids for treatment of tuberculosis
The present invention provides a compound having the structure: ##STR00001##
for use in combination with an anti-tuberculosis drug for treating a subject infected with M. tuberculosis.
TRIPTOLIDE DERIVATIVE AND PREPARATION METHOD THEREFOR AND USE THEREOF
A triptolide derivative, a preparation method therefor, and a method for use thereof are described. The triptolide derivative has the structure as shown in general formula I, and the definition of each substituent is as described in the description and claims. The triptolide derivative has improved immunosuppressive activity and anti-tumor activity, low toxicity and high safety, thus having good development and application prospects.
##STR00001##
Potent aromatase inhibitors through fungal transformation of anti-cancer drug testolactone: An approach towards treatment of breast cancer
Biotransformation of an aromatase inhibitor, testolactone (1), yielded five new metabolites, 7α-hydroxy-3-oxo-13,17-secoandrosta-1,4-dieno-17,13α-lactone (2), 7β-hydroxy-3-oxo-13,17-seco-5β-androsta-1-eno-17,13α-lactone (3), 3α,11β-dihydroxy-13,17-seco-5β-androsta-17,13α-lactone (4), 4β,5β-epoxy-3β-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (5), and 4β,5β-epoxy-3α-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (6). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+ (estrogen-positive) breast-cancers and several other diseases caused by overexpression of aromatase enzyme. Metabolites 3 (IC.sub.50=8.60±0.402 nM), and 4 (IC.sub.50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC.sub.50=0.716±0.031 μM), and the standard aromatase inhibiting drug, exemestane (IC.sub.50=0.232±0.031 μM). Derivatives 2 (IC.sub.50=11.68±0.73 μM), 5 (IC.sub.50=10.37±0.50 μM) and 6 (IC.sub.50=0.82±0.059 μM) have also a good inhibition against aromatase enzyme. Therefore, metabolites 2-6 have the potential to serve as therapeutic agents against diseases caused by aromatase enzyme, including breast cancer.
Low molecular weight modulators of the cold menthol receptor TRPM8 and use thereof
The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.
Small molecules active against gram-negative bacteria
Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
Small molecules active against gram-negative bacteria
Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF
The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.
##STR00001##
Small molecules active against gram-negative bacteria
Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
Small molecules active against gram-negative bacteria
Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.