Lawsozaheer, a new chromone produced by an endophytic fungus isolated from Lam. inhibits the growth of .

One new chromone, lawsozaheer (), and five known compounds 4-(2-hydroxyethyl) phenol (), viriditoxin (), stigmasta-4,6,8(14),22-tetraen-3-one (), -sitosterol () and stigmasterol () were isolated from the fungal broth of . Their structures were elucidated using spectroscopic data. The configuration of was determined by Horeau's method.

Structure-based design, synthesis and biological evaluation of β-glucuronidase inhibitors.

Using structure-based virtual screening approach, a coumarin derivative (1) was identified as β-glucuronidase inhibitor. A focused library of coumarin derivatives was synthesized by eco-benign version of chemical reaction, and all synthetic compounds were characterized by using spectroscopy. These compounds were found to be inhibitor of β-glucuronidase with IC50 values in a micromolar range.

Evaluation of bisindole as potent β-glucuronidase inhibitors: synthesis and in silico based studies.

Bisindole analogs 1-17 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. Out of seventeen compounds, the analog 1 (IC50=1.62±0.

Germa-gamma-lactones as novel inhibitors of bacterial urease activity.

Organogermanium compounds have been used as pharmacological agents. However, very few reports are available on the synthesis and antibacterial activities of lactones containing organogermaniums. The purpose of the present investigation was to determine the effects of different lactone-substituted organogermaniums on bacterial growth and their urease activity.

Cysteine based novel noncompetitive inhibitors of urease(s)--distinctive inhibition susceptibility of microbial and plant ureases.

Based on the catalysis mechanism of urease, a homologous series of 10 cysteine derivatives (CysDs) was designed and synthesized, and their inhibitory activities were evaluated for microbial ureases (Bacillus pasteurii, BPU, and Proteus mirabilis, PMU) and for a plant urease [jack bean (Cavavalia ensiformis), JBU]. As already described, thiol-compounds might inhibit urease activity by chelating the nickel atoms involved in the catalysis process. In contrast to cysteine, which has been reported to be a very weak urease inhibitor, we verified a potential inhibitory activity of these CysDs.

Tetraketones: a new class of tyrosinase inhibitors.

Twenty-eight tetraketones (1-28) with variable substituents at C-7 were synthesized and evaluated as tyrosinase inhibitors. Remarkably compounds 25 (IC(50)=2.06 microM), 11 (IC(50)=2.

Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles.

Based on structure of the substrate of urease and for the purpose of designing pharmacophore models for urease inhibitors, which could be effective in physiological and pharmacological studies, a series of twenty-five 1,3,4-diazole-2(3H)-thiones-2(3H)-thiones, 1,3,4-diazoles-2(3H)-thiones, and 1,2,4-tri-3-thiones (OSNs) were designed, synthesized, and evaluated for various kinetic parameters of urease inhibition. OSNs inhibited the activity of urease(s) in a concentration dependent fashion. Dixon as well as Lineweaver-Burk plots and their secondary replots indicated that the nature of inhibition was of pure competitive type for all the 25 compounds.

New tropane alkaloids from Erythroxylum moonii.

Four new tropane alkaloids were isolated from the leaves of Erythroxylum moonii and identified as 3 alpha-isobutyryloxy-7 beta-hydroxynortropane (1), 3 alpha-hydroxy-7 beta-phenylacetoxynortropane (2), 3 alpha-cis-cinnamoyloxytropane (3), and 3 alpha-hydroxy-6 beta-(3'-hydroxy-2'-methyl-3'-phenylpropionyloxy)-7 beta-hydroxytropane (4). Other alkaloids isolated for the first time from E. moonii were 3 alpha-benzoyloxytropane, 3 alpha-phenylacetoxytropane, 3 alpha-trans-cinnamoyloxytropane, and 3 alpha-phenylacetoxy-6 beta,7 beta-dihydroxynortropane.