Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:6.2.1.7 (BAL)
 1,977 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

To more rapidly prepare members of the 1,3-bis(acylamino)-2-butanone class of cysteine protease inhibitors, a solid-phase synthesis was developed. 1-Azido-3-amino-2,2-dimethoxybutane (4), which has the two amino groups differentiated and the ketone protected as a a ketal, served as a surrogate for the 1,3-diamino-2-butanone core. Amine (4) was coupled to the BAL-resin-linked carboxylic acids derived from alpha-amino acid esters. Evaluation of a small combinatorial array by measuring inhibition constants (Ki,appS) against cathepsins K, L, and B provided some structure-activity relationship trends with respect to selectivity and potency. Novel, potent inhibitors of cathepsins K and L were identified.
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PMID:Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L. 1074 10

A root extract of Valeriana jatamansi (code BAL-O) exhibited larvicidal and adulticidal activity against different mosquito species. The median lethal concentration (LC50) of BAL-O against larvae of Anopheles stephensi, Anopheles culicifacies, Aedes aegypti, Aedes albopictus, and Culex quinquefasciatus were 68.1, 42.8, 51.2, 53.8, and 80.6 mg/liter, respectively. The LC50 and the 90% lethal concentration against adult An. stephensi, An. culicifacies, Ae. aegypti, Ae. albopictus, and Cx. quinquefasciatus were 0.14, 0.16, 0.09, 0.08, and 0.17 and 0.24, 0.34, 0.25, 0.21, and 0.28 mg/cm2, respectively. The median knock-down time and 90% knock-down time of the fraction were 13, 13, 12, 13, and 18 and 24, 25, 21, 20, and 42 min against An. stephensi, An. culicifacies, Ae. aegypti, An. albopictus and Cx. quinquefasciatus, respectively, using 0.28 mg/cm2 impregnated papers. The median effective time and 90% effective time against An. stephensi at 4 degrees C were 46.6 and 8.7 days, and at 29 degrees C, 25.5 and 5.6 days, respectively. Gas chromatographic-mass spectrometric analysis of BAL-O showed 2-butanone,4-(2,6,6-trimethyl-2-cyclohexen-l-yl) (10.11%), patchouli alcohol (8.55%), cubenol (5.97%), caryophyllene oxide (5.46%), cadinol (5.23%), and aristolene (5.19%).
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PMID:Insecticidal activity of Valeriana jatamansi (Valerianaceae) against mosquitoes. 1866 42