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1. (WO2014182839) MACROCYCLIC PEPTIDOMIMETICS WITH NANOMOLAR ANTIFUNGAL AND ANTIMICROBIAL ACTIVITY
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/182839    International Application No.:    PCT/US2014/037186
Publication Date: 13.11.2014 International Filing Date: 07.05.2014
IPC:
A01N 43/90 (2006.01), A01N 43/72 (2006.01), A01P 1/00 (2006.01)
Applicants: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION [US/US]; 223 Grinter Hall Gainesville, FL 32611 (US)
Inventors: OLIFERENKO, Polina; (US).
OLIFERENKO, Alexander; (US).
IBRAHIM, Mohamed, A.; (US).
PANDA, Siva, S.; (US).
KATRITZKY, Alan, R.; (US).
GOPINATHAN-PILLAI, Girinath; (US).
PANDA, Chandramukhi, Sunita; (US)
Agent: RISSER, Jennifer; Edwards Wildman Palmer Llp P.o. Box 55874 Boston, MA 02205 (US)
Priority Data:
61/820,832 08.05.2013 US
Title (EN) MACROCYCLIC PEPTIDOMIMETICS WITH NANOMOLAR ANTIFUNGAL AND ANTIMICROBIAL ACTIVITY
(FR) PEPTIDOMIMÉTIQUES MACROCYCLIQUES PRÉSENTANT UNE ACTIVITÉ ANTIFONGIQUE ET ANTIMICROBIENNE NANOMOLAIRE
Abstract: front page image
(EN)Enantiopure cyclic peptidomimetic antimicrobials compounds that contain S-cysteine ester units and at least one pyridine unit within the macrocyclic ring have been prepared that show exceptional antifungal and antibacterial activity. These 17- or 18-membered macrocyclic compounds display MIC values as antifungal agents as low as 7.5 nm/mL and MIC values as antibacterial agents as low as 0.2 nm/mL. All the macrocyclic peptidomimetic compounds are isolated as crystalline solids in good yield.
(FR)La présente invention concerne la préparation de composés antimicrobiens peptidomimétiques cycliques énantiomériquement purs contenant des unités ester de S-cystéine ainsi qu'au moins une unité pyridine au sein du noyau macrocyclique, lesdits composés présentant une activité antifongique et antibactérienne exceptionnelle. Ces composés macrocycliques à 17 ou 18 chaînons affichent des valeurs de CMI pouvant descendre jusqu'à 7,5 nm/mL en tant qu'agents antifongiques et des valeurs de CMI pouvant descendre jusqu'à 0,2 nm/mL en tant qu'agents antibactériens. Tous les composés peptidomimétiques macrocycliques sont isolés en tant que solides cristallins en rendement satisfaisant.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)