N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents

    公开(公告)号:US09738684B2

    公开(公告)日:2017-08-22

    申请号:US14754002

    申请日:2015-06-29

    CPC classification number: C07K5/06156 A61K47/59 C07D209/04 C07D209/16

    Abstract: N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents. The invention relates to therapeutically viable antibacterial compositions based on ultra short mimetic of host defense cationic peptides (HDCPs). The invention relates to template based N-terminal modified di-peptidomimetics with or without modifications in polyamine backbone as new antibacterial agents. Most active peptidomimetics were bactericidal and caused a rapid decrease in viability of broad range of Gram-positive and Gram-negative bacterial strains in low micromolar concentration range including activity against clinically relevant pathogen methicillin resistant S. aureus (MRSA) andmethicillin resistant S. epidermidis(MRSE). Further the peptidomimetics were effective against MRSA biofilms (formation inhibition/killing of preformed biofilms) in vitro and were non toxic to human red blood cells and peripheral blood mononuclear cells. The molecules described in present invention do not develop resistance against MRSA under in vitro conditions and hence may be used as topical agents or in similar applications.

    METHOD FOR THE PREPARATION OF UNIFORM, HIGH MOLAR MASS CYCLIC IMINO ETHER POLYMERS

    公开(公告)号:US20170210853A1

    公开(公告)日:2017-07-27

    申请号:US15326866

    申请日:2015-07-10

    CPC classification number: C08G73/0233 A61K47/34 A61K47/59 C08L79/02

    Abstract: A method for production of a uniform polymer of high molar mass is provides, the method comprising: (a) polymerizing cyclic imino ether monomer in a first reaction mixture by cationic ring opening polymerization to produce a polymerized first reaction mixture containing (i) polymerized material and (ii) solvent and/or unreacted cyclic imino ether monomer; (b) separating solvent and/or unreacted cyclic imino ether monomer from polymerized material contained in the polymerized first reaction mixture; (c) copolyerizing by cationic ring opening polymerization a second liquid reaction mixture containing cyclic imino ether monomer and solvent by combining the separated unreacted cyclic imino ether monomer and/or the separated solvent with other components. Also disclosed are polyoxazoline polymers comprising at least 50 wt. % of repeating units derived from a 2-substituted 2-oxazoline monomer selected from 2-methyl-2-oxazoline, 2-ethyl-2-oxazoline, 2-n-propyl-2-oxazoline, 2-i-propyl-2-oxazoline and combinations thereof, said polymer having a DP of at least 250 and a very low dispersity.

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