Antibacterial guanidine oligomer with resistance to drug resistance, and preparation method and application thereof
A preparation method and antibacterial guanidine technology are applied in the field of antibacterial guanidine oligomers and their preparation, and can solve the problems of reduced drug resistance, low rate of bacterial drug resistance and the like
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Embodiment 1
[0039] After testing, the present invention develops 55 kinds of antibacterial guanidine oligomers with broad-spectrum antibacterial properties, and its chemical formula is as follows:
[0040]
[0041] where 5≤n≤8;
[0042] Wherein the molecular formula of R includes any one of formula (I), formula (II), formula (III), formula (IV) and formula (V); the molecular formula of R1 includes formula (I), formula (II), formula Any one of (III), formula (IV), formula (V), (VI), formula (VII), formula (VIII), (IX), (X) and (XI).
[0043]
[0044]For the convenience of recording, the molecular formula of R is formula (I), formula (II), formula (III), formula (IV) and formula (V) respectively numbered as D, A, B, C and E; the molecular formula of R1 is Formula (I), formula (II), formula (III), formula (IV), formula (V) (VI), formula (VII), formula (VIII), (IX), (X) and (XI) respectively They are numbered 9, 1, 2, 3, 5, 6, 4, 10, 8, 7, 11 in sequence. Numbering example: when R is...
Embodiment 2
[0054] like figure 1 As shown, the present invention also discloses a method for synthesizing anti-drug resistance antibacterial guanidine oligomers, comprising the steps of:
[0055] S1: preparing a dimethylmercapto imidium iodide monomer having the following molecular formula;
[0056]
[0057] S2: the dimethyl mercapto imidium iodide monomer and H 2 N-R 1 -NH 2 , reacting anhydrous N,N-dimethylformamide DMF and N,N-diisopropylethylamine DIPEA to obtain the guanidine oligomer;
[0058] Wherein the molecular formula of R in the dimethylmercapto imidium iodide monomer includes any one of formula (I), formula (II), formula (III), formula (IV) and formula (V); the molecular formula of R1 Including formula (I), formula (II), formula (III), formula (IV), formula (V) (VI), formula (VII), formula (VIII), (IX), (X) and (XI) any of the.
[0059]
[0060]
[0061] In the above step S1, the following steps are included:
[0062] S11: Weigh H 2 N-R-NH 2 and benzoyl isot...
experiment example 1
[0069] This experimental example takes the C3 compound as an example to describe in detail.
[0070] Materials and methods: All reagents were provided by Acros, TCI (USA), Sigma-Aldrich, McLean, Adamas and other organic reagent companies and Beyontian Biotechnology Co., Ltd., and were used directly without further purification (unless otherwise specified outside). The ultrapure water used in the experiment came from a Milli-Q purification instrument. The inert gas is nitrogen or argon.
[0071] The synthetic steps of C3 are as follows: figure 1 shown. Carry out the synthesis of dimethyl mercapto imidium iodide monomer first. Weigh 1,4-butanediamine (0.84g, 9.5mmol) and benzoyl isothiocyanate (3.25g, 20.0mmol), then add 100mL of dichloromethane and mix well, stir at room temperature for 24-48h to get The mixture was filtered and washed to obtain the dibenzamide dithiourea compound for the next reaction. Weigh the dibenzamide dithiourea compound (3.1g, 7.5mmol) obtained in...
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