Lincosamides of general formula I, where R1 is selected from C2-C8 alkyl or C2-C8 alkenyl; R3 is selected from OH, O(C1-C4 alkyl), SH, S(C1-C4 alkyl) or halogen; R4 is H or C1-C3 alkyl; each of R21, R22, R23, R24, R25 is independently selected from the group consisting of H, OH, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl, halogen, O(C1-C4 alkyl), O(C1-C4 alkenyl), O(C1-C4 alkynyl), NH.sub.2, N(C1-C4 alkyl).sub.2, N(C1-C4 alkenyl).sub.2, N(C1-C4 alkynyl).sub.2; and pharmaceutically acceptable salts thereof. A method of preparation thereof, in particular a biosynthetic method using newly discovered functions of celesticetin biosynthetic proteins Ccb1 and/or Ccb2. Lincosamides of general formula I are suitable for use as antibacterial and antiprotozoal substances.

Provided are lincosamide compounds for the treatment of infectious diseases. The lincosamides described herein are modified at the amino acid (southern) region. The lincosamides may have further modification at the C-1 and C-7 positions of the aminooctose (northern) region, thus distinguishing them from lincomycin and clindamycin. Also provided are methods for preparing the lincosamide compounds, pharmaceutical compositions comprising the lincosamide compounds, and methods of treating infectious diseases using the disclosed lincosamide compounds.

Lincosamides of general formula I, where R1 is selected from C2-C8 alkyl or C2-C8 alkenyl; R3 is selected from OH, O(C1-C4 alkyl), SH, S(C1-C4 alkyl) or halogen; R4 is H or C1-C3 alkyl; each of R21, R22, R23, R24, R25 is independently selected from the group consisting of H, OH, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl, halogen, O(C1-C4 alkyl), O(C1-C4 alkenyl), O(C1-C4 alkynyl), NH.sub.2, N(C1-C4 alkyl).sub.2, N(C1-C4 alkenyl).sub.2, N(C1-C4 alkynyl).sub.2; and pharmaceutically acceptable salts thereof. A method of preparation thereof, in particular a biosynthetic method using newly discovered functions of celesticetin biosynthetic proteins Ccb1 and/or Ccb2. Lincosamides of general formula I are suitable for use as antibacterial and antiprotozoal substances.

Lincosamides of general formula I, where R1 is selected from C2-C8 alkyl or C2-C8 alkenyl; R3 is selected from OH, O(C1-C4 alkyl), SH, S(C1-C4 alkyl) or halogen; R4 is H or C1-C3 alkyl; each of R21, R22, R23, R24, R25 is independently selected from the group consisting of H, OH, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl, halogen, O(C1-C4 alkyl), O(C1-C4 alkenyl), O(C1-C4 alkynyl), NH.sub.2, N(C1-C4 alkyl).sub.2, N(C1-C4 alkenyl).sub.2, N(C1-C4 alkynyl).sub.2; and pharmaceutically acceptable salts thereof. A method of preparation thereof, in particular a biosynthetic method using newly discovered functions of celesticetin biosynthetic proteins Ccb1 and/or Ccb2. Lincosamides of general formula I are suitable for use as antibacterial and antiprotozoal substances.

The invention provides a process of controlling the impurities of clindamycin hydrochloride, comprising a step of purifying said clindamycin hydrochloride by two-phase high performance liquid chromatography, wherein the chromatographic conditions are as follows: the detection wavelength is 200-220 nm; the column temperature is 20-40 C.; the flow rate is 0.8-1 ml/min; Mobile phase A: 0.025 mol/L potassium dihydrogen phosphate solution; Mobile phase B: Acetonitrile; and gradient elution is performed. The method of controlling impurities of the invention can solve the problem of the interference by excipients and the problem of the separation of many impurities at the same time. It also provides an effective method for setting quality standard of impurities in such a formulation.

The invention provides a process of controlling the impurities of clindamycin hydrochloride, comprising a step of purifying said clindamycin hydrochloride by two-phase high performance liquid chromatography, wherein the chromatographic conditions are as follows: the detection wavelength is 200-220 nm; the column temperature is 20-40 C.; the flow rate is 0.8-1 ml/min; Mobile phase A: 0.025 mol/L potassium dihydrogen phosphate solution; Mobile phase B: Acetonitrile; and gradient elution is performed. The method of controlling impurities of the invention can solve the problem of the interference by excipients and the problem of the separation of many impurities at the same time. It also provides an effective method for setting quality standard of impurities in such a formulation.

The disclosure is directed to compounds identified as allosteric modulators of 5-HT 2CR, as well as pharmaceutical compositions and methods using the same. Certain embodiments also include methods of identifying and methods of synthesizing the compounds. Optimization and development of allosteric 5-HT 2CR modulators that bind sites other than the primary ligand binding site generate novel, highly selective, and potent ligands of 5-HT2CR. Such molecules can be used as small molecule probes for the nervous system and as effective therapeutics for a variety of diseases.

The disclosure is directed to compounds identified as allosteric modulators of 5-HT 2CR, as well as pharmaceutical compositions and methods using the same. Certain embodiments also include methods of identifying and methods of synthesizing the compounds. Optimization and development of allosteric 5-HT 2CR modulators that bind sites other than the primary ligand binding site generate novel, highly selective, and potent ligands of 5-HT2CR. Such molecules can be used as small molecule probes for the nervous system and as effective therapeutics for a variety of diseases.