Journal: Journal of Medicinal Chemistry

Article Title: Proline-Hinged α-Helical Peptides Sensitize Gram-Positive Antibiotics, Expanding Their Physicochemical Properties to Be Used as Gram-Negative Antibiotics

doi: 10.1021/acs.jmedchem.3c01473

Figure Lengend Snippet: Determination of “more” and “less” potentiated antibiotics in five different classes, and comparisons of their physicochemical characteristics. The five classes included rifamycins (R), macrolides (M), pleuromutilin (P), oxazolidinone (O), and tetracyclines (T). The IC 50 value of each antibiotic was measured using the E. coli S30 extract system. “More” and “less” potentiated antibiotics in each class were defined by the dashed correlation line in (a)–(e), respectively. Comparisons of the physicochemical characteristics between MPG and LPG in the presence of 1403. (f) Charge at pH 7.0, (g) ClogD 7.4 , (h) PSA/MSA, (i) flexibility, (j) MW, (k) amphiphilic moment, (l) and globularity. P values between the two groups were analyzed using the Mann–Whitney test (* P < 0.05, ** P < 0.005, and *** P < 0.0005).

Article Snippet: Telithromycin (HYA0062), erythromycin ethylsuccinate (HYB0957), tylosin (HYB0519A), midecamycin (HYB1908), tilmicosin (HYB0905), tulathromycin A (HY15662), cadazolid (HY100436), radezolid (HY14800), delplazolid (HY100180), lefamulin (HY16908A), pleuromutilin (HYN2301), azamulin (HYW019847), valnemulin (HYB0027), chlortetracycline (HYB1327A), demeclocycline (HY121268), eravacycline (HY16980), rolitetracycline (HY18257), minocycline (HY17412A), meclocycline (HYB1366), omadacycline (HY14865), and sarecycline (HY13858A) were purchased from MedChemExpress.

Techniques: MANN-WHITNEY

Journal: Antibiotics

Article Title: Pipeline of Known Chemical Classes of Antibiotics

doi: 10.3390/antibiotics2040500

Figure Lengend Snippet: Pipeline of antibiotics in known chemical classes.

Article Snippet: , Discovery/development of pleuromutilins , Nabriva , Discovery , Broad spectrum , , [ , , , ] .

Techniques: Bacteria, Northern Blot

Journal: Antibiotics

Article Title: Synthesis and Antibacterial Activity of Alkylamine-Linked Pleuromutilin Derivatives

doi: 10.3390/antibiotics13111018

Figure Lengend Snippet: Structures of pleuromutilin 1 and semisynthetic derivative lefamulin ( 2 ).

Article Snippet: Pleuromutilin was purchased from AK Scientific (Union City, CA, USA) and used as supplied.

Techniques:

Journal: Antibiotics

Article Title: Synthesis and Antibacterial Activity of Alkylamine-Linked Pleuromutilin Derivatives

doi: 10.3390/antibiotics13111018

Figure Lengend Snippet: Structure amine-linked pleuromutilin 22 and bis-pleuromutilin 23 .

Article Snippet: Pleuromutilin was purchased from AK Scientific (Union City, CA, USA) and used as supplied.

Techniques:

Journal: Antibiotics

Article Title: Synthesis and Antibacterial Activity of Alkylamine-Linked Pleuromutilin Derivatives

doi: 10.3390/antibiotics13111018

Figure Lengend Snippet: General method for synthesis of target pleuromutilin derivatives 39 – 41 . Reagents and conditions: (i) preincubate: carboxylic acid RCO 2 H ( 32 – 34 ), EDC·HCl, DMAP, DMF/CH 2 Cl 2 (1:1), 0 °C, N 2 , 30 min, then add amine 24 , rt, N 2 , 18 h (65–80%); (ii) TFA/CH 2 Cl 2 (10% v / v ), rt, 2 h (89–99%); (iii) pre-incubate: tosylate 3 , KI, MeCN, 70 °C, N 2 , 30 min, then add amines 36 , 37 or 38 , DIPEA, 70 °C, N 2 , 4 h (40–56%).

Article Snippet: Pleuromutilin was purchased from AK Scientific (Union City, CA, USA) and used as supplied.

Techniques:

Journal: Antibiotics

Article Title: Synthesis and Antibacterial Activity of Alkylamine-Linked Pleuromutilin Derivatives

doi: 10.3390/antibiotics13111018

Figure Lengend Snippet: General method for preparation of target pleuromutilin derivatives 42 – 47 . Reagents and conditions: (i) carboxylic acid 32 – 35 , HBTU, HOBt, DIPEA, DMF, rt, N 2 , 1.5 h (46–75% yields).

Article Snippet: Pleuromutilin was purchased from AK Scientific (Union City, CA, USA) and used as supplied.

Techniques: