Table 2.

The ClogP, LLE, and melting point of 1a–i

Compounds	ClogPa	LLEb	Mp (oC)	tPSA
Macozinone	5.1	3.6	185–187	87.7
1a	3.1	–	151–153	59.7
1b	3.7	–	162–165	59.7
1c	4.2	2.5	196–198	59.7
1d	4.8	2.1	218–221	59.7
1e	2.0	3.8	173–175	68.9
1f	1.3	–	172–174	68.9
1g	5.8	–	182–185	59.7
1h	5.8	–	180–182	59.7
1i	4.1	–	193–195	68.5

^aClogP and tPSA were determined by Chemdraw Professional Version 16.0

^bLipophilic Ligand Efficiency (LLE) was calculated from the equation: LLE = log₁₀MIC − Clog₁₀P