Table 3. Biological Evaluation of Pyrazolo[1,5-a]pyrimidin-7(4H)-one Derivatives.

	MIC (μM)						reporter gene assay
hit	7H9a	GASTb	GBSA/DBSAc	nitrate/butyrated	Chole	CydKOf	cell wallg	DNA damageh
1	12.5	2.3	12.5	12.5	9.40	12.5	no	no
2	19.0	19.0	4.70	6.25	12.5	25.0	no	no
4	12.5	3.13	9.40	6.25	12.5	9.40	no	no
P19	3.13	1.20	3.13	1.56	3.13	3.13	no	no
INH	0.39	0.10	0.30	N/Di	0.20	0.30	N/D	N/D
SQ109	N/D	N/D	N/D	N/D	N/D	N/D	yes	N/D
MOX	N/D	N/D	N/D	N/D	N/D	N/D	N/D	yes

^aMIC of compound against Mtb strain H37Rv in Middlebrook 7H9/BSA containing glucose/glycerol/Tween 80.

^bMIC of compound against Mtb strain H37Rv in GAST/Fe.

^cMIC of compound against Mtb strain H37Rv in Middlebrook 7H9/BSA/Tyloxapol with glucose (GBSA) or dipalmitoylphosphatidylcholine (DBSA) as the carbon source.

^dMIC of compound against Mtb strain H37Rv in Middlebrook 7H9/BSA/Tyloxapol/butyrate/0.1 mM nitrite/pH 6.0.

^eMIC of compound against Mtb strain H37Rv in Middlebrook 7H9/BSA/Tyloxapol/cholesterol.

^fMIC of compound against Mtb strain H37Rv in Middlebrook 7H9/ADC with cydC::aph.

^gInduction of the cell wall responsive iniBAC promoter as measured using the piniB-LUX reporter strain.

^hInduction of the DNA damage responsive recA and radA reporters using the precA-LUX and pradA-LUX reporter strains.

ⁱNot determined.