3033486-43-7

Name	[1,1′-Biphenyl]-3-carbonitrile, 5-[[1-[(4,5-dihydro-4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl]oxy]-3′-methyl-
CAS	3033486-43-7
Molecular Formula	C24H18F3N5O3
Molecular Weight	481.43
MOL File	3033486-43-7.mol

Synonyms

[1,1′-Biphenyl]-3-carbonitrile, 5-[[1-[(4,5-dihydro-4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl]oxy]-3′-methyl-

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Chemical Properties

density	1.39±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
pka	8.05±0.20(predicted)

Hazard Information

Uses

ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS[1].

in vivo

Zlm-66 (1-5 mg/kg; i.v. and p.o. once) shows good druggability and have a good effect in vivo after oral administration^[1].

1.19Pharmacokinetic Parameters of ZLM-66 in rat^[1].
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	Rat IV 1 mg/kg	Rat PO 5 mg/kg
T_1/2 (h)	1.90±0.28	8.45±4.88
T_max (h)	0.08±0.00	6.67±1.15
C_max (ng/mL)	468.67±63.09	583.33±290.11
AUC_0-t (h*ng/ml)	891.94±79.30	4983.22±3220.11
AUC_0-∞ (h*ng/ml)	940.41±105.00	6594.05±1547.74
CL (ml/h/kg)	1072.31±120.40	791.14±210.66
MRT_0-t (h)	2.03±0.2	6.79±1.90
MRT_0-∞ (h)	2.48±0.35	13.92±6.44
F (%)		140.24

Animal Model:	Six- to 8-week-old male Sprague-Dawley rats (180?230 g)^[1]
Dosage:	1, 5 mg/kg
Administration:	Intravenous injection, oral gavage; 1-5 mg/kg; once
Result:	Possed a better in vivo effect of oral administration with half-life, plasma clearance and oral bioavailability of 8.45 h, 791.14 ml/h/kg and 140.24% respectively.

IC 50

HIV-1 (WT): 13 nM (EC₅₀); HIV-1 (K103N): 13 nM (EC₅₀); HIV-1 (L100I): 24 nM (EC₅₀); HIV-1 (E138K): 25 nM (EC₅₀); HIV-1 (Y181C): 58 nM (EC₅₀); HIV-1 (K103N+Y181C): 260 nM (EC₅₀); HIV-1 (F227L+V106A): 27530 nM (EC₅₀)

References

[1] Zhao LM, et al. Discovery of novel biphenyl-substituted pyridone derivatives as potent non-nucleoside reverse transcriptase inhibitors with promising oral bioavailability. Eur J Med Chem. 2022 Jun 30;240:114581. DOI:10.1016/j.ejmech.2022.114581

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