Title: Atevirdine
CAS Registry Number: 136816-75-6
CAS Name: 1-[3-(Ethylamino)-2-pyridinyl]-4-[(5-methoxy-1H-indol-2-yl)carbonyl]piperazine
Additional Names: N-ethyl-2-[4-(5-methoxy-1H-indol-2-ylcarbonyl)-1-piperazinyl]-3-pyridinamine; 1-[5-methoxyindolyl-2-carbonyl]-4-[3-(ethylamino)-2-pyridinyl]piperazine
Manufacturers' Codes: U-87201
Molecular Formula: C21H25N5O2
Molecular Weight: 379.46
Percent Composition: C 66.47%, H 6.64%, N 18.46%, O 8.43%
Literature References: Bisheteroarylpiperazine (BHAP) reverse transcriptase inhibitor. Prepn: D. L. Romero et al., WO 9109849 (1991 to Upjohn); and structure-activity studies: idem et al., J. Med. Chem. 37, 999 (1994). Mechanism of action study: I. W. Althaus et al., J. Biol. Chem. 268, 6119 (1993). Clinical pharmacokinetics: A. M. M. Been-Tiktak et al., Antimicrob. Agents Chemother. 39, 602 (1995). Clinical evaluation of combination with zidovudine in AIDS: R. C. Reichman et al., J. Infect. Dis. 171, 297 (1995). Clinical trial in HIV: A. M. M. Been-Tiktak et al., Antimicrob. Agents Chemother. 40, 2664 (1996).
Properties: mp 153-154°.
Melting point: mp 153-154°
Derivative Type: Methanesulfonate
CAS Registry Number: 138540-32-6
Additional Names: Atevirdine mesylate
Manufacturers' Codes: U-87201E
Molecular Formula: C21H25N5O2.CH3SO3H
Molecular Weight: 475.56
Percent Composition: C 55.56%, H 6.15%, N 14.73%, O 16.82%, S 6.74%
Properties: Crystals from diethyl ether, mp 215-216°.
Melting point: mp 215-216°
Therap-Cat: Antiviral.
Keywords: Antiviral; Reverse Transcriptase Inhibitor.
Status: This monograph has been retired and is no longer subject to revision or update.

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