Search Results - "GROZINGER, K. G"

Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones by Skiles, Jerry W, Fuchs, Victor, Miao, Clara, Sorcek, Ronald, Grozinger, Karl G, Mauldin, Scott C, Vitous, Jana, Mui, Philip W, Jacober, Stephen

“…A series of tripeptides possessing trifluoromethyl or aryl ketone residues at P1 were prepared and evaluated both in vitro and in vivo as potential inhibitors…”
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Synthesis of nevirapine and its major metabolite by Grozinger, K. G., Fuchs, V., Hargrave, K. D., Mauldin, S., Vitous, J., Campbell, S., Adams, J.

“…Several synthetic methods were developed during the process optimization for the large scale synthesis of nevirapine (1), a non‐nucleoside inhibitor of HIV‐1…”
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Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones by Hargrave, Karl D, Proudfoot, John R, Grozinger, Karl G, Cullen, Ernest, Kapadia, Suresh R, Patel, Usha R, Fuchs, Victor U, Mauldin, Scott C, Vitous, Jana

“…Novel pyrido[2,3-b][1,4]benzodiazepinones (I), pyrido[2,3-b][1,5]benzodiazepinones (II), and dipyrido[3,2-b:2',3'-e][1,4]diazepinones (III) were found to…”
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Novel Non-nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones as Potent Inhibitors of Both Wild-Type and Cysteine-181 HIV-1 Reverse Transcriptase Enzymes by Proudfoot, John R, Hargrave, Karl D, Kapadia, Suresh R, Patel, Usha R, Grozinger, Karl G, McNeil, Daniel W, Cullen, Ernest, Cardozo, Mario, Tong, Liang

“…The major cause of viral resistance to the potent human immunodeficiency virus type 1 reverse transcriptase (RT) inhibitor nevirapine is the mutation…”
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Amidomethylation of phenanthridines: Synthesis and structure determination by 1H NMR by Freter, K. R., Grözinger, K. G., Kriwacki, R. W.

“…Phenanthridine reacts with N‐(hydroxymethyl)phthalimide to give, in two steps, three monosubstituted aminomethylphenanthridines. The three isomers were…”
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A novel stereoselective route to (S)-(+)-α-(fluromethyl)histidine : α-halomethylation of (2R,4S)-3-benzoyl-2-(1,1-dimethylethyl)-1-methyl-4-[(N-tritylimidazol-4'-yl)methyl]-1,3-imidazolidin-5-one. Synthesis and 1H NMR spectroscopy by GROZINGER, K. G, KRIWACKI, R. W, LEONARD, S. F, PITNER, T. P

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Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. IV: 2-substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes by PROUDFOOT, J. R, HARGRAVE, K. D, ROSE, J, DAVID, E, MAULDIN, S. C, FUCHS, V. U, VITOUS, J, HOERMANN, M, KLUNDER, J. M, PALAYAKOTAI RAGHAVAN, SKILES, J. W, MUI, P, KAPADIA, S. R, RICHMAN, D. D, SULLIVAN, J. L, CHENG-KON SHIH, GROB, P. M, ADAMS, J, PATEL, U. R, GROZINGER, K. G, MCNEIL, D. W, CULLEN, E, CARDOZO, M, LIANG TONG, KELLY, T. A

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Syntheses and reactions of some 1-substituted-7-alkyl-2-thioxopurines: X-Ray structure of 6-methylamino-7-nonyl-2-thioxopurine by Grözinger, Karl G., Onan, Kay D.

“…Several 1‐substituted‐7‐alkyl‐2‐thioxopurines 8,9,10 were synthesized by the reaction of isothiocyanates with 1‐alkyl‐4‐amino‐5‐cyanoimidazoles 3. Treatment of…”
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Synthesis of five nevirapine metabolites by Grozinger, Karl G., Byrne, Denis P., Nummy, Laurence J., Ridges, Michael D., Salvagno, Annette

“…Nevirapine (1) is a non‐nucleoside reverse transcriptase inhibitor marketed for HIV treatment by Boehringer Ingelheim as Viramune® since 1996. In vitro studies…”
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Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. I, Tricyclic pyridobenzo- and dipyridodiazepinones by HARGRAVE, K. D, PROUDFOOT, J. R, KLUNDER, J. M, PAL, K, SKILES, J. W, MCNEIL, D. W, ROSE, J. M, CHOW, G. C, SKOOG, M. T, WU, J. C, SCHMIDT, G, ENGEL, W. W, GROZINGER, K. G, CULLEN, E, KAPADIA, S. R, PATEL, U. R, FUCHS, V. U, MAULDIN, S. C, VITOUS, J, BEHNKE, M. L

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Amidomethylation of phenanthridines: Synthesis and structure determination by 1 H NMR by Freter, K. R., Grözinger, K. G., Kriwacki, R. W.

“…Phenanthridine reacts with N ‐(hydroxymethyl)phthalimide to give, in two steps, three monosubstituted aminomethylphenanthridines. The three isomers were…”
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Synthesis of imidazo[5,4-d] [1,3]thiazines: X-ray structure of N-methyl-N′-[5-(methylamino)-3-nonylimidazo[5,4-d] [1,3]thiazin-7(3H)-ylidene]thiourea by Grözinger, Karl G., Onan, Kay D.

“…N‐Alkyl‐N′‐[5‐(alkylamino)‐3‐alkylimidazo[5,4‐d] [1,3]thiazin‐7(3H)‐ylidene]thioureas were obtained by the reaction of 1‐substituted 5‐amino‐4‐cyanoimidazoles…”
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