排序方式: 共有33条查询结果,搜索用时 15 毫秒
21.
P. Franchetti L. Cappellacci G. Abu Sheikha M. Grifantini A. G. Loi A. De Montis 《Nucleosides, nucleotides & nucleic acids》2013,32(3-5):607-610
Abstract The syntheses and antiviral activity of analogues of the anti-HIV agents PMEA, PMEDAP, (R)-PMPA, (R)-PMPDAP are described. In these analogues the adenine moiety is replaced by 4,6-diamino-5-nitro-pyrimidine (the aglycon of clitocine) or 2,4,6-triamino-5-nitro-pyrimidine. The synthesis of similar acyclic phosphonates related to PMEG and (R)-2′-methyl-PMEG is also reported. Some compounds proved to be active as anti-HIV agents. 相似文献
22.
Palmarisa Franchetti Ghassan Abu Sheikha Paolo Perlini Farhat Farhat Mario Grifantini Graziella Perra 《Nucleosides, nucleotides & nucleic acids》2013,32(10-11):1921-1932
Abstract The synthesis of 9-[2-(phosphonomethoxy)allyl]guanine (1) and 9-[2-(phosphonomethoxy)allyl]-8-aza-guanine (2), two new unsaturated acyclic phosphonate nucleosides analogues of the anti-HIV agents PMPG and 8-aza-PMPG, is described. Compounds 1 and 2 were evaluated for activity against human immunodeficiency virus (HIV-1 and HIV-2) and herpes simplex virus (HSV-1 and HSV-2). 相似文献
23.
P. Franchetti L. Messini L. Cappellacci G. Abu Sheikha M. Grifantini P. Guarracino 《Nucleosides, nucleotides & nucleic acids》2013,32(8):1739-1755
Abstract 2′,3′-Dideoxy-8-aza-1-deazaadenosine (21) and its α-anomer (20) were synthesized via glycosylation of 7-chloro-3H-1,2,3-triazolo[4,5-b]pyridi-ne with 2,3-dideoxy-5-O-[(1, 1)-dimethylethyl)diphenylsilyl]-D-glycero-o-pen-tofuranosyl chloride. The reaction gave a mixture of α- and β-anomers of N3-, N4- and N1-glycosylated regioisorners (12–15). The α- and β-anomers of the N4-glycosylated isomer 26 and 27 were also synthesized through the glycosylation of 8-aza-1-deazaadenine with 1-acetoxy-2,3-dideoxy-5-O-f(1,1-di-methylethyl)dimethylsilyl]-D-glycero-pentouranose. These dideoxynucleo-sides and a series of previously synthesized 8-aza-1-deazapurine nucleosidcs were tested for activity against several DNA and RNA viruses, HIV-1 included. The α- and β-anomers of 7-chloro-3-(2-deoxy-D-erythro-pentofuranosyl)-3H-1,2,3-triazolo[4,5-b]pyridine (3a and 4) showed activities against Sb-1 and Coxs viruses. The α- and β-anomers of 2′,3′-dideoxy-8-aza-1-deazaadenosine (20 and 21) were found active as inhibitors of adenosine deaminase. 相似文献
24.
Franchetti P Marchetti S Cappellacci L Yalowitz JA Jayaram HN Goldstein BM Grifantini M 《Bioorganic & medicinal chemistry letters》2001,11(1):67-69
2-Beta-D-ribofuranosylimidazole-4-carboxamide, an imidazole analogue of the antitumor agent tiazofurin, was synthesized and evaluated for the growth inhibitory activity of human myelogenous leukemia K562 cells. 相似文献
25.
Franchetti P Pasqualini M Petrelli R Ricciutelli M Vita P Cappellacci L 《Bioorganic & medicinal chemistry letters》2004,14(18):4655-4658
The beta-anomers of N-ribofuranosylnicotine-3-carboxamide (beta-NAR) and its nicotinic acid analog (beta-NaR) were obtained by stereoselective synthesis via glycosylation of the presilylated bases under Vorbruggen's protocol. A NAR analog, methylated in position 3 of the ribosylic moiety, is also reported. 相似文献
26.
Sorci L Cimadamore F Scotti S Petrelli R Cappellacci L Franchetti P Orsomando G Magni G 《Biochemistry》2007,46(16):4912-4922
Initial-rate and product inhibition studies revealed distinctive ordered ternary complex kinetic mechanisms, substrate specificities, and metal ion preferences for the three isozymes of human nicotinamide mononucleotide adenylyl-transferase (NMNAT, EC 2.7.7.1). ATP binds before NMN with nuclear isozyme NMNAT1 and Golgi apparatus NMNAT2, but the opposite order is observed with the mitochondrial isozyme NMNAT3. Only the latter utilizes ITP efficiently in place of ATP, and while NMNH conversion to NADH by NMNAT1 and NMNAT3 occurs at similar rates, conversion by NMNAT2 is much slower. These isozymes can also be discriminated by their action on tiazofurin monophosphate (TrMP), a metabolite of the antineoplastic prodrug tiazofurin. Our finding that TrMP is only a substrate with NMNAT1 and NMNAT3 reveals for the first time an organelle selectivity in the metabolism of this important drug. In search of additional ways to discriminate these isozymes, we synthesized and tested the P1-(nicotinamide/nicotinate-riboside-5')-Pn-(adenosine-5') dinucleotides Np3AD, Np4AD, and Nap4AD. In addition to being highly effective inhibitors, these multisubstrate geometric inhibitors gave inhibition patterns that are consistent with the aforementioned isozyme differences in substrate binding order. Distinctive differences in their substrate specificity and metal ion selectivity also permitted us to quantify individual isozyme contributions to NAD+ formation in human cell extracts. 相似文献
27.
Palmarisa Franchetti Ghassan Abu Sheikha Loredana Cappellacci Mario Grifantini Emanuela Balestra Carlo-Federico Perno 《Nucleosides, nucleotides & nucleic acids》2013,32(4-5):989-990
Abstract A new antiviral drug with both anti-HSV and anti-HIV activity was synthesized by coupling Acyclovir and the acyclic nucleoside phosphonate (R)PMPA. The heterodinucleotide ACVpPMPA encapsulated into autologous erythrocytes was added to human macrophages providing an effective in vitro protection from HSV-1 and HIV-1 replication. 相似文献
28.
G. Abu Sheika E. Tramontano A. G. Loi P. Franchetti M. Grifantini P. La Colla 《Nucleosides, nucleotides & nucleic acids》2013,32(4-5):849-851
Abstract Integrase (IN) is an essential enzyme in the human immunodeficiency virus type-1 (HIV-1) replication cycle and, thus, a potential target for chemotherapeutic agents. Because various nucleotide analogues have been reported to inhibit IN in vitro, we investigated the effect of acyclic nucleoside phosphonates. Both unphosphorylated and diphosphorylated derivatives were inhibitory to IN at concentrations ranging between 60 and 800 μM, with diphosphorylated derivatives being 5- to 8-fold more potent than unphosphorylated counterparts. 相似文献
29.
Cappellacci L Franchetti P Vita P Petrelli R Grifantini M 《Nucleosides, nucleotides & nucleic acids》2008,27(5):460-468
A heterodinucleotide comprising BVDU and Gemcitabine bound together by a 5',5'-pyrophospate bridge (BVDUp(2)dFdC) has been synthesized and evaluated as antitumor agent against AH13 rat sarcoma cells. BVDUp(2)dFdC showed a cytotoxicity similar to that of Gemcitabine. 相似文献
30.
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists
Ko H Carter RL Cosyn L Petrelli R de Castro S Besada P Zhou Y Cappellacci L Franchetti P Grifantini M Van Calenbergh S Harden TK Jacobson KA 《Bioorganic & medicinal chemistry》2008,16(12):6319-6332
The phosphate, uracil, and ribose moieties of uracil nucleotides were varied structurally for evaluation of agonist activity at the human P2Y(2), P2Y(4), and P2Y(6) receptors. The 2-thio modification, found previously to enhance P2Y(2) receptor potency, could be combined with other favorable modifications to produce novel molecules that exhibit high potencies and receptor selectivities. Phosphonomethylene bridges introduced for stability in analogues of UDP, UTP, and uracil dinucleotides markedly reduced potency. Truncation of dinucleotide agonists of the P2Y(2) receptor, in the form of Up(4)-sugars, indicated that a terminal uracil ring is not essential for moderate potency at this receptor and that specific SAR patterns are observed at this distal end of the molecule. Key compounds reported in this study include 9, alpha,beta-methylene-UDP, a P2Y(6) receptor agonist; 30, Up(4)-phenyl ester and 34, Up(4)-[1]glucose, selective P2Y(2) receptor agonists; dihalomethylene phosphonate analogues 16 and 41, selective P2Y(2) receptor agonists; 43, the 2-thio analogue of INS37217 (P(1)-(uridine-5')-P(4)-(2'-deoxycytidine-5')tetraphosphate), a potent and selective P2Y(2) receptor agonist. 相似文献