- Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs
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A series of compounds containing one or two salicylic acid moieties were synthesized, and their efficacy to inhibit the phosphohydrolase activity of PTP1B examined. Some of the methylenedisalicylic acid derivatives were potent inhibitors of PTP1B. Of those derivatives, 3c exhibited about a 14-fold selectivity against TC-PTP, and this compound was tested in a mouse model for its efficacy to prevent diet-induced obesity. It effectively suppressed the increases in body weight and adipose mass, without any noticeable toxic effect. The compound also prevented increases in the plasma triglyceride, cholesterol, and nonesterified fatty acid concentrations; thus, expanding its therapeutic potential to other related metabolic diseases, such as hyperlipidemia and hypercholesterolemia.
- Shrestha, Suja,Bhattarai, Bharat Raj,Lee, Keun-Hyeung,Cho, Hyeongjin
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p. 6535 - 6548
(2008/04/12)
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- Synthesis and biological evaluation of certain alkenyldiarylmethanes as anti-HIV-1 agents which act as non-nucleoside reverse transcriptase inhibitors
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Several novel alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors were synthesized. The most potent of these proved to be 3',3'-dibromo-4',4'-dimethoxy-5',5'-bis(methoxycarbonyl)-1,1-diphenyl-1- heptene (8). ADAM 8 inhibited
- Cushman, Mark,Golebiewski, W. Marek,Graham, Lisa,Turpin, Jim A.,Rice, William G.,Fliakas-Boltz, Valerie,Buckheit Jr., Robert W.
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p. 3217 - 3227
(2007/10/03)
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- Synthesis and Anti-HIV Activities of Low Molecular Weight Aurintricarboxylic Acid Fragments and Related Compounds
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Several compounds corresponding to fragments of the schematic representation of the polymeric structure of aurintricarboxylic acid (ATA) have been prepared and tested for prevention of the cytopathic effect of HIV-1 and HIV-2 in MT-4 cell culture and HIV-
- Cushman, Mark,Kanamathareddy, Suseela,Clerq, Erik de,Schols, Dominique,Goldman, Mark E.,Bowen, Julie A.
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p. 337 - 342
(2007/10/02)
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- The Synthesis of 4,11,18,25-Tetrachloro4>metacyclophane-7,14,21,28-tetrol. Structural Analogues of Phloroglucides
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The synthesis of the title compounds is described.Some of the compounds prepared exhibited antimicrobial activity in vitro.Structure-activity relationship is briefly discussed.
- Moshfegh, Ali A.,Badri, Rashid,Hojjatie, Massoud,Kaviani, Mehrangiz,Naderi, Basirat,et al.
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p. 1221 - 1228
(2007/10/02)
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