ResumenIntroducciónEl cidofovir es un antiviral que inhibe la ADN-polimerasa de diferentes virus. Ha sido utilizado en infecciones originadas por el virus del papiloma humano.

The Orthopoxvirus (OPV) genus of the Poxviridae family contains several human pathogens, including Vaccinia virus (VACV), which have been implicating in outbreaks of a zoonotic disease called Bovine Vaccinia in Brazil. So far, no approved treatment exists for OPV infections, but ST-246 and Cidof...

Parvovirus B19 (B19V) is a human ssDNA virus responsible for a wide range of clinical manifestations, still lacking for a specific antiviral therapy. The identification of compounds active against B19V may add therapeutic options to the treatment of B19V infections, that now entirely relies on s...

ObjectiveThe treatment of recurrent respiratory papillomatosis (RRP) continues to be difficult. Adjuvant pharmacological treatment is increasingly being used, and intralesional cidofovir injection remains the leading option. Almost all papers regarding the treatment come from the United States a...

Condylomata acuminata (CA) or anogenital warts are benign proliferative lesions caused by low-risk human papillomaviruses (HPV). Treating CA can be very frustrating for patients and clinicians due to the high recurrence rates. Immunosuppression is associated with larger size of CA that are more ...

BK virus–associated hemorrhagic cystitis (BK-HC) is a common complication after allogeneic hematopoietic stem cell transplantation (allo-HCT), with incidences up to 70%. Cidofovir is an antiviral agent with growing evidence as a therapeutic intervention. To assess the safety profile and efficac...

Cidofovir is primarily indicated for the treatment of cytomegalovirus (CMV) retinitis in patients with AIDS, and in the treatment of acyclovir-resistant mucocutaneous herpes simplex virus (HSV) infections in immunocompromised patients and in transplant recipients. Cidofovir selectively inhibits ...

Most adenovirus infections are self-limiting in immunocompetent individuals. Here, we report a case of adenovirus pneumonia in a 17-year-old immunocompetent male. He was admitted to our emergency room complaining of a febrile sense, cough, and diarrhea for four days. Crackles in the left lung an...

Acyclic nucleotide analogues 9-(2-phosphonomethoxyethyl)adenine (PMEA) and 9-(S)-(3-hydroxy-2-phosphonomethoxypropyl) adenine ((S)-HPMPA) which display potent antiviral activity are transformed in the cells to their mono- and disphosphoryl derivatives. We purified from mouse L1210 cells the enzy...

A FeCl3-catalyzed multicomponent reaction was developed for the facile synthesis of coumarin-3-carboxylic ester derivatives in a highly atom-economic and environmentally friendly way. Using simple and cheaply available salicylaldehydes, Meldrum's acid and alcohols as the starting materials,...

The highly enantioselective kinetic resolution of a racemic primary alcohol by lipase-catalyzed transesterification with vinyl 3-(4-trifluoromethylphenyl)propanoate afforded an enantiomerically pure primary alcohol. The versatility of this approach is shown in the asymmetric synthesis of 5,6-deh...

Based on reaction of (+)- or (-)-dimenthyl phosphite with trifluoroacetonitrile the synthesis of optically active O,O-dimenthyl α-iminotrifluoroethylphosphonates was developed. The synthetic potential of these novel chiral synthons was demonstrated by their easy diastereoselective functionaliza...

The ontogenesis of vasopressin receptors in the rat collecting duct was studied by measuring the binding of [1-(β-mercapto-β, β-cyclopentamethylenepropionic acid), 2-O-methyltyrosine, 4-threonine, 8-ornithine, 9-125I-tyrosylamide]-vasotocin (125I-d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH92]-OVT) to isolat...

High-performance liquid chromatography and microchemical reactions identified 5α-pregnane-3β,7α,17,20β- and -20α-tetrols as final metabolic products from ovaries of the common carp, Cyprinus carpio, incubated with progesterone and 17-hydroxyprogesterone.

The design, synthesis and structure–activity relationships of a novel series of 3,4-disubstituted pyrrolidine acid analogs as PPAR ligands is outlined. In both the 1,3- and 1,4-oxybenzyl pyrrolidine acid series, the preferred stereochemistry was shown to be the cis-3R,4S isomer, as exemplified ...

A new method for synthesis of trifluoromethylated and pyrrolidinedione-fused pyrrolidines is developed through a three-component and decarboxylative [3 + 2] cycloaddition of non-stabilized N-unsubstituted azomethine ylides with commercially available trifluoroacetophenones. This efficient and ec...

Highly effective and safe drugs for the treatment of neuropathic pain are urgently required and it was shown that blocking T-type calcium channels can be a promising strategy for drug development for neuropathic pain. We have developed pyrrolidine-based T-type calcium channel inhibitors by struc...

Twenty-two new 1-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]pyrrolidine-2,5-diones were synthesized and tested for anticonvulsant activity. Initial anticonvulsant screening was performed using standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens in mice. Several co...

In the present study, on the development of new anticonvulsants, the series of N-[(4-arylpiperazin-1-yl)-alkyl]-3-(2-methylphenyl)- (8a–e, 10a–h) and 3-(2-trifluoromethyl-phenyl)-pyrrolidine-2,5-diones (9a–e, 11a–i) were synthesized and tested for anticonvulsant activity using the maximal el...

Ketones and imines bearing a 2-(trifluoromethyl)allylic moiety successfully underwent nucleophilic 5-endo-trig cyclization via their metal enolates and enamides. O- or N-Cyclization proceeded exclusively in each case to afford the corresponding five-membered heterocycles with both exo-difluorome...