Bio-orthogonal chemistry has been widely used for conjugation of polymer molecules to proteins. Here, we demonstrate the conjugation of polyethylene glycol (PEG) to bovine beta-lactoglobulin (BLG) by photo-induced cyclo-addition of tetrazole-appended PEG and allyl-modified BLG. During the course of the investigation, a significant side-reaction was found to occur for the conjugation of PEG-tetr...

Rationale. The goal of antihypertensive treatment is to reduce risk of cardiovascular morbidity and mortality. Apart from blood pressure lowering per se, also reducing the activities of the renin-angiotensin system and sympathetic nervous system appears to be important. Angiotensin II receptor blocker drugs (ARBs) have provided a useful class of anti-hypertensive drugs. Eprosartan is a relative...

Peroxisome proliferators-activated receptors (PPARα, γ and δ) are potentially effective targets for Type 2 diabetes mellitus therapy. The severe effects of known glitazones and the successfully approved agents (saroglitazar and lobeglitazone) motivated us to study novelly potent PPARs drugs with improved safety profile. In this work, we received 15 carboxylic acids based on the combination prin...

Treatments of tetrazolate salts prepared in situ from various aldehyde; malononitrile and sodium azide in the presence of NiO nanoparticles with benzyl bromide gave the corresponding 1,5- and 2,‌5-disubstituted tetrazoles. Reaction of tetrazolate salts with 2,4′-dibromoacetophenone in the presence of NiO nanoparticles provided the corresponding 2,5-disubstituted derivatives as an only isomer. T...

In the present work, we have planned a new magnetically recoverable nanocatalyst. The obtained nanocatalyst designated as Fe3O4@SiO2@DOPisatin-Ni (II) was characterized by FTIR, XRD, SEM, EDAX, VSM, AAS and TGA techniques. It was found that Fe3O4@SiO2@DOPisatin-Ni (II) successfully catalyses the synthesis of 2,3-dihydroquinazolin-4(1H)-ones, polyhydroquinoline and 5-substituted 1H-tetrazoles in...

2 The present work deals with the synthesis of some novel heterocyclic compounds such as benzoxazoles , 7, 13 and 19, imidazoles 3, 8, 14 and 20, benzimidazoles 4, 9, 15 and 21, and tetrazoles 10, 16, and 22. The synthesized compounds were characterized by IR, 1H NMR, mass spectrometry and elemental analysis. The compounds were evaluated for cytotoxicity against human cancer cell lines such as ...

En este trabajo se realizó el diseño in silico de 17 moléculas basadas en la estructura una quinolona, las que evaluó efecto triazoles, tetrazoles e isatinas como grupos funcionales a través del aumento concentración mínima inhibitoria (MIC, por sus siglas inglés) calculado mediante un estudio relación cuantitativa estructura-actividad (QSAR, haciendo comparativa con MIC experimental quinolonas...