Design, synthesis and structure-activity relationships of novel non-ketolides: 9-Oxime clarithromycin featured with seven-to thirteen-atom-length diamine linkers at 3-OH.

We report here on the structure-activity relationships of hybrids combining 3-descladinosyl clarithromycin with quinolones linked by extended diamine connectors. Several hybrids, exemplified by 23Bc, 23Be, 23Bf, 26Be, and 30Bc, not only restored potency against inducibly resistant pathogens but also exhibited significantly enhanced activities against constitutively resistant strains of Staphylococcus pneumoniae and Staphylococcus pyogenes, which express high-level resistance independent of clarithromycin or erythromycin induction. Additionally, the novel hybrids showed susceptibility against Gram-negative Haemophilus influenzae.

Association between inflammatory bowel disease, nephrolithiasis, tubulointerstitial nephritis, and chronic kidney disease: A propensity score-matched analysis of US nationwide inpatient sample 2016-2018.

Objectives: The incidence and prevalence of inflammatory bowel disease (IBD), mainly including ulcerative colitis (UC) and Crohn's disease (CD), are increasing globally. We aimed to evaluate the potential association between IBD and nephrolithiasis, tubulointerstitial nephritis, and chronic kidney disease (CKD).

Methods: Data of hospitalized adults ≥20 years of age were extracted from the U.

The construction of a near-infrared fluorescent probe with dual advantages for imaging carbon monoxide in cells and .

As a kind of toxic gas, carbon monoxide (CO) can hinder uptake of oxygen in humans. However, more and more studies have shown that CO is an important gaseous messenger in the body and playing an indispensable role in intracellular signaling pathways. So, it is necessary to develop an analytical method to study CO in living organisms.

Synthesis and structure-bactericidal activity relationships of non-ketolides: 9-Oxime clarithromycin 11,12-cyclic carbonate featured with three-to eight-atom-length spacers at 3-OH.

In general, potent non-ketolide versions of erythromycin possessed conformationally constricted two- or three-atom-length sidechains at 3-OH. Novel 14-membered non-ketolides possessing long spacers beyond three-atom length were evaluated for antibacterial activity. The most potent one is 34a, featuring a five-atom-length flexible linker from of a pyridine ring to the aglycone.

Discovery of efficient stimulators for adult hippocampal neurogenesis based on scaffolds in dragon's blood.

Reduction of hippocampal neurogenesis caused by aging and neurological disorders would impair neural circuits and result in memory loss. A new lead compound (N-trans-3',4'-methylenedioxystilben-4-yl acetamide 27) has been discovered to efficiently stimulate adult rats' neurogenesis. In-depth structure-activity relationship studies proved the necessity of a stilbene scaffold that is absent in highly cytotoxic analogs such as chalcones and heteroaryl rings and inactive analogs such as diphenyl acetylene and diphenyl ethane, and validated the importance of an NH in the carboxamide and a methylenedioxy substituent on the benzene ring.

[Photosynthetic activity of Gloiopeltis furcata (intertidal red macroalga) in response to desiccation].

In this study, the diurnal change of photosynthesis activity in response to various tidal patterns, the relationship between photosynthetic activity and tissue water content, and the interactive effect of desiccation and irradiance on photosynthetic activity in Gloiopeltis furcata were investigated by using portable pulse amplitude modulated (PAM) fluorometer. Results showed that Fv/Fm decreased more rapidly during the noon low tide than during the morning- or evening low tide. F/Fm decreased slowly at the beginning of desiccation during the morning low tide, but decreased rapidly throughout the evening low tide.

[Spatiotemporal variation and related affecting factors of Gloiopeltis furcata biomass and length around Xiaoheishan Island, Shandong of China].

Gloiopeltis furcata, an important economic red macroalga, has been severely depleted due to human disturbances. Taking the natural G. furcata populations around the Xiaoheishan Island of Shandong, China as test objects, this paper studied the spatiotemporal variation pattern of their biomass and length and related affecting factors.