Various novel barbituric and thiobarbituric acid derived sulphonamides were synthesized in excellent yield via three components single pot reaction; and these were screened for in vitro urease inhibition studies against jack bean urease. The compounds 1‐7 were found to exhibit a low to moderate activity whereas compounds 8‐14 showed a significant activity (88.3‐99.9% inhibition determined at 500 μM concentration). Structures of the synthesized compounds were confirmed by 1H‐NMR, 13C‐NMR, mass spectrometry and elemental analysis data.

No abstract

The reactivity of benzyl hypervalent iodine intermediates was explored in congruence with the reductive iodonio-Claisen rearrangement (RICR) to show that there may be an underlying mechanism which expands the reasoning behind the previously known C–C bond-forming reaction. By rationalizing the hypervalent iodine’s metal-like properties it was concluded that a transmetallation mechanism could be occurring with metalloid groups such as silicon and boron. Hypervalent iodine reagents such as Zefirov’s reagent, cyclic iodonium reagents, iodosobenzene/BF3, and PhI(OAc)2/BF3 or triflate-based activators were tested. A desirable facet of the reported reaction is that iodine(I) is incorporated into the product thus providing greater atom economy and a valuable functional group handle for further transformations. The altering of the RICR’s ortho-selectivity to form para-selective products with benzyl hypervalent iodine intermediates suggests a mechanism that involves hypervalent iodine-guided electrophilic substitution (HIGES).

Purpose: To design and synthesize a series of new structural motifs of urease inhibitors, 3-[{(substituted phenyl) amino} methyl]-5-(3, 4, 5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones and 3-{[(pyridin-2-yl)amino]methyl}- 5-(3,4,5-trimethoxy phenyl)-1,3,4-oxadiazole-2(3H) 4,5,9,10,12,13, values in the range of 5. 93 ± 0.13 to 9.76 ± 0.11,

Naphthamides have pharmacological potential as they express strong activities against microorganisms. The commercially available naphthoyl chloride and 4-bromoaniline were condensed in dry dichloromethane (DCM) in the presence of Et 3 N to form N-(4-bromophenyl)-1-naphthamide (86%) (3). Using a Pd(0) catalyzed Suzuki-Miyaura Cross-Coupling reaction of (3) and various boronic acids, a series of N-([1,1ʹ-biaryl]-4-yl)-1-naphthamide derivatives (4a-h) were synthesized in moderate to good yields. The synthesized derivatives were evaluated for cytotoxicity haemolytic assay and biofilm inhibition activity through in silico and in vitro studies. Molecular docking, ADME (absorption, distribution, metabolism, and excretion), toxicity risk, and other cheminformatics predict synthesized molecules as biologically active moieties, further validated through in vitro studies in which compounds (4c) and (4f) showed significant haemolytic activity whereas (4e) exhibited an efficient biofilm inhibition activity against Gram-negative bacteria Escherichia coli and Gram-positive bacteria Bacillus subtilis. When forming biofilms, bacteria become resistant to various antimicrobial treatments. Currently, research is focused on the development of agents that inhibit biofilm formation, thus the present work is valuable for preventing future drug resistance.

No abstract

In elementary chemistry courses students often demonstrate difficulty with real understanding of Resonance Theory i.e. canonical structure vs. real molecule difference, so unanswered puerile questions during lecture made the subject boring. Particularly students unable to understand the difference between a real microscopic moiety and it's proposed sketch or model at early stages of their learning. In such situations use of suitable analogy in front of students other than the subject area make the teaching more effective. Observation through five senses act as a powerful tool to explain curious questions efficiently to develop the interest of the students in subject. Sharing of personal experiences and analogies among scientific community is an effective way to spread scientific knowledge magnificently.

Confusions about basic concepts are common among number of students during early stages of education in any field, which later on reduced as they got more advance knowledge about their subject. This study is focused on the most important basic concept of chemistry i.e. Resonance phenomena to explain the benzene molecule structure and its canonical forms. Enormous literature available on this topic; however, still chemistry students find difficult to understand the difference between a real molecular moiety and it’s proposed sketch or model at early stages of their learning. To solve this issue macro entity and its sketches analogy used in front of students and found it more effective. A tough or difficult topic during class lecture can be simplified by using a suitable analogy with minimal resources.