Synthesis, characterization and biological screening of 5-substituted-1,3,4-oxadiazole-2yl-N-[2-methoxy-5-chlorophenyl]-2-sulfanyl acetamide

In the current study, a series of 5-substituted-1,3,4-oxadiazole-2yl-N-[2-methoxy-5-chlorophenyl]-2-sulfanyl acetamide was synthesized by converting variously substituted/unsubstituted aromatic organic acids successively into the corresponding esters, hydrazides and then 5-substituted-1,3,4-oxadiazole-2-thiols. Finally the target compounds were obtained by stirring 5-substituted-1,3,4-oxadiazole-2-thiols with N-[2-methoxy-5-chlorophenyl]-2-bromoacetamide in the presence of N,N-dimethyl formamide [DMF] and sodium hydride [NaH]. The structures of the synthesized compounds were confirmed based on [1]H-NMR, IR and mass spectral data. The synthesized compounds were screened against acetylcholinesterase [AChE], butyrylcholinesterase [BChE] and lipoxygenase enzymes [LOX] and were found to be relatively more active against acetyl cholinesterase

Synthesis, characterization and biological screening of N-substituted derivatives of 5-benzyl-1,3,4-oxadiazole-2yl-2''-sulfanyl acetamide

A series of new N-substituted derivatives of 5-benzyl-1, 3, 4-oxadiazole-2yl-2''-sulfanyl acetamide [6a-n] were synthesized in three phases. The first phase involved the sequentially converting phenyl acetic acid into ester, hydrazide and finally cyclized in the presence of CS[2] to afford 5-benzyl-1, 3, 4-oxadiazole-2-thiol. In the second phase N-substituted-2-bromoacetamides were prepared by reacting substituted amines with bromoacetyl bromide in basic media. In the third phase, 5-benzyl-1,3,4-oxadiazole-2-thiol was stirred with N-substituted-2-bromoacetamides in the presence of N,N-dimethyl formamide [DMF] and sodium hydride [NaH] to get the target compounds. Spectral techniques were used to confirm the structures of synthesized compounds. Synthesized compounds were screened against butyrylcho linesterase [BChE], acetylcholinesterase [AChE], and lipoxygenase enzymes [LOX] and were found to be relatively more active against acetylcholinesterase

Muscle activity of mandibular unilateral distal extension RPDS wearers with two direct retainers

The aim of the present study was to evaluate and investigate the activity of masticatory muscles [Masseter and Anterior fibers of Temporalis] in ten male patients wearing mandibular distal extension removable partial denture with two different direct retainers. They were divided into two groups RPT clasp assembly was used for group I and combination clasp assembly [Modified T or half T buccally and half Akers lingually] for group II Computerized Electromyography [Cad Wel Excel high power EMG/EP instrument U.S.A.] recorded the activity of Masseter and Temporalis muscles during maximum clenching before denture insertion and six times after insertion with an interval of one month each. Results showed a jaw jerk reflex was recorded in all patients wearing RPD with RPI clasp in the second month of follow up, which was not recorded with the group II jaw jerk reflex is typical a reaction of periodontal receptor with orthodontic movement which occur when load is not regular. In the second month a significance in Mean Voltage Amplitude, Root Mean Square RMS] and Power at [P-value <0.001] was found There was a significant difference in the muscle activity between the two types of retainers used for this study. It could be concluded that EMG instrument can be used as a diagnostic aid to record and detect a jaw jerk reflex with different types of prostheses and to select the proper direct retainer for RPD. Combination clasp assembly is superior to RPI assembly as direct retainer for unilateral distal tension RPD