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Twelve new 3-(isobutyl)-5-substituted-tetrahydro-2H-1,3,5-thiadiaz-ine-2-thiones were synthesized... more Twelve new 3-(isobutyl)-5-substituted-tetrahydro-2H-1,3,5-thiadiaz-ine-2-thiones were synthesized by the reaction of isobutylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and appropriate alkyl, cycloalkyl aralkyl amines, amino acid, and INH. Their structures have been elucidated by spectral data and elemental analysis. The title compounds were tested for antimicrobial activity in vitro against gram-positive bacteria (Staphylococcus aureus,and Micrococcus leuteus), gram-negative bacteria (Serratia marcescens and Escherichia coli) and some fungi (Candida albicans, Scopulariopsis brevicalus, Geotrichum candidum, Macrophomina phaseolina, Fusarium oxysporum and Trichoderma harzianum) using agar cup diffusion method. The antimicrobial activity was found to be greatly affected by the bulkiness of the side chain and the presence of polar carboxylic group. Highest activity was obtained with compounds 4a and 4k (R= CH 3 , CH 2 -COOH).

Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3- a]benzimidazol-2... more Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3-
a]benzimidazol-2-ylsulfanyl) acetohydrazides (4a-k), N`-(α-arylethylidene)-2-(1H-1,2,4-
triazolo[2,3-a]benzimidazol-2-ylsulfanyl) acetohydrazides (5a-d), and 2-({[5-(alkyl or
aralkylsulfanyl)-1,3,4-oxadiazol-2-yl]methyl}sulfanyl)-1H-1,2,4-triazolo[2,3-a]benzimidazoles
(7a-e) were synthesized. Reaction of compound (1) with methyl bromoacetate afforded (2),
which when refluxed with hydrazine hydrate yielded (3). The latter was condensed with
aromatic aldehydes and substituted acetophenones to afford compounds (4a-k) and (5a-d)
respectively. Treatment of compound (3) with carbon disulfide in the presence of potassium
hydroxide resulted in the formation of (6). The latter was alkylated with the appropriate alkyl
or aralkyl halides to afford compounds (7a-e). The purity of all new compounds was checked by
TLC and elucidation of their structures was confirmed by IR,
1
HNMR, and mass spectrometry
along with elemental microanalyses. All the target compounds were evaluated for their in-vitro
antimicrobial and in-vivo anti-inflammatory activities in comparison with ampicillin,
fluconazole, and indomethacin as reference drugs respectively. In addition to molecular
docking of compound 5c was performed.

The present work describes the synthesis and evaluation of some new acetohydrazones, 1,3,4-oxadia... more The present work describes the synthesis and evaluation of some new acetohydrazones, 1,3,4-oxadiazoles and 1,2,4-triazoles of 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflamm atory-analgesic agents. Structure elucidation of these compounds was confirmed by IR, 1 H NMR, and mass spectrometry along with elemental microanalyses. Most compounds exhibited significant anti-inflammatory activity in comparison to indomethacin. Further, some compounds were tested for their analgesic effects where two compounds showed results comparable to indomethacin at 4 h interval. The most active anti-inflammatory and analgesic compounds (4c and 11a) were examined on gastric mucosa and didn't show any gastric ulcerogenic effect compared with the reference indomethacin. Moreover, LD 50 of compounds (4c and 11a) were determined in mice; they were found non toxic up to 240 and 300 mg/kg (i.p.). Also, docking simulation of some compounds into COX active sites was studied.