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This review article examines the synthetic pathways for triazolothiadiazine derivatives, such as triazolo[3,4-b]thiadiazines, triazolo[5,1-b]thiadiazines, and triazolo[4,3-c]thiadiazines, originating from triazole derivatives, thiadiazine derivatives, or thiocarbohydrazide. The triazolothiadiazine derivatives exhibit several biological actions, including antibacterial, anticancer, antiviral, antiproliferative, analgesic, anti-inflammatory, and antioxidant properties. The review article aims to assist researchers in creating new biologically active compounds for designing target-oriented triazolothiadiazine-based medicines to treat multifunctional disorders.

Abstract A novel series of substituted 4,6-dimethyl-2-oxo-1-(thiazol-2-ylamino)-1,2-dihydropyridine-3-carbonitrile derivatives 6, 9, 13, 15, and 17 was synthesized in a good to excellent yield from the reaction of 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)thiourea with 2-oxo-N'-arylpropanehydrazonoyl chloride, chloroacetone, α-bromoketones, ethyl chloroacetate, and 2,3-dichloroquinoxaline, respectively. The potential DNA gyrase inhibitory activity was examined using in silico molecular docking simulation. The novel thiazoles exhibit dock score values between − 6.4 and − 9.2 kcal/mol and they were screened for their antimicrobial activities. Compound 13a shown good antibacterial activities with MIC ranged from 93.7–46.9 μg/mL, in addition, it shown good antifungal activities with MIC ranged from 7.8 and 5.8 μg/mL.

The asymmetric unit of the title compound, C17H13N5O, comprises four independent molecules (A–D). The respective interplanar angles between the phenyl/oxadiazole/methyltriazole/phenyl rings for the four independent molecules are A 8.8 (2), 13.0 (2), 22.5 (2)°; B 6.3 (2), 8.9 (2), 29.0 (1)°; C 4.0 (2), 10.0 (2), 24.5 (2)°; D 3.5 (2), 10.1 (2), 27.2 (2)°. In the crystal, molecules form two separate stacks parallel to the b-axis direction: one consists of A and D molecules, and the other of B and C molecules. Aromatic π–π stacking is observed within each stack, with the shortest centroid–centroid separation being 3.552 (2) Å.

The title compound, C19H16N4O3, crystallizes with two molecules (A and B) in the asymmetric unit. In molecule A, the dihedral angles between the triazole ring and the toluyl and nitrobenzene rings are 62.68 (16) and 10.77 (15)°, respectively. The corresponding data for molecule B are 68.61 (17) and 15.59 (15)°, respectively. In the crystal, the B molecules are linked by C—H...N hydrogen bonds to generate [001] chains. Weak C—H...π(benzene) and N—O...π(triazole) contacts are also present.

In the title compound, C37H28Br2N8S, the dihedral angles between the planes of tolyl–triazolyl–pyrazolyl–phenyl rings are 47.5 (1), 11.4 (2) and 22.4 (2)°, respectively, and the angles between the bromophenyl–thiazolyl–dihydropyrazolyl–bromophenyl rings are 16.0 (2), 5.1 (2) and 0.8 (2)°, respectively. The dihedral angle between the planes of the pyrazolyl and dihydropyrazolyl rings is 67.7 (1)°. In the crystal, weak C—H...Br interactions form chains of molecules propagating in the [010] direction.

The asymmetric unit of the title compound, C20H18N8O2, comprises one complete molecule and a half molecule completed by crystallographic twofold symmetry leading to Z = 12. The dihedral angles between the planes of the linked phenyl and methyltriazolyl groups are 69.48 (5) and 44.85 (9)° for the first molecule and 42.88 (9)° for the second. The conformations of the diformyl hydrazyl groups of the molecules are similar as indicated by C—N—N—C torsion angles of −83.4 (2) and −86.4 (3)°. In the crystal, neighbouring molecules are linked by pairs of N—H...O hydrogen bonds to form independent columns propagating parallel to the c-axis direction.

The asymmetric unit of the title compound, C37H28BrClN8S, comprises one molecule. The molecule consists of two ring systems joined by a C—C bond between the dihydropyrazolyl and pyrazolyl rings of the two extended ring systems. The angles between adjacent ring planes of the tolyl–triazolyl–pyrazolyl–phenyl ring system are 48.2 (1), 12.3 (2) and 22.2 (2)°, respectively, with angles of 19.7 (1), 5.6 (2) and 0.9 (2)° between the rings of the chlorophenyl–thiazolyl–dihydropyrazolyl–bromophenyl set. The pyrazolyl and dihydropyrazolyl rings are inclined at 68.3 (1)° to one another. In the crystal, C—H...Cl interactions form chains of molecules parallel to the b-axis direction.

In the title compound, C24H22N4O2S, the dihedral angle between the triazole and thiophene rings is 4.83 (14)°. The dihedral angles between the triazole and tolyl rings and between the thiophene and phenyl rings are 48.42 (16) and 9.23 (13)°, respectively. An intramolecular N—H...O hydrogen bond closes an S(6) loop. In the crystal, molecules are stacked parallel to the a-axis direction with weak π–π interactions between adjacent thiophenyl and triazolyl groups within the stack [centroid–centroid separation = 3.9811 (16) Å].

In this study, the equation for the punching shear strength prescribed in the Canadian code is evaluated based on a database of experimental results. This paper also includes a discussion of the effect of several parameters on the punching shear strength in the Canadian and European codes. The experimental work presented includes testing of ten full-scale two-way slabs with different reinforcement ratios to examine the effect of reinforcement ratio on punching shear capacity. A simplified practical punching shear equation is also proposed based on statistical analysis of experimental results from the database. Statistical regression analysis is conducted on 190 test data available in the literature to evaluate the influence of reinforcement ratio on punching shear strength. The proposed equation accounts for the effect of slab depth using fracture mechanics concepts. The analytical study showed that the reinforcement ratio has a strong influence on punching shear strength. The proposed equation could be an alternative to the current punching shear equation used by Canadian Standards Association CSA-A23.3-04 design code. Key words: concrete strength, reinforcement ratio, size effect, database, statistical analysis, regression, ductility, punching. Dans la presente etude, l'equation de la resistance au cisaillement par poinconnement dans le code canadien est evaluee en se basant sur une base de donnees de resultats experimentaux. Cet article comprend egalement une discussion de l'effet des parametres sur la resistance au cisaillement par poinconnement dans les codes canadien et europeen. Le travail experimental presente comprend des essais sur 10 dalles bidirectionnelles a pleine echelle presentant differents pourcentages d'armature afin d'etudier l'effet du pourcentage d'armature sur la resistance au cisaillement par poinconnement. Une equation pratique et simplifiee du cisaillement par poinconnement est egalement proposee, basee sur une analyse statistique des resultats experimentaux de la base de donnees. Une analyse statistique de regression est realisee sur 190 donnees d'essai disponibles dans la litterature afin d'evaluer l'influence du pourcentage d'armature sur la resistance au cisaillement par poinconnement. L'equation proposee tient compte de l'effet de l'epaisseur de la dalle en utilisant les concepts de mecanique des fractures. L'etude analytique indique que le pourcentage d'armature a une forte influence sur la resistance au cisaillement par poinconnement. L'equation proposee pourrait constituer un autre choix que l'equation actuelle de cisaillement par poinconnement utilisee dans le code de calcul CSA-A23,3-04. Mots-cles : resistance du beton, pourcentage d'armature, effet de dimensionnement, base de donnees, analyse statistique, regression, ductilite, poinconnement. [Traduit par la Redaction], Introduction The two-way slab system is a unique efficient structural system. It is economical and is widely used in different structural applications such as floors, roofs of buildings, and walls [...]

The current review summarizes the known synthetic routes of fused imidazopyrazoles. This review is classified into two main categories based on the type of annulations, for example, annulation of the imidazole ring onto a pyrazole scaffold or annulation of the pyrazole ring onto an imidazole scaffold. Some medicinal applications of imidazopyrazoles are mentioned.

The strut-and-tie method is a rational approach to structural concrete design that results in a uniform and consistent design philosophy. A strut-and-tie model has been developed to model the punching-shear behaviour of thick concrete plates. This model provides a quick and simple approach to check the punching-shear behaviour. Thick concrete slabs (250-500 mm) without shear reinforcement can exhibit brittle shear failure under a central force and an unbalanced moment. Shear reinforcement has proven to be very effective in preventing such failures. The developed strut-and-tie model has also been used to evaluate the minimum shear reinforcement required to prevent brittle shear failure of two-way slabs in the vicinity of concentrated loads. The strut-and-tie model for symmetric punching consists of a 'bottle-shaped' compressive zone in the upper section of the slab depth, leading to a 'rectangular-stress' compressive zone in the lower section of the slab depth. Inclined shear cracking develops in the bottle-shaped zone prior to failure in the lower zone. Cracking in the bottle-shaped zone is related to the splitting tensile strength of concrete. Key words: thick plates, strut-and-tie model, shear reinforcement, size effect, splitting bond stress, punching, bottle-shaped strut. La methode de modele a treillis est une approche rationnelle au calcul du beton structural qui resulte en une philosophie de conception uniforme et constante. Un modele a treillis a ete developpe pour simuler le comportement en cisaillement par poinconnement de plaques de beton epaisses. Ce modele represente une approche rapide et simple de verifier le comportement en cisaillement par poinconnement. Les dalles de beton epaisses (250-500 mm) sans armature contre le cisaillement peuvent montrer une rupture fragile en cisaillement sous une force centrale et un moment non equilibre. L'armature contre le cisaillement s'est montree tres efficace pour prevenir de telles ruptures. Le modele a treillis developpe aegalement ete utilise; pour eevaluer l'armature minimale requise contre le cisaillement afin d'empeecher la rupture fragile en cisaillement dans les dalles bidirectionnelles pres des charges concentrees. Le modele a treillis pour determiner le poinconnement symeetrique consiste en une zone de compression en << forme de bouteille >> dans la section superieure de la dalle, engendrant une zone de compression de << contrainte rectangulaire >> dans la section inferieure. Une fissuration de cisaillement inclineeese developpe dans la zone en forme de bouteille avant la rupture dans la zone inferieure. La fissuration dans la zone en forme de bouteille est associeeea la resistance du beton a la traction par fendage. Mots-cles: plaques epaisses, modele a treillis, armature contre le cisaillement, effet de taille, contrainte d'adheerence en fendage, poinconnement, entretoise en forme de bouteille. [Traduit par la Redaction], Introduction Thick concrete slabs (250-500 mm) without shear reinforcement usually exhibit brittle shear failure under a central force and an unbalanced moment that is transferred between the column and the [...]

The central pyrazole ring in the title compound, C17H16FN3S, adopts an envelope conformation with the methine C atom bearing the 4-fluorophenyl substituent as the flap atom. Whereas the tolyl ring is slightly twisted out of the least-squares plane through the pyrazole ring [dihedral angle = 13.51 (11)°], the fluorobenzene ring is almost perpendicular [dihedral angle = 80.21 (11)°]. The thioamide group is almost coplanar with the N—N bond of the ring [N—N—C—N torsion angle = 1.2 (3)°] and the amine group forms an intramolecular hydrogen bond with a ring N atom. In the crystal, supramolecular double layers in the bc plane are formed via N—H...S, N—H...F and C—H...F interactions.

A novel series of dihydropyrimidines (DHPMs) 4a–j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC50 values ranging from 0.014–5.87 μg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ).

CDK2, which exhibits an indispensable role as an organizer of cell growth, is the powerfully studied protein Kinases objective of anticancer suppressors. The present study was dedicated to design (pharmacophore, docking, and binding energy) and to prepare an inspired derivatives of pyrazole and pyrazolo[1,5-d]pyrimidine as promising anticancer agents, which can act by targeting CDK2. The promising compounds were selected according to their fit-value and binding energy scores. The anticancer activity against MCF-7 was tested for the prepared compounds and compounds 2, 3b, and 7b showed expressive activity with IC50 1.75, 0.89 and 1.32 µM respectively. The CDK2 evaluation was carried out to estimate the efficiency of the prepared compounds as promising inhibitors. The results revealed that compound 3b with effective inhibitory activity against tumor growth and with its potent inhibition against the CDK2 enzyme with percent inhibition 86 would be a prospective anticancer agent. The prepared compounds with high biological activity could be used as lead inhibitors for the CDK2 kinase domain. [ABSTRACT FROM AUTHOR]