Abstract: The state of Goiás, in central Brazil, is covered mainly by the Cerrado domain, with the Alto Paraná Atlantic Forest occupying its central-southern portion. Goiás is one of the 20 Brazilian federative units without a mammal checklist. In this study, we provide the first checklist of mammals from Goiás state. We recorded mammal species based primarily on the analysis of specimens housed in scientific collections as well as on literature with associated voucher material. We listed 191 mammalian species belonging to 125 genera, 31 families and 10 orders, which represents 25.2% of the mammal species occurring in Brazil. The most speciose orders were Chiroptera (90 spp.), followed by Rodentia (43 spp.), Carnivora (19 spp.) and Didelphimorphia (17 spp.). The following orders accounted for a smaller portion of the state diversity: Cetartiodactyla (7 spp.), Cingulata (7 spp.), Primates (4 spp.), Pilosa (2 spp.), Lagomorpha (1 sp.), and Perissodactyla (1 sp.). A total of 28 species (14.7%), mainly represented by medium and large-sized mammals, are nationally threatened while 12 (6.3%) are globally threatened. Our results indicate great portions of the state lacking a proper survey of mammals, especially the northwestern portion. We discuss species richness, distribution and conservation status of the mammals of Goiás state in national and regional scenarios. We highlight the need for mammal inventories based on complementary survey techniques with the collection of vouchers in order to provide karyologic, molecular, morphologic, parasitologic, and ecological data. These informations are the basis for integrative studies that lead to the understanding of current mammalian richness and diversity. Indeed, knowledge on species richness distribution in the state will guide conservation strategies, especially in areas undergoing habitat loss and fragmentation, such as the central-southern portion of Goiás.
Resumo: O estado de Goiás, no Brasil central, é coberto principalmente pelo domínio do Cerrado, com a Mata Atlântica do Alto Paraná ocupando sua porção centro-sul. Goiás é uma das 20 unidades federativas brasileiras que ainda não possui uma lista de espécies de mamíferos. Neste estudo, apresentamos a primeira lista de mamíferos para o estado. Registramos as espécies de mamíferos com base principalmente na análise de espécimes depositados em coleções científicas, bem como na literatura apresentando material testemunho associado. Listamos 191 espécies pertencentes a 125 gêneros, 31 famílias e 10 ordens, as quais representam 25,2% das espécies de mamíferos que ocorrem no Brasil. As ordens mais especiosas foram Chiroptera (90 spp.), seguida pelas ordens Rodentia (43 spp.), Carnivora (19 spp.) e Didelphimorphia (17 spp.), com as demais ordens respondendo por uma porção menor da diversidade: Cetartiodactyla (7 spp.), Cingulata (7 spp.), Primates (4 spp.), Pilosa (2 spp.), Lagomorpha (1 sp.) e Perissodactyla (1 sp.). Um total de 28 espécies (14,7%), principalmente representadas por mamíferos de médio e grande porte, estão ameaçadas nacionalmente e 12 (6,3%) encontram-se globalmente ameaçadas. Nossos resultados indicaram grandes porções do estado ainda não devidamente pesquisadas em relação aos seus mamíferos, com informações escassas e fragmentadas, principalmente no que diz respeito à sua porção noroeste. Discutimos a riqueza de espécies, a distribuição e o estado de conservação dos mamíferos do estado de Goiás nos cenários nacional e regional. Ressaltamos a importância da realização de inventários que utilizem técnicas complementares de amostragem, incluindo a coleta de material testemunho, proporcionando a obtenção de dados cariotípicos, moleculares, morfológicos, parasitológicos e ecológicos. Estas informações são a base de estudos integrativos, os quais aumentam nossa compreensão a respeito da riqueza e diversidade atual dos mamíferos. O conhecimento a respeito da distribuição da riqueza de espécies em Goiás é essencial para embasar estratégias de conservação, tão necessárias em áreas que vem sofrendo com a perda e fragmentação de seus hábitats naturais, como a porção centro-sul do estado.
Micelles have aroused interest due to their ability to assist in the transport of poorly soluble drugs. In this study the mixture of copolymers F127/E45S8 in different proportions (F/ES 30/70, 50/50 and 70/30) was performed to improve the bioavailability of griseofulvin and quercetin. The results of cytotoxicity (MTT assay) revealed that the copolymers F127 and E45S8 had considerable biocompatibility and did not affect the metabolism of human neutrophils. The binary systems were also evaluated by critical micellar concentration (CMC) and thermoresponsive behavior. The CMC values were intermediate to those of the isolated copolymers. The systems maintained the thermoresponsive properties present in F127 making the systems interesting for subcutaneous administration. The systems presented small size, an average range in size from 17 to 38 nm, and the samples prepared with higher hydrophobic proportion presented more uniform sizes. Results suggest stability and the increasing of the nanosystems circulation time. The F/ES 30/70 system has polydispersity smaller than 0.1 and showed an increase of 129 times for quercetin solubility. Thus, it is possible to consider F127/E45S8 micelles as potential nanosystems for poorly soluble drug delivery.
In this work, it is described the design of twenty-four heterocyclic amine-azachalcones compounds through molecular hybridization of chalcone scaffold and fragments of isoniazid, fluoroquinolones, and linezolid with antituberculosis potential. The new compounds were synthesized via Claisen-Schmidt condensation, providing yields of 36-95%. Fifteen compounds showed antituberculosis activity against Mycobacterium tuberculosis H37Rv strain. Two amine-azachalcones 15 and 17 showed relevant biological activity with minimum inhibitory concentration (MIC) values of 6.62 and 4.85 µM, respectively. Compound 12 showed the best profile of antitubercular activity with MIC = 9.54 µM and selectivity index (SI) = 9.33. It was found that morpholine group is important to increase potency of antimycobacterial activity but also to add some toxicity to the chalcone molecular framework. The results described herein would be a guide in the designing of novel and optimized antitubercular derivatives based on the chalcone scaffold.
ABSTRACT This study assessed the fitting of mathematical models to the convective drying kinetics of osmotically pre-dehydrated papaya cubes. Papaya cubes were subjected to osmotic dehydration in sucrose solutions at 40 and 50 ºBrix, at temperatures of 50 and 60 ºC, followed by complementary convective drying in forced air circulation oven under three temperatures (50, 60 and 70 °C) and constant air velocity of 1.0 m s-1. Ten thin-layer drying mathematical models were fitted to the experimental data. The increase in air temperature and the decrease in osmotic solution concentration resulted in increased water removal rate. Based on the statistical indices, the Two Terms model was the one that best described the drying kinetics of the samples for all evaluated conditions. The effective diffusion coefficients increased with the elevation of air temperature, ranging from 1.766 x 10-10 to 3.910 x 10-6 m2 s-1, whereas the convective mass transfer coefficients ranged from 3.910 x 10-7 to 1.201 x 10-6 m s-1 with Biot number from 0.001 to 12.500.
RESUMO Este estudo avaliou o ajuste de modelos matemáticos na cinética de secagem convectiva de cubos de mamão pré-desidratados osmoticamente. Os cubos de mamão foram submetidos à desidratação osmótica em soluções de sacarose a 40 e 50 ºBrix, em temperaturas de 50 e 60 ºC, seguida de secagem convectiva complementar em estufa com circulação forçada de ar sob três temperaturas (50, 60 e 70 °C) e velocidade do ar constante de 1,0 m s-1. Aos dados experimentais foram ajustados dez modelos matemáticos de secagem em camada fina. O aumento da temperatura do ar e a diminuição da concentração da solução osmótica resultou em aumento da taxa de remoção de água. Com base nos índices estatísticos, o modelo de Dois Termos foi o que melhor descreveu a cinética de secagem das amostras para todas as condições avaliadas. Os coeficientes de difusão efetivos aumentaram com a elevação da temperatura do ar, variando de 1,766 x 10-10 a 3,910 x 10-6 m2 s-1, enquanto os coeficientes convectivos de transferência de massa variaram entre 3,910 x 10-7 a 1,201 x 10-6 m s-1 com número de Biot de 0,001 a 12,500.
RESUMEN Se evaluó el efecto de la inclusión de Vitafert (0 y 1 %) y tubérculos de boniato (0, 5, 10 y 15 %), en el valor nutritivo de ensilajes mixtos de C. purpureus vc. CUBA CT-169 y M. oleifera. No se apreció diferencias en el contenido de materia seca, proteína bruta, y fibra detergente neutro de los ensilajes evaluados (P>0.05). La materia orgánica fue mayor al 85% y solo difirió entre control y tratamiento con 10% de boniato (P<0.05). Ambos aditivos incrementaron la producción de ácido acético respecto al control (P<0.0001). Solo el ensilaje con Vitafert y 15% de boniato redujeron los niveles de NH3 respecto al control (P< 0.001). En la producción de gas hubo interacción entre los dos factores en la primera fase de la fermentación (P < 0.05). En los tres primeros horarios de la fase inicial, el ensilaje con Vitafert produjo más gas que el control, pero no mostró diferencias respecto al resto, excepto a las dos horas. En la fase final de la fermentación no hubo interacción entre tratamientos y horarios (P>0.05), y los aditivos mejoraron la producción de gas (P< 0.0001). Hubo una tendencia al incremento en el potencial de producción de gas y Vmáx, al incluir Vitafert e incrementar los niveles de tubérculo. La inclusión de aditivos disminuyó NH3 e incrementó ácidos acético y butírico, así como AGCC totales, EM y DMO (P<0.01). Se incrementó la DIVMS al incluir boniato (P<0.0001). Se concluye que los aditivos Vitafert y tubérculo de boniato, a las concentraciones evaluadas, no influyeron significativamente en la composición química de los ensilados mixtos pero ambos aditivos mejoraron las características fermentativas de los ensilajes al reducir los niveles de ácido butírico e incrementar propiónico. De igual manera, su uso optimizó el comportamiento de los parámetros cinéticos de la fermentación in vitro e incrementó la producción de gas y AGCC individuales y totales, la DIVMS, EM y DMO, con un efecto positivo del nivel de inclusión del boniato en varios de estos indicadores.
ABSTRACT The effect of including Vitafert (0 and 1 %) and sweet potato (0, 5, 10 and 15 %) on the nutritional value of mixed silages of C. purpureus cv. CUBA CT-169 and M. oleifera was evaluated. There were no differences on dry matter content, crude protein, and neutral detergent fiber of evaluated silages (P>0.05). Organic matter was superior to 85% and differed between control and treatment with 10% of sweet potato (P< 0.05). Both additives increased the production of acetic acid regarding control (P< 0.0001). Only silage with Vitafert and 15% of sweet potato reduced levels of NH3 regarding control (P<0.001). In gas production, there was interaction between the two factors in the first stage of fermentation (P< 0.05). In the first three times of the initial phase, silage with Vitafert produced more gas than control, but there were no differences regarding the rest, except at 2 h. In the final stage of fermentation, there was no interaction between treatments and times. There was a tendency to increase the potential of gas production and Vmax, with the inclusion of Vitafert and increase of tuber levels. The inclusion of additives decreased NH3 levels and increased acetic and butyric acids, as well as SCFAs, ME and OMD (P< 0.01). The IVDDM increased with the inclusion of sweet potato (P< 0.0001). It can be concluded that Vitafert and sweet potato additives, at the evaluated concentrations, had no significant influence on chemical composition of mixed silages but both additives improved the fermentative characteristic of silages by reducing the levels of butyric acid and increasing propionic acid levels. Likewise, its use optimized the performance of kinetic parameters of in vitro fermentation and increased gas production, total and individual SCFAs, IVDDM, ME and OMD, having a positive effect of sweet potato inclusion level on several of these indicators.
Derivatives of the thiazolidine-2,4-dione core represent a heterocyclic class with several correlated properties. In this context, the synthesis of structural analogues of these bioactive substances becomes attractive in the field of medicinal chemistry. These analogues act as antimicrobial agents against Gram-positives pathogens. The present work aimed to synthesize 10 different derivatives of 5-arylidene-thiazolidine-2,4-dione, employing urea as the catalyst in a solvent-free reaction medium, with yields that ranged from 45 to 99%. The compounds obtained were submitted to an antimicrobial assay against S. aureus ATCC 29213. Two compounds presented minimum inhibitory concentration of 62.5 and 32.5 µg mL-1 and minimum bactericidal concentration < 500 µg mL-1, demonstrating their antibacterial potential. Principal component analysis was carried out to discriminate the compounds in active and inactive classes. Four geometric and electronic molecular descriptors were required to completely discriminate the compounds. The selected descriptors can guide us in designing new 5-arylidene-thiazolidine-2,4-dione derivatives with enhanced activity.
Abstract: Several microbiological indicators of soil quality present high sensitivity, but little is known about the influence of topographic factors on them. This work aimed to evaluate variability of biological indicators of soil quality across a hillslope under native forest and the influence of topographic factors on them. Four positions on a hillslope were evaluated. Activity of the enzymes β-glucosidase, acid phosphatase, urease and fluorescein diacetate (FDA) hydrolysis were determined, as well as basal and substrate-induced respiration, and density of microorganisms: total bacteria, total fungi, actinobacteria, phosphate solubilizers, ammonifiers, native rhizobia, free-living N2-fixing bacteria, spores of arbuscular mycorrhizal fungi and percentage of root colonization by arbuscular mycorrhizal fungi. Activity and density of microorganisms were correlated with topographic factors. The relation of these factors to the variations of the evaluated indicators was determined using the random forest algorithm. Microbiological indicators varied according to the hillslope positions. The indicators urease, basal respiration, spore density, mycorrhizal colonization, total bacteria and fungi, phosphate solubilizers, and free-living N2-fixing bacteria detected in JNFB and FAM culture medium did not vary with terrain attributes and were therefore more indicated in cases of topographic variations. This and future studies can help to select the best microbiological indicators for different conditions.
ABSTRACT N-acylhydrazone is an interesting privileged structure that has been used in the molecular design of a myriad of bioactive compounds. In order to identify new antinociceptive drug candidates, we described herein the design, synthesis, X-ray diffraction study and the pharmacological evaluation of a series of 3-amino-4-methylthiophene-2-acylcarbohydrazone derivatives (8a-t). Compounds were prepared in good overall yields through divergent synthesis from a common key intermediate and were characterized by classical spectroscopy methods. X-ray diffraction study was employed for unequivocal determination of the imine double bond stereochemistry. 8a-t were evaluated in vivo through oral administration using the classical writhing test in mice. N-acylhydrazone derivatives 8j and 8l displayed relative potency similar to dipyrone, highlighting them as promising analgesic lead-candidates for further investigation.
Abstract Impaired wound healing represents a serious complication in some pathologies and the use of plant extracts has proved to improve tissue repair. The objectives of this study were to evaluate the healing potential of the ointment of Sebastiana hispida compared with Aluminum-Gallium Indium-Phosphide Laser (InGaAlP) in surgically induced wounds in rats and to perform the phytochemical analysis. The phytochemical analysis was performed in the classic way and also by HPLC. A controlled study was developed with 80 rats (200-250 g) in which a linear excision was performed in the dorsal region after shaving, measuring 2 cm × 1 cm (epidermis and dermis) exposing the muscle fascia. The rats were randomly divided into four groups of twenty animals each. The experimental groups (n = 5) were G1 (Saline); G2 (crude methanol plant extract 2% + Carbopol Gel 98%); G3 (crude methanol plant extract 2% + lanolin/vaseline) and G4 (laser). The incision healing processes were monitored during 3, 7, 14 and until 21 days after excision. The histologic parameters evaluated were Collagen fiber types, microscopic examination and neovascularization. There was a significant increase in the deposition of collagen fibers, as evidenced by a better organized epithelial tissue, keratinized and showing greater proliferation of new blood vessels in the inflammatory phase in the group treated with both the extract and laser. The results were correlated to the phenolic derivatives found after qualitative and quantitative analysis. These compounds were considered responsible for the healing process. The topical treatment with S. hispida leaves, in the two different formulations, was more effective than the application of the laser (Ingan ALP) 660 nm in the model used.
Resumo A cicatrização deficiente representa uma complicação grave em algumas patologias e o uso de extratos de plantas tem demonstrado melhora no processo de reparação tecidual. O objetivo deste estudo foi avaliar o potencial cicatrizante da pomada de Sebastiania hispida comparado ao Laser Indio Phosphide-Gallium-Aluminum (InGaAlP) em feridas cutâneas induzidas cirurgicamente em ratos e realizar analise fitoquímica. A análise fitoquímica foi via clássica e por CLAE. O experimento foi desenvolvido com 80 ratos (200-250 g), divididos aleatoriamente em quatro grupos (n = 5): G1 (salina); G2 (extrato bruto metanólico 2% + Carbopol Gel 98%); G3 (extrato bruto metanólico 2% + lanolina/vaselina) e G4 (laser). Após a tricotomia da região dorsal realizou uma excisão linear, medindo 2 cm × 1 cm (epiderme e derme), expondo a fáscia muscular. Em sequência os tratamentos e o monitoramento do processo de cicatrização das feridas cirúrgicas ocorreu nos tempos de: 3, 7, 14 e até 21 dias após a excisão. Os parâmetros histológicos avaliados foram: tipos de fibras colágenas, avaliação morfológica e neovascularização. Houve uma deposição significativa de fibras colágenas, evidenciado por um tecido epitelial mais bem organizado, queratinizado e mostrando uma maior proliferação de novos vasos sanguíneos na fase inflamatória do grupo tratado com o extrato e o laser. A eficiência do processo de cicatrização pode estar relacionada com a presença de compostos fenólicos e derivados detectados na análise qualitativa e quantitativa. A utilização do tratamento tópico com as duas formulações diferentes de S. hispida foram mais eficazes do que a aplicação do Laser (InGaAlP) no modelo utilizado.
Abstract Streptococcus agalactiae is one of the most common pathogens leading to mastitis in dairy herds worldwide; consequently, the pathogen causes major economic losses for affected farmers. In this study, multilocus sequence typing (MLST), genotypic capsular typing by multiplex polymerase chain reaction (PCR), and virulence gene detection were performed to address the molecular epidemiology of 59 bovine (mastitis) S. agalactiae isolates from 36 dairy farms located in the largest milk-producing mesoregions in Brazil (Minas Gerais, São Paulo, Paraná, and Pernambuco). We screened for the virulence genes bac, bca, bibA, cfb, hylB, fbsA, fbsB, PI-1, PI-2a, and PI-2b, which are associated with adhesion, invasion, tissue damage, and/or immune evasion. Furthermore, five capsular types were identified (Ia, Ib, II, III, and IV), and a few isolates were classified as non-typeable (NT). MLST revealed the following eight sequence types (STs): ST-61, ST-67, ST-103, ST-146, ST-226, ST-314, and ST-570, which were clustered in five clonal complexes (CC64, CC67, CC103, CC17, and CC314), and one singleton, ST-91. Among the virulence genes screened in this study, PI-2b, fbsB, cfb, and hylB appear to be the most important during mastitis development in cattle. Collectively, these results establish the molecular epidemiology of S. agalactiae isolated from cows in Brazilian herds. We believe that the data presented here provide a foundation for future research aimed at developing and implementing new preventative and treatment options for mastitis caused by S. agalactiae.
Alkyl polyglycosides (APGs) are new biodegradable surfactants, non-toxic, synthesized from abundant renewable sources, potentially more appropriate than anionic surfactants. A range of glycosides denoted APG-Cy was synthesized by the Köenig-Knorr reaction using C10, C16 and C18 alcohols and derived from the degradation of amylose from English potato. The molecular structures of the glycosides were characterized by Nuclear Magnetic Resonance (1H and 13C NMR) together with Infrared Spectroscopy (FTIR) and Gel Permeation Chromatography (GPC). The study by NMR allowed the junctions between hydrophilic head groups and hydrophobic tail-groups to be characterized in detail. Conformation of the glycosidic units is 4C1 type with a b anomeric configuration. The formation of glycosides with five glucose rings linked to the alkyl chain was confirmed by 1H NMR and GPC. Liquid crystals identified by the presence of double melting points were observed by Differential Scanning Calorimetry (DSC) showing thermotropic properties. The surface tension (γ) and critical micelle concentration (cmc) were determined by du Noüy method, noting that increasing the length of alkyl chain led to the expected reduction in the cmc. The energies of adsorption and micellization processes calculated from isotherms γ versus ln c (g.dm-3) indicate cooperativeness of hydrophilic and hydrophobic groups.
Abstract Osteoporosis, a metabolic disease characterized by low bone mass, deterioration of the bone tissue microarchitecture and increased susceptibility to fractures, is commonly regarded as a women's health problem. This point of view is based on the fact that compared with men, women have lower bone mineral density and longer lifespans and lose bone mass faster, especially after menopause, due to a marked decrease in serum estrogen levels. However, in the last 20 years, osteoporosis in men has become recognized as a public health problem due to the occurrence of an increasingly higher number of fragility fractures. Approximately 30% of all hip fractures occur in men. Recent studies show that the probability of fracture due to hip, vertebral or wrist fragility in Caucasian men older than fifty years, for the rest of their lives, is approximately 13% versus a 40% probability of fragility fractures in women. Men show bone mass loss and fractures later than women. Although older men have a higher risk of fracture, approximately half of all hip fractures occur before the age of 80. Life expectancy is increasing for both sexes in Brazil and worldwide, albeit at a higher rate for men than for women. This Guideline was based on a systematic review of the literature on the prevalence, etiology, diagnosis and treatment of osteoporosis in men.
Resumo Osteoporose, uma doença metabólica caracterizada por baixa massa óssea, deterioração da microarquitetura do tecido ósseo e aumento da suscetibilidade a fraturas, é comumente vista como um problema de saúde feminino. Essa visão tem fundamentos: em comparação com os homens as mulheres têm densidade mineral óssea menor, têm vida mais longa e perdem massa óssea mais rapidamente, principalmente após a menopausa, devido à diminuição acentuada dos níveis séricos de estrógeno. Entretanto, nos últimos 20 anos a osteoporose no homem tem sido reconhecida como um problema de saúde pública devido à ocorrência cada vez maior de fraturas por fragilidade. Cerca de 30% de todas as fraturas de quadril ocorrem em homens. Estudos recentes mostram que a probabilidade de fratura por fragilidade do quadril, vértebra ou punho em homens brancos após os 50 anos, pelo resto de suas vidas, situa-se em torno de 13%, 40% nas mulheres. Os homens apresentam perda de massa óssea e fraturas mais tardiamente do que as mulheres. Embora os homens mais idosos tenham maior risco de fratura, cerca de metade das fraturas de quadril ocorre antes dos 80 anos. A expectativa de vida tem aumentado para ambos os sexos no Brasil e em todo o mundo, porém em uma velocidade maior para homens do que para mulheres. Esta Diretriz foi baseada em uma revisão sistemática da literatura com relação a prevalência, etiologia, diagnóstico e tratamento da osteoporose em homens.
ABSTRACT Piperaceae species can be found worldwide in tropical and subtropical areas and many of them have been used for centuries in traditional folk medicine and in culinary. In Brazil, species of Piperaceae are commonly used in some communities as local anesthetic and analgesic. Countrified communities have known some species of the genus Ottonia as "anestesia" and it is a common habit of chewing leaves and roots of Ottonia species to relief toothache. The purpose of this study is to report our findings on new molecules entities obtained from the roots of Ottonia anisum Spreng, in which local anesthetic activity (sensory blockage) is demonstrated for the first time in vivo guinea pig model. Phytochemical investigation led to the isolation of three amides (pipercallosidine, piperine and valeramide) and in an enriched mixture of seven amides (valeramide, 4,5-dihydropiperlonguminine, N-isobutil-6-piperonil-2-hexenamide, piperovatine, dihydropipercallosidine, pipercallosidine and pipercallpsine). Our findings demonstrated the anesthetic potential for the methanolic extract from roots, its n-hexane partition and amides from O. anisum and it is in agreement with ethnobotanical survey.
A series of β-carboline derivatives with amino or guanidinium were synthesized and evaluated in vitro against anti-Mycobacterium tuberculosis and for antiproliferative activities against nine human cancer cell lines. The compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline (24.9 µg mL-1) and 1-(4-methoxyphenyl)-3-carboxamide(ethylamine) β-carboline (26.9 µg mL-1) were the most active against M. Tuberculosis (MTB). Compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline and 1-(4-methoxyphenyl)-3-carboxamide(propylamine) β-carboline, which had the same substituted groups, inhibited the growth of all human tumor cell lines with growth inhibitory activity (GI50) values from 1.37 to 9.20 mmol L-1. Also in this series, compounds 1-(4-hydroxyphenyl)-3-carboxamide(propylamine) β-carboline and 1-(3-nitrophenyl)-3-carboxamide(propylamine) β-carboline demonstrated significant activity against NCI/ADR cells. Among compounds with a terminal guanidine group, compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethyl)guanidine β-carboline (27.8 µg mL-1) and 1-(3-nitrophenyl)-3-carboxamide(ethyl)guanidine β-carboline (37.4 µg mL-1) demonstrated the greatest activity against MTB. Additionally, compounds 1-(4-methoxyphenyl)-3-carboxamide(ethyl)guanidine β-carboline (GI50 = 0.45 mmol L-1) effectively inhibited growth and was highly selective against NCI/ADR. The in silico study revealed that 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline, 1-(4-methoxyphenyl)-3-carboxamide(ethylamine) β-carboline, 1-(4-hydroxyphenyl)-3-carboxamide(propylamine) β-carboline, 1-(4-methoxyphenyl)-3-carboxamide(propylamine) β-carboline and 1-(3-nitrophenyl)-3-carboxamide(propylamine) β-carboline compounds follow the rules established by Lipinski, suggesting that this compound has no problems with oral bioavailability.